DNA/RNA Synthesis

Choose Selective DNA/RNA Synthesis Inhibitors

DNA/RNA Synthesis Signaling Pathway Map

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Products

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  • DNA/RNA Synthesis Inhibitors (111)
  • DNA/RNA Synthesis Antibodies (8)
  • DNA/RNA Synthesis Activators (5)
  • DNA/RNA Synthesis Antagonists (1)
  • DNA/RNA Synthesis Modulators (3)
  • New DNA/RNA Synthesis Products
Catalog No. Product Name Information Product Use Citations Product Validations
S0054 D-I03 D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively.
S0063 RG3039 RG3039 (PF-06687859, PF 6687859, Quinazoline 495) is an orally bioavailable and brain-penetrant inhibitor of the mRNA decapping enzyme DcpS with IC50 of 4.2 nM and IC90 of 40 nM, respectively.
S0102 L 189 L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage.
S0161 ML367 ML367 is a potent, micromolar inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization. ML367 blocks DNA repair pathways and general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
S0280 Madrasin Madrasin (DDD00107587) is a potent and cell-penetrant pre-mRNA splicing inhibitor. Madrasin interferes with the early stages of spliceosome assembly and stalls spliceosome assembly at the A complex.
S0469 ML216 ML216 (CID-49852229) is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM636-1298 and BLMfull-length, respectively.
S0780 Oncrasin-1 Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
S0816 Brr2 Inhibitor C9 Brr2 inhibitor C9 (Brr2 Inhibitor 9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa a group of progressive retinal degenerative disorders.
S1117 Triciribine (NSC 154020) Triciribine (NSC 154020, VD-0002, vqd-002, API-2, TCN) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.
Aging (Albany NY), 2021, 13(5):7096-7119
Int J Mol Sci, 2021, 22(14)7660
J Leukoc Biol, 2021, 10.1002/JLB.1A0920-588R
S1135 Pemetrexed (LY-231514) disodium Pemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S1149 Gemcitabine (LY-188011) HCl Gemcitabine (LY-188011, NSC 613327) HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.
Cell, 2021, 184(25):6119-6137.e26
Nat Commun, 2021, 12(1):4917
Nat Commun, 2021, 12(1):1602
S1156 Capecitabine (RO 09-1978) Capecitabine (RO 09-1978) is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis.
Adv Sci (Weinh), 2021, e2103360
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1166 Cisplatin (NSC 119875) Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP) is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy. Solutions are best fresh-prepared.
Cancer Cell, 2021, S1535-6108(21)00659-0
Nat Commun, 2021, 12(1):5404
Nat Commun, 2021, 12(1):7064
S1192 Raltitrexed Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.
Cell, 2021, 184(2):334-351.e20
Cancers (Basel), 2021, 13(9)2061
Anal Chem, 2020, 10.1021/acs.analchem.0c02756
S1199 Cladribine (RWJ 26251) Cladribine (RWJ 26251, Leustatin, 2-CdA, 2-chlorodeoxyadenosine, 2-Chloro-2′-deoxyadenosine, CldAdo, Jk 6251, NSC 105014) is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
Neoplasia, 2021, 23(12):1183-1191
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1209 Fluorouracil (5-Fluorouracil, 5-FU) Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.
Cell, 2021, 184(25):6119-6137.e26
Sci Adv, 2021, 7(36):eabh1684
Nat Commun, 2021, 12(1):4840
S1213 Nelarabine Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
World Scientific, 2021, Vol. 20, No. 03, pp. 305-322
S1215 Carboplatin (NSC 241240) Carboplatin (NSC 241240, JM-8, CBDCA) is a DNA synthesis inhibitor by binding to DNA and interfering with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. Solutions are best fresh-prepared.
Cancer Cell, 2021, S1535-6108(21)00659-0
Nat Commun, 2021, 12(1):3636
Cell Rep, 2021, 34(10):108814
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
iScience, 2021, 24(9):103080
S1221 Dacarbazine (NSC-45388) Dacarbazine (NSC-45388, DTIC-Dome, Imidazole Carboxamide) is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers.
Cancer Res, 2021, 81(23):6044-6057
Biochem Biophys Res Commun, 2021, 557:213-220
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1224 Oxaliplatin (NSC 266046) Oxaliplatin (NSC 266046, L-OHP, Eloxatin) is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells. DMF is recommended for dissolution. Solutions are best fresh-prepared.
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, e2103360
S1229 Fludarabine Phosphate Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
Aging (Albany NY), 2021, 13(8):12160-12178
Int J Mol Sci, 2021, 22(16)8864
Lab Invest, 2021, 10.1038/s41374-021-00703-5
S1289 Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.
Cancer Cell, 2021, S1535-6108(21)00659-0
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1299 Floxuridine (NSC 27640) Floxuridine (NSC 27640, Deoxyfluorouridine, FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV.
Cell Chem Biol, 2021, S2451-9456(21)00306-8
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1300 Tegafur (FT-207) Tegafur (FT-207, NSC 148958) is a substance being used in the treatment of some types of cancer.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cancer Cell Int, 2020, 19;20:58
S1302 Ifosfamide (NSC109724) Ifosfamide (NSC109724, Isophosphamide) is a nitrogen mustard alkylating agent used in the treatment of cancer.
Cancer Cell Int, 2021, 21(1):646
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1305 Mercaptopurine (6-MP) Mercaptopurine is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
Theranostics, 2021, 11(9):4011-4029
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1373 Daptomycin (LY146032) Daptomycin (LY146032) is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.
J Phys Chem B, 2021, 125(22):5775-5785
Sci Adv, 2020, 6(34):eaba8968
Front Microbiol, 2020, 21;11:646
S1384 Mizoribine Mizoribine (Bredinin, NSC 289637) is an imidazole nucleoside and an immunosuppressant that inhibits HCV RNA replication with IC50 of ~ 100 μM for anti-HCV activity. Mizoribine is a selective inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase. Mizoribine also inhibits SARS-CoV.
Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
JCI Insight, 2020, 9;5(7):e135071
S1491 Fludarabine (NSC 118218) Fludarabine (NSC 118218, FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.
Cell Metab, 2021, 33(1):110-127.e5
Cell Rep, 2021, 34(1):108584
Cell Rep, 2021, 34(1):108584
S1516 Cidofovir Cidofovir (HPMPC) suppresses virus replication by selective inhibition of viral DNA synthesis.
Oncol Lett, 2021, 21(4):280
Nat Biotechnol, 2019, 37(3):303-313
J Virol, 2019, 93(4)
S1648 Cytarabine (U-19920A) Cytarabine (U-19920A, Cytarabin, Ara-C, Arabinofuranosyl Cytidine, Cytosine β-D-arabinofuranoside, Cytosine arabinoside, NSC 63878, NSC 287459) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
Leukemia, 2021, 10.1038/s41375-021-01361-8
Blood Cancer J, 2021, 11(6):111
Cell Rep, 2021, 36(7):109559
S1714 Gemcitabine (LY-188011) Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Nat Commun, 2021, 12(1):1602
Cancer Res, 2021, canres.1337.2021
Cell Rep, 2021, 34(10):108814
S1760 Rifapentine Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.
Front Microbiol, 2020, 10:2936
mSphere, 2018, 3(5)
S1764 Rifampin (NSC-113926) Rifampin (NSC-113926, Rimactane, Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Front Oncol, 2021, 11:715193
PLoS One, 2021, 16(11):e0260633
Pharmacogenomics J, 2020, 10.1038/s41397-020-0160-7
S1778 Trifluridine (NSC 75520) Trifluridine (NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.
Cell Chem Biol, 2021, S2451-9456(21)00261-0
Sci Adv, 2020, 6(49)eabd9443
Ocul Surf, 2019, 10.1016/j.jtos.2019.11.011
S1784 Vidarabine Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.
Neuron, 2017, 96(6):1290-1302
ACS Appl Mater Interfaces, 2016, 8(39):25818-25824
Biogerontology, 2016, 17(5-6):907-920
S1790 Rifaximin Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria.
S1807 Aciclovir (BW 248U) Acyclovir (BW 248U, Acyclovir, Acycloguanosine, Zovirax, ACV, NSC 645011) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells.
Microbiol Spectr, 2021, 9(3):e0064621
Front Microbiol, 2021, 12:722748
Vet Microbiol, 2021, 265:109313
S1826 Nedaplatin Nedaplatin is a derivative of cisplatin and DNA damage agent for tumor colony forming units with IC50 of 94 μM.
Nat Commun, 2019, 10(1):5654
Cancer Res, 2018, 78(19):5694-5705
Oncol Lett, 2016, 12(5):4195-4202
S1896 Hydroxyurea (NSC-32065) Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
Nat Commun, 2021, 12(1):5572
Cancer Res, 2021, canres.3761.2020
Cell Death Dis, 2021, 12(2):183
S1907 Metronidazole Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa.
Elife, 2021, 10e69795
Bone Joint Res, 2020, 16;9(4):152-161
S1949 Menadione (NSC 4170) Menadione (NSC 4170, Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
Mol Cell, 2021, S1097-2765(21)00269-0
DNA Repair (Amst), 2021, 105:103152
BMC Urol, 2021, 21(1):96
S1973 Cyclocytidine HCl Cyclocytidine (NSC 145668) is the prodrug of cytarabine, which is a pyrimidine nucleoside analog that inhibits the DNA synthesis and used mainly in the treatment of leukemia.
Acta Biochim Biophys Sin (Shanghai), 2020, 14 pii: gmaa017
J Med Virol, 2019, 91(8):1440-1447
Int J Mol Sci, 2018, 19(6)
S1995 Procarbazine HCl Procarbazine HCl (NSC-77213) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound, used for the treatment of Hodgkin's lymphoma.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cancer Cell Int, 2020, 19;20:58
S2239 Tubacin Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis.
Signal Transduct Target Ther, 2021, 6(1):333
STAR Protoc, 2021, 2(3):100674
Cancers (Basel), 2020, 12(11)E3172
S2427 Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry.
S2600 Fexinidazole Fexinidazole (HOE-239, Fexinidazole Winthrop) is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness).
S2678 NSC 207895 NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
Sci Rep, 2019, 9(1):1897
S2684 Pidnarulex (CX-5461) Pidnarulex (CX-5461) is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation.
Genes Dev, 2021, 35(7-8):483-488
Elife, 2021, 10e65184
Int J Mol Sci, 2021, 22(11)5782
S2794 Sofosbuvir (GS-7977) Sofosbuvir (PSI-7977, GS-7977) is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection.
Int J Mol Sci, 2021, 22(9)4559
J Toxicol Sci, 2021, 46(8):359-369
Cells, 2020, 9(4)E1003
S2961 GC7 Sulfate GC7 (N1-guanyl-1,7-diaminoheptane) Sulfate is an inhibitor of deoxyhypusine synthase (DHPS). GC7 inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins.
S3001 Clevudine Clevudine is an antiviral drug for the treatment of hepatitis B.
S3009 Menthone

Menthone is one of the main volatile components of the essential oil of peppermint (Mentha piperita L.). Menthone is used as antioxidant agent and has a good compensatory effect with significant reduction in DNA damages in sperm cells.

S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Blood, 2021, 138(9):790-805
Int J Mol Sci, 2021, 22(3)1362
Sci Rep, 2021, 11(1):12148
S3356 Phosphonoacetic acid

Phosphonoacetic acid (PAA) is an active endogenous metabolite that possesses a restricted potential to block DNA biosynthesis. Phosphonoacetic acid exhibits anti-viral activities.

S3360 Bis(2-ethylhexyl) phthalate

Bis(2-ethylhexyl) phthalate (Dioctyl phthalate, DOP, Diplast O, ESBO-D 82, Ergoplast FDO, Ergoplast FDO-S, Etalon) induces DNA strand breaks and gene expression alterations in larval zebrafish Danio rerio.

S3472 Metarrestin (ML246) Metarrestin (ML246) is an orally active and specific perinucleolar compartment (PNC) inhibitor that disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
S3549New PFM01 PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity.
S3641 Osalmid Osalmid suppresses ribonucleotide reductase (RNR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM.
S3669 Carmustine Carmustine (bis-chloroethylnitrosourea, BCNU, BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms.
Cancer Res, 2021, 81(23):6044-6057
S4035 Vitamin D2 Vitamin D2 (Ergocalciferol) is a selective inhibitor of mammalian DNA polymerase A (pol A) with IC50 of 123 μM.
Aging (Albany NY), 2020, 12
S4227 Fidaxomicin Fidaxomicin (OPT-80, PAR-101) is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.
Sci Rep, 2021, 11(1):15007
Sci Rep, 2020, 18;10(1):8159
PLoS One, 2020, 15(2):e0228509
S4236 Proflavine Hemisulfate Proflavine Hemisulfate is a topical antiseptic by interchelating DNA, thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands.
S4239 Bergapten Bergapten is a psoralen that can be photoactivated and is capable of crossing-linking DNA, covalently modifying proteins and lipids, and consequently inhibiting cell replication.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab037
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S4252 Mechlorethamine HCl Mechlorethamine is the prototype of alkylating agents, it works by binding to DNA, crosslinking two strands and preventing cell duplication.
Cell Rep, 2021, 34(10):108814
Cancer Cell Int, 2020, 19;20:58
Hum Cell, 2020, 10.1007/s13577-020-00425-8
S4288 Chloroambucil Chloroambucil (Chlorambucil) is a nitrogen mustard alkylating agent, used in the treatment of chronic lymphocytic leukemia.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Cancer Cell Int, 2020, 19;20:58
S4297 Mupirocin Mupirocin is an isoleucyl t-RNA synthetase inhibitor, used in the treatment of bacterial skin infections.
Anaerobe, 2020, 62:102169
Life Sci, 2019, 224:51-57
Biogerontology, 2016, 17(5-6):907-920
S4504 6-Mercaptopurine (6-MP) Monohydrate 6-Mercaptopurine (6-MP) Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
S4537 Oxolinic acid Oxolinic acid (Urinox, NSC 110364) is a quinolone antibiotic, inhibiting the enzyme DNA gyrase and DNA synthesis.It also acts as a dopamine reuptake inhibitor.
S4737 Psoralen Psoralen (Psoralene, Ficusin, Furocoumarin) is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division.
S4782 5-methoxyflavone 5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity.
S5293 Nimustine Hydrochloride Nimustine Hydrochloride (Nidran) is the hydrochloride salt of nimustine, a nitrosourea with antineoplastic activity that alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death.
S5297 Vidarabine monohydrate Vidarabine (Spongoadenosine, Vira-A) is a nucleoside antibiotic with antiviral acitivity that interferes with the synthesis of viral DNA. It is used to treat herpes simplex and varicella zoster viruses.
S5484 Rimantadine Hydrochloride Rimantadine is an RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. It works by inhibiting a viral protein called M2, which normally mediates the transport of acid ions across the influenza virion shell.
bioRxiv, 2020, 2020.08.12.246389
S5552 Amenamevir Amenamevir (ASP2151) is a potent helicase-primase inhibitor and a novel class of antiviral agent.
J Biomol Struct Dyn, 2020, 1-14
S5582 Cytarabine hydrochloride Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA.
Leukemia, 2021, 10.1038/s41375-021-01361-8
Blood Cancer J, 2021, 11(6):111
Cell Death Dis, 2021, 12(1):9
S5948 Amodiaquine Amodiaquine is a synthetic aminoquinoline that acts by binding to the protozoal or parasitic DNA and preventing DNA and RNA production and subsequent protein synthesis. It is used for the therapy of malaria.
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
bioRxiv, 2020, 10.1101/2020.04.13.039917
bioRxiv, 2020, 2020/9/20.4.7.30734
S5953New Menadione bisulfite sodium Menadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
Life Sci, 2020, 242:117159
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043
S6115 Pyridoxal 5′-phosphate hydrate Pyridoxal 5′-phosphate (pyridoxal phosphate, Vitamin B6 phosphate, PAL-P, PLP), a vitamin B6 phosphate, is a coenzyme in a variety of enzymatic reactions. Pyridoxal 5′-phosphate at concentrations < 0.5 mM inhibits of polymerization deoxynucleoside triphosphate catalysed by variety of DNA polymerases isolated from type C RNA tumor viruses. The combination of Pyridoxal 5′-phosphate and NEIL2 will make NEIL2 completely lose its ability to bind damaged DNA.
S6848 3'-Fluoro-3'-deoxythymidine (Alovudine) 3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.
S6854 Triazavirin Triazavirin (TZV, Riamilovir) is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza.
S7418 Cycloheximide (NSC-185) Cycloheximide (NSC-185, Actidione, Naramycin A, CHX, FT 3422-2, NM-MCD 80), an antifungal antibiotic, is an eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.
Open Med (Wars), 2022, 17(1):1-14
Biomaterials, 2021, 271:120720
Theranostics, 2021, 11(2):700-714
S7419 Blasticidin S HCl Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.
Theranostics, 2021, 11(6):2966-2986
Cell Rep, 2021, 34(7):108713
Nat Commun, 2020, 11(1):5842
S7445 E3330 E3330 (APX-3330) is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
Cancer Research on Prevention and Treatment, 2020, 47(7): 492-497
Cancer Research on Prevention and Treatment, 2020, (7): 492-497
Cancer Research on Prevention and Treatment, 2020, 47(7): 492-497
S7449 CRT0044876 CRT0044876 (NSC 69877, 7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.
Nat Biotechnol, 2017, 35(5):463-474
S7470 Triapine Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.
Cell, 2021, 184(2):334-351.e20
Mol Cancer, 2021, 20(1):97
Sci Rep, 2021, 11(1):13474
S7546 Pritelivir (BAY 57-1293) Pritelivir (BAY 57-1293, AIC316) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
PLoS Pathog, 2021, 17(11):e1010117
J Virol, 2021, JVI0166621
S7637 DTP3 DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
S7679 YK-4-279 YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).
Front Oncol, 2021, 11:649323
Clin Cancer Res, 2020, 21;clincanres35732019
Cancers (Basel), 2020, 12(11)E3205
S7718 BMH-21 BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.
Cell Death Differ, 2021, 10.1038/s41418-021-00882-0
Lab Invest, 2021, 10.1038/s41374-021-00642-1
Front Genet, 2020, 11:43
S7742 SCR7 SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.
Protein Cell, 2021, 10.1007/s13238-021-00879-y 10.1126/science.abc5386
Pharmacol Res, 2021, S1043-6618(21)00518-1
Cold Spring Harb Protoc, 2021, 10.1101/pdb.prot106989
S7757 6-Thio-dG 6-thio-dG (β-TGdR) is a nucleoside analog and telomerase substrate.
Clin Sci (Lond), 2020, 10.1042/CS20190890
S7975 Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
mBio, 2021, 12(1)e02754-20
Antiviral Res, 2021, S0166-3542(21)00068-1
Toxicol Sci, 2021, kfab079
S8095 Tubercidin Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.
Mol Cell, 2020, 80(6):1104-1122.e9
S8144 Halofuginone Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
Gastric Cancer, 2021, 10.1007/s10120-021-01259-5
Research Square, 2021, 10.21203/rs.3.rs-738132/v1
Sci Rep, 2020, 10(1):19723
S8146 Mitomycin C Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.
Cell Res, 2021, 10.1038/s41422-021-00592-9
Cell Res, 2021, 1-13
Proc Natl Acad Sci U S A, 2021, 118(10)e2005568118
S8246 RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.
Nat Commun, 2021, 12(1):2475
Cancer Res, 2021, 81(13):3607-3620
Front Immunol, 2021, 12:616402
S8328 CeMMEC1 HCl CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM).
S8329 CeMMEC13 CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM).
S8376 Rbin-1 Rbin-1 (Ribozinoindole-1) is a potent chemical inhibitor of eukaryotic ribosome assembly. It inhibits recombinant full-length Mdn1's ATPase activity in vitro.
S8434 B02 B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).
Mol Cell, 2021, 81(19):4026-4040.e8
Protein Cell, 2021, 10.1007/s13238-021-00879-y 10.1126/science.abc5386
Cell Death Differ, 2021, 10.1038/s41418-020-00733-4
S8539 TAS-102 TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
Adv Sci (Weinh), 2021, e2103360
S8850 JH-RE-06 JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).
S8932 Remdesivir (GS-5734) Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.
Nat Commun, 2021, 12(1):5553
Nat Commun, 2021, 12(1):668
EMBO J, 2021, e107826
S8977 BCH001 BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif.
S9521 Pentostatin Pentostatin is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.
Nat Metab, 2020, 10.1038/s42255-020-0227-4
S9649 Acelarin (NUC-1031) Acelarin (NUC-1031, Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389), a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine, is a DNA synthesis inhibitor with EC50 of 0.2 nM.
S9718 TK216

TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.

S9775New SCR130 SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining.
A5172 MCM2 Rabbit Recombinant mAb MCM2 Rabbit Recombinant mAb detects endogenous level of total MCM2.
A5242 DGCR8 Rabbit Recombinant mAb DGCR8 Rabbit Recombinant mAb detects endogenous level of total DGCR8.
A5274 MSI2 Rabbit Recombinant mAb MSI2 Rabbit Recombinant mAb detects endogenous level of total MSI2.
A5275 hnRNP K Rabbit Recombinant mAb hnRNP K Rabbit Recombinant mAb detects endogenous level of total hnRNP K.
A5297 PABPN1 Rabbit Recombinant mAb PABPN1 Rabbit Recombinant mAb detects endogenous level of total PABPN1.
A5301 FMRP Rabbit Recombinant mAb FMRP Rabbit Recombinant mAb detects endogenous level of total FMRP.
A5314 hnRNP A1 Rabbit Recombinant mAb hnRNP A1 Rabbit Recombinant mAb detects endogenous level of total hnRNP A1.
A5323 DAZL Rabbit Recombinant mAb DAZL Rabbit Recombinant mAb detects endogenous level of total DAZL.
S3168New cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S4423New Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4476New PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S6893 PIN1 inhibitor API-1 PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor with IC50 of 72.3 nM. PIN1 inhibitor API-1 targets Pin1 peptidyl-prolyl isomerase domain and inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 up-regulates miRNA biogenesis by retaining active XPO5 conformation and suppresses HCC development.
S8326 Saccharin 1-methylimidazole (SMI) Saccharin 1-methylimidazole (SMI) is considered a general-purpose activator for DNA and RNA synthesis.
S1334 Flupirtine maleate Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.
Assay Drug Dev Technol, 2019, 17(7):310-321
Elife, 2015, 4
S6909New Levomefolic acid Levomefolic acid (5-MTHF, LMSR, Metafolin, Nutrifolin) is a natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions.
S6997New CHAPS CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome.
S9603 Lurbinectedin (PM01183) Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.
S1212 Bendamustine (SDX105) HCl Bendamustine (SDX-105, Cytostasane) HCl is a DNA-damaging agent with IC50 of 50 μM in cell-free assay.
Cell Death Differ, 2021, 10.1038/s41418-021-00880-2
Front Immunol, 2021, 12:699128
Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0864
S1214 Bleomycin (NSC125066) sulfate Bleomycin Sulfate (NSC125066) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.
EMBO J, 2021, e107403
Proc Natl Acad Sci U S A, 2021, 118(35)e2106685118
Cell Rep, 2021, 34(7):108713
S1237 Temozolomide (CCRG 81045) Temozolomide (CCRG81045, NSC 362856, TMZ) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.
Cell Res, 2021, 10.1038/s41422-021-00528-3
Clin Cancer Res, 2021, clincanres.2092.2021
Theranostics, 2021, 11(4):1991-2005
S1840 Lomustine Lomustine (NSC79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging the DNA and stops cells from dividing.
Sci Rep, 2021, 11(1):20338
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1981 Adenine Adenine is a purine derivative and a nucleobase with a variety of roles in biochemistry.
PLoS Pathog, 2020, 16;16(3):e1008341
S1982 Adenine sulfate Adenine sulfate is a sulfate salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.
S1983 Adenine HCl Adenine HCl is a hydrochloride salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Cancer Cell Int, 2020, 19;20:58
S2029 Uridine Uridine (NSC 20256) is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond.
J Med Chem, 2021, 64(18):13918-13932
bioRxiv, 2021, 10.1101/2021.06.28.450163
bioRxiv, 2021, 10.1101/2021.06.28.450163
S3190 N6-methyladenosine (m6A) N6-methyladenosine (m6A, NSC-29409, 6-Methyladenosine, N-Methyladenosine) is a base modified analog of adenosine and is found as a minor nucleoside in natural RNAs.
Nat Commun, 2021, 12(1):2159
Nat Commun, 2021, 12(1):3780
Nat Genet, 2020, 10.1038/s41588-020-0677-3
S4194 Azaguanine-8 Azaguanine-8 (NSC-749, SF-337, SK 1150) is a purine analogs showing antineoplastic activity by competing with guanine in the metabolism.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Cancer Cell Int, 2020, 19;20:58
S4803 Thymidine (NSC 21548) Thymidine (Deoxythymidine, 2'-Deoxythymidine, 5-Methyldeoxyuridine, DThyd, NSC 21548) is a pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix.
Elife, 2021, 10e65234
J Biol Chem, 2021, S0021-9258(21)01252-7
bioRxiv, 2020, 10.1101/2020.11.26.400499
S4888 Guanine Guanine is one of the four main nucleobases found in the nucleic acids DNA and RNA.
S5374 5'-Cytidylic acid 5'-Cytidylic acid (Cytidine monophosphate, Cytidine 5'-phosphate) is a nucleotide that is used as a monomer in RNA.
S5384 UTP Trisodium Salt Uridine-5'-triphosphate (UTP) is a pyrimidine nucleoside triphosphate and a substrate for the synthesis of RNA during transcription.
S5505 2’-deoxyuridine 2'-deoxyuridine (dU, 2'-dU) is frequently halogenated to create thymidine analogues useful for studies of DNA synthesis and degradation mechanisms.
S6077 Cytidine 5′-triphosphate (disodium salt) Cytidine 5'-triphosphate is a pyrimidine nucleoside triphosphate that is involved in a variety of biochemical reactions. It is used in the synthesis of RNA by RNA polymerases.
S6359 Purine Purine is a heterocyclic aromatic organic compound which plays crucial roles in DNA and RNA. It is also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A.
S7918 Bromodeoxyuridine (BrdU) Bromodeoxyuridine (BrdU, 5-Bromo-2'-deoxyuridine, BUdR) is a nucleoside analog that competes with thymidine for incorporation into DNA, and used in the detection of proliferating cells.
Int J Ophthalmol, 2021, 14(4):489-496
Am J Cancer Res, 2021, 11(2):389-415
Neurobiol Stress, 2021, 15:100358
S9382 Thymine Thymine (5-methyluracil) is one of the four nucleobases in the nucleic acid of DNA.
S0054 D-I03 D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively.
S0063 RG3039 RG3039 (PF-06687859, PF 6687859, Quinazoline 495) is an orally bioavailable and brain-penetrant inhibitor of the mRNA decapping enzyme DcpS with IC50 of 4.2 nM and IC90 of 40 nM, respectively.
S0102 L 189 L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage.
S0161 ML367 ML367 is a potent, micromolar inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization. ML367 blocks DNA repair pathways and general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
S0280 Madrasin Madrasin (DDD00107587) is a potent and cell-penetrant pre-mRNA splicing inhibitor. Madrasin interferes with the early stages of spliceosome assembly and stalls spliceosome assembly at the A complex.
S0469 ML216 ML216 (CID-49852229) is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM636-1298 and BLMfull-length, respectively.
S0780 Oncrasin-1 Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells.
S0816 Brr2 Inhibitor C9 Brr2 inhibitor C9 (Brr2 Inhibitor 9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa a group of progressive retinal degenerative disorders.
S1117 Triciribine (NSC 154020) Triciribine (NSC 154020, VD-0002, vqd-002, API-2, TCN) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.
Aging (Albany NY), 2021, 13(5):7096-7119
Int J Mol Sci, 2021, 22(14)7660
J Leukoc Biol, 2021, 10.1002/JLB.1A0920-588R
S1135 Pemetrexed (LY-231514) disodium Pemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S1149 Gemcitabine (LY-188011) HCl Gemcitabine (LY-188011, NSC 613327) HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.
Cell, 2021, 184(25):6119-6137.e26
Nat Commun, 2021, 12(1):4917
Nat Commun, 2021, 12(1):1602
S1156 Capecitabine (RO 09-1978) Capecitabine (RO 09-1978) is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis.
Adv Sci (Weinh), 2021, e2103360
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1166 Cisplatin (NSC 119875) Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP) is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy. Solutions are best fresh-prepared.
Cancer Cell, 2021, S1535-6108(21)00659-0
Nat Commun, 2021, 12(1):5404
Nat Commun, 2021, 12(1):7064
S1192 Raltitrexed Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.
Cell, 2021, 184(2):334-351.e20
Cancers (Basel), 2021, 13(9)2061
Anal Chem, 2020, 10.1021/acs.analchem.0c02756
S1199 Cladribine (RWJ 26251) Cladribine (RWJ 26251, Leustatin, 2-CdA, 2-chlorodeoxyadenosine, 2-Chloro-2′-deoxyadenosine, CldAdo, Jk 6251, NSC 105014) is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
Neoplasia, 2021, 23(12):1183-1191
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1209 Fluorouracil (5-Fluorouracil, 5-FU) Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.
Cell, 2021, 184(25):6119-6137.e26
Sci Adv, 2021, 7(36):eabh1684
Nat Commun, 2021, 12(1):4840
S1213 Nelarabine Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
World Scientific, 2021, Vol. 20, No. 03, pp. 305-322
S1215 Carboplatin (NSC 241240) Carboplatin (NSC 241240, JM-8, CBDCA) is a DNA synthesis inhibitor by binding to DNA and interfering with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. Solutions are best fresh-prepared.
Cancer Cell, 2021, S1535-6108(21)00659-0
Nat Commun, 2021, 12(1):3636
Cell Rep, 2021, 34(10):108814
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
iScience, 2021, 24(9):103080
S1221 Dacarbazine (NSC-45388) Dacarbazine (NSC-45388, DTIC-Dome, Imidazole Carboxamide) is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers.
Cancer Res, 2021, 81(23):6044-6057
Biochem Biophys Res Commun, 2021, 557:213-220
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1224 Oxaliplatin (NSC 266046) Oxaliplatin (NSC 266046, L-OHP, Eloxatin) is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells. DMF is recommended for dissolution. Solutions are best fresh-prepared.
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, e2103360
S1229 Fludarabine Phosphate Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
Aging (Albany NY), 2021, 13(8):12160-12178
Int J Mol Sci, 2021, 22(16)8864
Lab Invest, 2021, 10.1038/s41374-021-00703-5
S1289 Carmofur Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer.
Cancer Cell, 2021, S1535-6108(21)00659-0
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1299 Floxuridine (NSC 27640) Floxuridine (NSC 27640, Deoxyfluorouridine, FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV.
Cell Chem Biol, 2021, S2451-9456(21)00306-8
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1300 Tegafur (FT-207) Tegafur (FT-207, NSC 148958) is a substance being used in the treatment of some types of cancer.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cancer Cell Int, 2020, 19;20:58
S1302 Ifosfamide (NSC109724) Ifosfamide (NSC109724, Isophosphamide) is a nitrogen mustard alkylating agent used in the treatment of cancer.
Cancer Cell Int, 2021, 21(1):646
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1305 Mercaptopurine (6-MP) Mercaptopurine is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
Theranostics, 2021, 11(9):4011-4029
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1373 Daptomycin (LY146032) Daptomycin (LY146032) is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.
J Phys Chem B, 2021, 125(22):5775-5785
Sci Adv, 2020, 6(34):eaba8968
Front Microbiol, 2020, 21;11:646
S1384 Mizoribine Mizoribine (Bredinin, NSC 289637) is an imidazole nucleoside and an immunosuppressant that inhibits HCV RNA replication with IC50 of ~ 100 μM for anti-HCV activity. Mizoribine is a selective inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase. Mizoribine also inhibits SARS-CoV.
Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
JCI Insight, 2020, 9;5(7):e135071
S1491 Fludarabine (NSC 118218) Fludarabine (NSC 118218, FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.
Cell Metab, 2021, 33(1):110-127.e5
Cell Rep, 2021, 34(1):108584
Cell Rep, 2021, 34(1):108584
S1516 Cidofovir Cidofovir (HPMPC) suppresses virus replication by selective inhibition of viral DNA synthesis.
Oncol Lett, 2021, 21(4):280
Nat Biotechnol, 2019, 37(3):303-313
J Virol, 2019, 93(4)
S1648 Cytarabine (U-19920A) Cytarabine (U-19920A, Cytarabin, Ara-C, Arabinofuranosyl Cytidine, Cytosine β-D-arabinofuranoside, Cytosine arabinoside, NSC 63878, NSC 287459) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
Leukemia, 2021, 10.1038/s41375-021-01361-8
Blood Cancer J, 2021, 11(6):111
Cell Rep, 2021, 36(7):109559
S1714 Gemcitabine (LY-188011) Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Nat Commun, 2021, 12(1):1602
Cancer Res, 2021, canres.1337.2021
Cell Rep, 2021, 34(10):108814
S1760 Rifapentine Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis.
Front Microbiol, 2020, 10:2936
mSphere, 2018, 3(5)
S1764 Rifampin (NSC-113926) Rifampin (NSC-113926, Rimactane, Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Front Oncol, 2021, 11:715193
PLoS One, 2021, 16(11):e0260633
Pharmacogenomics J, 2020, 10.1038/s41397-020-0160-7
S1778 Trifluridine (NSC 75520) Trifluridine (NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye.
Cell Chem Biol, 2021, S2451-9456(21)00261-0
Sci Adv, 2020, 6(49)eabd9443
Ocul Surf, 2019, 10.1016/j.jtos.2019.11.011
S1784 Vidarabine Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.
Neuron, 2017, 96(6):1290-1302
ACS Appl Mater Interfaces, 2016, 8(39):25818-25824
Biogerontology, 2016, 17(5-6):907-920
S1790 Rifaximin Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria.
S1807 Aciclovir (BW 248U) Acyclovir (BW 248U, Acyclovir, Acycloguanosine, Zovirax, ACV, NSC 645011) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells.
Microbiol Spectr, 2021, 9(3):e0064621
Front Microbiol, 2021, 12:722748
Vet Microbiol, 2021, 265:109313
S1826 Nedaplatin Nedaplatin is a derivative of cisplatin and DNA damage agent for tumor colony forming units with IC50 of 94 μM.
Nat Commun, 2019, 10(1):5654
Cancer Res, 2018, 78(19):5694-5705
Oncol Lett, 2016, 12(5):4195-4202
S1896 Hydroxyurea (NSC-32065) Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
Nat Commun, 2021, 12(1):5572
Cancer Res, 2021, canres.3761.2020
Cell Death Dis, 2021, 12(2):183
S1907 Metronidazole Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa.
Elife, 2021, 10e69795
Bone Joint Res, 2020, 16;9(4):152-161
S1949 Menadione (NSC 4170) Menadione (NSC 4170, Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
Mol Cell, 2021, S1097-2765(21)00269-0
DNA Repair (Amst), 2021, 105:103152
BMC Urol, 2021, 21(1):96
S1973 Cyclocytidine HCl Cyclocytidine (NSC 145668) is the prodrug of cytarabine, which is a pyrimidine nucleoside analog that inhibits the DNA synthesis and used mainly in the treatment of leukemia.
Acta Biochim Biophys Sin (Shanghai), 2020, 14 pii: gmaa017
J Med Virol, 2019, 91(8):1440-1447
Int J Mol Sci, 2018, 19(6)
S1995 Procarbazine HCl Procarbazine HCl (NSC-77213) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound, used for the treatment of Hodgkin's lymphoma.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Cancer Cell Int, 2020, 19;20:58
S2239 Tubacin Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis.
Signal Transduct Target Ther, 2021, 6(1):333
STAR Protoc, 2021, 2(3):100674
Cancers (Basel), 2020, 12(11)E3172
S2427 Triglycidyl Isocyanurate (Teroxirone) Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry.
S2600 Fexinidazole Fexinidazole (HOE-239, Fexinidazole Winthrop) is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness).
S2678 NSC 207895 NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
Sci Rep, 2019, 9(1):1897
S2684 Pidnarulex (CX-5461) Pidnarulex (CX-5461) is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation.
Genes Dev, 2021, 35(7-8):483-488
Elife, 2021, 10e65184
Int J Mol Sci, 2021, 22(11)5782
S2794 Sofosbuvir (GS-7977) Sofosbuvir (PSI-7977, GS-7977) is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection.
Int J Mol Sci, 2021, 22(9)4559
J Toxicol Sci, 2021, 46(8):359-369
Cells, 2020, 9(4)E1003
S2961 GC7 Sulfate GC7 (N1-guanyl-1,7-diaminoheptane) Sulfate is an inhibitor of deoxyhypusine synthase (DHPS). GC7 inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins.
S3001 Clevudine Clevudine is an antiviral drug for the treatment of hepatitis B.
S3009 Menthone

Menthone is one of the main volatile components of the essential oil of peppermint (Mentha piperita L.). Menthone is used as antioxidant agent and has a good compensatory effect with significant reduction in DNA damages in sperm cells.

S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Blood, 2021, 138(9):790-805
Int J Mol Sci, 2021, 22(3)1362
Sci Rep, 2021, 11(1):12148
S3356 Phosphonoacetic acid

Phosphonoacetic acid (PAA) is an active endogenous metabolite that possesses a restricted potential to block DNA biosynthesis. Phosphonoacetic acid exhibits anti-viral activities.

S3360 Bis(2-ethylhexyl) phthalate

Bis(2-ethylhexyl) phthalate (Dioctyl phthalate, DOP, Diplast O, ESBO-D 82, Ergoplast FDO, Ergoplast FDO-S, Etalon) induces DNA strand breaks and gene expression alterations in larval zebrafish Danio rerio.

S3472 Metarrestin (ML246) Metarrestin (ML246) is an orally active and specific perinucleolar compartment (PNC) inhibitor that disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
S3549New PFM01 PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity.
S3641 Osalmid Osalmid suppresses ribonucleotide reductase (RNR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM.
S3669 Carmustine Carmustine (bis-chloroethylnitrosourea, BCNU, BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms.
Cancer Res, 2021, 81(23):6044-6057
S4035 Vitamin D2 Vitamin D2 (Ergocalciferol) is a selective inhibitor of mammalian DNA polymerase A (pol A) with IC50 of 123 μM.
Aging (Albany NY), 2020, 12
S4227 Fidaxomicin Fidaxomicin (OPT-80, PAR-101) is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.
Sci Rep, 2021, 11(1):15007
Sci Rep, 2020, 18;10(1):8159
PLoS One, 2020, 15(2):e0228509
S4236 Proflavine Hemisulfate Proflavine Hemisulfate is a topical antiseptic by interchelating DNA, thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands.
S4239 Bergapten Bergapten is a psoralen that can be photoactivated and is capable of crossing-linking DNA, covalently modifying proteins and lipids, and consequently inhibiting cell replication.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab037
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S4252 Mechlorethamine HCl Mechlorethamine is the prototype of alkylating agents, it works by binding to DNA, crosslinking two strands and preventing cell duplication.
Cell Rep, 2021, 34(10):108814
Cancer Cell Int, 2020, 19;20:58
Hum Cell, 2020, 10.1007/s13577-020-00425-8
S4288 Chloroambucil Chloroambucil (Chlorambucil) is a nitrogen mustard alkylating agent, used in the treatment of chronic lymphocytic leukemia.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Cancer Cell Int, 2020, 19;20:58
S4297 Mupirocin Mupirocin is an isoleucyl t-RNA synthetase inhibitor, used in the treatment of bacterial skin infections.
Anaerobe, 2020, 62:102169
Life Sci, 2019, 224:51-57
Biogerontology, 2016, 17(5-6):907-920
S4504 6-Mercaptopurine (6-MP) Monohydrate 6-Mercaptopurine (6-MP) Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
S4537 Oxolinic acid Oxolinic acid (Urinox, NSC 110364) is a quinolone antibiotic, inhibiting the enzyme DNA gyrase and DNA synthesis.It also acts as a dopamine reuptake inhibitor.
S4737 Psoralen Psoralen (Psoralene, Ficusin, Furocoumarin) is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division.
S4782 5-methoxyflavone 5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity.
S5293 Nimustine Hydrochloride Nimustine Hydrochloride (Nidran) is the hydrochloride salt of nimustine, a nitrosourea with antineoplastic activity that alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death.
S5297 Vidarabine monohydrate Vidarabine (Spongoadenosine, Vira-A) is a nucleoside antibiotic with antiviral acitivity that interferes with the synthesis of viral DNA. It is used to treat herpes simplex and varicella zoster viruses.
S5484 Rimantadine Hydrochloride Rimantadine is an RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. It works by inhibiting a viral protein called M2, which normally mediates the transport of acid ions across the influenza virion shell.
bioRxiv, 2020, 2020.08.12.246389
S5552 Amenamevir Amenamevir (ASP2151) is a potent helicase-primase inhibitor and a novel class of antiviral agent.
J Biomol Struct Dyn, 2020, 1-14
S5582 Cytarabine hydrochloride Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA.
Leukemia, 2021, 10.1038/s41375-021-01361-8
Blood Cancer J, 2021, 11(6):111
Cell Death Dis, 2021, 12(1):9
S5948 Amodiaquine Amodiaquine is a synthetic aminoquinoline that acts by binding to the protozoal or parasitic DNA and preventing DNA and RNA production and subsequent protein synthesis. It is used for the therapy of malaria.
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
bioRxiv, 2020, 10.1101/2020.04.13.039917
bioRxiv, 2020, 2020/9/20.4.7.30734
S5953New Menadione bisulfite sodium Menadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
Life Sci, 2020, 242:117159
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043
S6115 Pyridoxal 5′-phosphate hydrate Pyridoxal 5′-phosphate (pyridoxal phosphate, Vitamin B6 phosphate, PAL-P, PLP), a vitamin B6 phosphate, is a coenzyme in a variety of enzymatic reactions. Pyridoxal 5′-phosphate at concentrations < 0.5 mM inhibits of polymerization deoxynucleoside triphosphate catalysed by variety of DNA polymerases isolated from type C RNA tumor viruses. The combination of Pyridoxal 5′-phosphate and NEIL2 will make NEIL2 completely lose its ability to bind damaged DNA.
S6848 3'-Fluoro-3'-deoxythymidine (Alovudine) 3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.
S6854 Triazavirin Triazavirin (TZV, Riamilovir) is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza.
S7418 Cycloheximide (NSC-185) Cycloheximide (NSC-185, Actidione, Naramycin A, CHX, FT 3422-2, NM-MCD 80), an antifungal antibiotic, is an eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.
Open Med (Wars), 2022, 17(1):1-14
Biomaterials, 2021, 271:120720
Theranostics, 2021, 11(2):700-714
S7419 Blasticidin S HCl Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.
Theranostics, 2021, 11(6):2966-2986
Cell Rep, 2021, 34(7):108713
Nat Commun, 2020, 11(1):5842
S7445 E3330 E3330 (APX-3330) is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
Cancer Research on Prevention and Treatment, 2020, 47(7): 492-497
Cancer Research on Prevention and Treatment, 2020, (7): 492-497
Cancer Research on Prevention and Treatment, 2020, 47(7): 492-497
S7449 CRT0044876 CRT0044876 (NSC 69877, 7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.
Nat Biotechnol, 2017, 35(5):463-474
S7470 Triapine Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.
Cell, 2021, 184(2):334-351.e20
Mol Cancer, 2021, 20(1):97
Sci Rep, 2021, 11(1):13474
S7546 Pritelivir (BAY 57-1293) Pritelivir (BAY 57-1293, AIC316) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
PLoS Pathog, 2021, 17(11):e1010117
J Virol, 2021, JVI0166621
S7637 DTP3 DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
S7679 YK-4-279 YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).
Front Oncol, 2021, 11:649323
Clin Cancer Res, 2020, 21;clincanres35732019
Cancers (Basel), 2020, 12(11)E3205
S7718 BMH-21 BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.
Cell Death Differ, 2021, 10.1038/s41418-021-00882-0
Lab Invest, 2021, 10.1038/s41374-021-00642-1
Front Genet, 2020, 11:43
S7742 SCR7 SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.
Protein Cell, 2021, 10.1007/s13238-021-00879-y 10.1126/science.abc5386
Pharmacol Res, 2021, S1043-6618(21)00518-1
Cold Spring Harb Protoc, 2021, 10.1101/pdb.prot106989
S7757 6-Thio-dG 6-thio-dG (β-TGdR) is a nucleoside analog and telomerase substrate.
Clin Sci (Lond), 2020, 10.1042/CS20190890
S7975 Favipiravir (T-705) Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
mBio, 2021, 12(1)e02754-20
Antiviral Res, 2021, S0166-3542(21)00068-1
Toxicol Sci, 2021, kfab079
S8095 Tubercidin Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.
Mol Cell, 2020, 80(6):1104-1122.e9
S8144 Halofuginone Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
Gastric Cancer, 2021, 10.1007/s10120-021-01259-5
Research Square, 2021, 10.21203/rs.3.rs-738132/v1
Sci Rep, 2020, 10(1):19723
S8146 Mitomycin C Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.
Cell Res, 2021, 10.1038/s41422-021-00592-9
Cell Res, 2021, 1-13
Proc Natl Acad Sci U S A, 2021, 118(10)e2005568118
S8246 RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.
Nat Commun, 2021, 12(1):2475
Cancer Res, 2021, 81(13):3607-3620
Front Immunol, 2021, 12:616402
S8328 CeMMEC1 HCl CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM).
S8329 CeMMEC13 CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM).
S8376 Rbin-1 Rbin-1 (Ribozinoindole-1) is a potent chemical inhibitor of eukaryotic ribosome assembly. It inhibits recombinant full-length Mdn1's ATPase activity in vitro.
S8434 B02 B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).
Mol Cell, 2021, 81(19):4026-4040.e8
Protein Cell, 2021, 10.1007/s13238-021-00879-y 10.1126/science.abc5386
Cell Death Differ, 2021, 10.1038/s41418-020-00733-4
S8539 TAS-102 TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
Adv Sci (Weinh), 2021, e2103360
S8850 JH-RE-06 JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).
S8932 Remdesivir (GS-5734) Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.
Nat Commun, 2021, 12(1):5553
Nat Commun, 2021, 12(1):668
EMBO J, 2021, e107826
S8977 BCH001 BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif.
S9521 Pentostatin Pentostatin is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.
Nat Metab, 2020, 10.1038/s42255-020-0227-4
S9649 Acelarin (NUC-1031) Acelarin (NUC-1031, Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389), a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine, is a DNA synthesis inhibitor with EC50 of 0.2 nM.
S9718 TK216

TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.

S9775New SCR130 SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining.
A5172 MCM2 Rabbit Recombinant mAb MCM2 Rabbit Recombinant mAb detects endogenous level of total MCM2.
A5242 DGCR8 Rabbit Recombinant mAb DGCR8 Rabbit Recombinant mAb detects endogenous level of total DGCR8.
A5274 MSI2 Rabbit Recombinant mAb MSI2 Rabbit Recombinant mAb detects endogenous level of total MSI2.
A5275 hnRNP K Rabbit Recombinant mAb hnRNP K Rabbit Recombinant mAb detects endogenous level of total hnRNP K.
A5297 PABPN1 Rabbit Recombinant mAb PABPN1 Rabbit Recombinant mAb detects endogenous level of total PABPN1.
A5301 FMRP Rabbit Recombinant mAb FMRP Rabbit Recombinant mAb detects endogenous level of total FMRP.
A5314 hnRNP A1 Rabbit Recombinant mAb hnRNP A1 Rabbit Recombinant mAb detects endogenous level of total hnRNP A1.
A5323 DAZL Rabbit Recombinant mAb DAZL Rabbit Recombinant mAb detects endogenous level of total DAZL.
S3168New cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S4423New Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4476New PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S6893 PIN1 inhibitor API-1 PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor with IC50 of 72.3 nM. PIN1 inhibitor API-1 targets Pin1 peptidyl-prolyl isomerase domain and inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 up-regulates miRNA biogenesis by retaining active XPO5 conformation and suppresses HCC development.
S8326 Saccharin 1-methylimidazole (SMI) Saccharin 1-methylimidazole (SMI) is considered a general-purpose activator for DNA and RNA synthesis.
S1334 Flupirtine maleate Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.
Assay Drug Dev Technol, 2019, 17(7):310-321
Elife, 2015, 4
S6909New Levomefolic acid Levomefolic acid (5-MTHF, LMSR, Metafolin, Nutrifolin) is a natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions.
S6997New CHAPS CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome.
S9603 Lurbinectedin (PM01183) Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.
S3549New PFM01 PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity.
S5953New Menadione bisulfite sodium Menadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
Life Sci, 2020, 242:117159
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043
S9775New SCR130 SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining.
S3168New cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S4423New Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4476New PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S6909New Levomefolic acid Levomefolic acid (5-MTHF, LMSR, Metafolin, Nutrifolin) is a natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions.
S6997New CHAPS CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome.