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Australia
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Finland
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United States
Synthetic Lethality Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S1009 | Dactolisib (BEZ235) | Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. It inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell, induces autophagy, and suppresses HIV-1 replication. Phase 2. |
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| S1092 | KU-55933 | KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy. |
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| S2913 | BAY 11-7082 (BAY 11-7821) | BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells. |
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| S2758 | Wortmannin (SL-2052) | Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity. |
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| S8007 | VE-821 | VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ. |
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| S1004 | Veliparib (ABT-888) | Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. This compound is inactive to SIRT2 and increases autophagy and apoptosis. Phase 3. |
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| S1525 | Adavosertib (AZD1775, MK-1775) | Adavosertib (MK-1775, AZD1775) is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2. |
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| S4157 | Chloroquine diphosphate | Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs). |
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| S1570 | KU-60019 | KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer. |
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| S1098 | Rucaparib phosphate | Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. |
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| S2741 | Niraparib (MK-4827) | Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. This compound can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3. |
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| S2817 | Torin 2 | Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. This compound inhibits ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. It decreases cell viability and induces autophagy and apoptosis. |
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| S4948 | Rucaparib (AG-014699) | Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
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| S7050 | AZ20 | AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR. |
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| S2243 | Degrasyn (WP1130) | Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). This compound induces apoptosis and blocks autophagy. |
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| S8375 | AZD0156 | AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. |
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| S7300 | PJ34 HCl | PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
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| S7888 | Spautin-1 | Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. This compound enhances apoptosis. |
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| S7625 | Niraparib tosylate | Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. |
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| S2178 | AG-14361 | AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides. |
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| S8096 | Mirin | Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. This compound inhibits MRN-dependent activation of ATM. |
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| S7748 | EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
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| S7134 | IU1 | IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. This compound induces autophagy. |
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| S7315 | PFI-3 | PFI-3 is a selective chemical probe for SMARCA bromodomains, including SMARCA2, SMARCA4 and PB1(5) bromodomains. |
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| S7529 | ML323 | ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM. |
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| S1087 | Iniparib (BSI-201) | Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
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| S5195 | Rucaparib Camsylate | Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
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| S8111 | GSK591 | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM. |
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| S2245 | CP-466722 | CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells. |
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| S9864 | Elimusertib (BAY 1895344) | Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM. |
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| S7239 | G007-LK | G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively. |
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| S2197 | A-966492 | A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
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| S8050 | ETP-46464 | ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. |
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| S8592 | Pamiparib | Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. |
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| S2271 | Berberine chloride | Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. This compound activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. It decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. This chemical induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. It is a dual topoisomerase I and II inhibitor. It is also a potential autophagy modulator. |
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| S3600 | Schisandrin B | Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety. |
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| S8666 | Elimusertib (BAY-1895344) hydrochloride | Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM. |
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| S8038 | UPF 1069 | UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
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| S8363 | NMS-P118 | NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). |
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| S8419 | Stenoparib (E7449) | Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. |
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| S8148 | PD0166285 | PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations (IC50=24 nM for Wee1 and 72 nM for Myt1). This compound is also a novel G2 checkpoint abrogator. It induces apoptosis. |
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| S9639 | VX-803 (M4344) | VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. This compound potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. It exhibits potential antineoplastic activity. |
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| S7029 | AZD2461 | AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1. |
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| S7438 | ME0328 | ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
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| S8370 | BGP-15 2HCl | BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
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| S9612 | ACBI1 | ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 induces anti-proliferative effects and apoptosis. |
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| S8624 | Onametostat (JNJ-64619178) | Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties. |
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| S1132 | 3-Aminobenzamide | 3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way. |
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| S9875 | AZD5305 (Saruparib) | Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM). |
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| S7238 | NVP-TNKS656 | NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2. |
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| S0435 | PF-9366 | PF-9366 is a human methionine adenosyltransferase 2A (MAT2A) inhibitor with IC50 of 420 nM and Kd of 170 nM. |
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| S7136 | CGK 733 | CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM. |
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| S7730 | NU1025 | NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM. |
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| E1175 | RP-6306 (lunresertib) | lunresertib (RP-6306) is a Protein Kinase, Membrane Associated Tyrosine/Threonine 1 (PKMYT1) inhibitor, which can be used for the research of cancer. |
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| S9936 | ART558 | ART558 is a potent, selective, low molecular weight, allosteric inhibitor of DNA Polθ with an IC50 of 7.9 nM. |
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| E1024 | MRTX1719 (Navlimetostat) | MRTX1719 is a potent, selective inhibitor of the protein arginine methyltransferase 5·methylthioadenosine phosphorylase complex (PRMT5•MTA), a potentially tumor-selective target for therapeutic intervention. |
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| S4715 | Benzamide | Benzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM. |
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| S8556 | AZ31 | AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ). |
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| S0399 | SJB2-043 | SJB2-043 is a potent USP1 inhibitor that inhibits the activity of native USP1/UAF1 with IC50 of 544 nM. |
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| S2837 | BCI chemical | BCI ((E)-BCI, compound 1) is an allosteric dual specificity phosphatase (DUSP) inhibitor with EC50 of 13.3 μM and 8.0 μM in cells for DUSP6 and DUSP1, respectively. |
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| S8209 | HLCL-61 HCL | HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia. |
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| S7490 | WIKI4 | WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling. |
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| S6745 | JW55 | JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). |
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| E1103 | AU-15330 | AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, which can induce potent inhibition of tumor growth in xenograft models of prostate cancer. |
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| E1479 | I-138 | I-138 is an orally active, potent reversible inhibitor of USP1-UAF1 with IC50 0f 4.1 nM. This compound is structurally related to ML323 and induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells and increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells. |
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| E1528 | RP-6685 | RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ). RP-6685 exhibits antitumor efficacy in animal models. |
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| S8993 | Atamparib (RBN-2397) | RBN-2397 (Atamparib) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. This compound has the potential for the research of tumor treatment. |
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| S9778 | Zedoresertib (Debio-0123, WEE1-IN-5) | WEE1-IN-5 (Debio 0123) is a potent Wee1 inhibitor that inhibits phospho-CDC2 and abrogates the G2 check point. |
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| S8729 | AZ32 | AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability. |
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| S9712 | Fluzoparib (SHR-3162) |
Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity, with an IC50 of 1.46±0.72 nM for PARP1. |
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| S5967 | Berberine chloride hydrate | Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
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| E1000 | Azenosertib (Zn-C3) | Azenosertib (Zn-C3) is an oral active, highly effective and selective Wee1 inhibitor with IC50 of 3.9 nM, which can be used in cancer research. |
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| S0148 | HAMNO | HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. This compound inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR. |
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| S6885 | Ailanthone | Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. This compound triggers DNA damage characterized by activation of the ATM/ATR pathway. It induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. This chemical is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. |
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| E1057 | Lartesertib (M4076) | Lartesertib (M4076) inhibits Ataxia telangiectasia-mutated (ATM) kinase activity with a sub-nanomolar potency and shows remarkable selectivity against other protein kinases, suppresses DSB repair, clonogenic cancer cell growth, and potentiates antitumor activity of ionizing radiation in cancer cell lines. |
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| S8992 | RBN012759 | RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. This compound contributes to anti-tumor immune response. |
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| E1177 | CFT8634 | CFT8634 is a potent BRD9 degrader with DC50 of 3 nM. It forms a ternary complex with BRD9 and an E3 ligase, resulting in BRD9 ubiquitination. This compound is used in the treatment of SMARCB1-perturbed cancers. |
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| E1214 | KSQ-4279 (USP1-IN-1) | KSQ-4279 (USP1-IN-1) is an orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1) with anti-proliferative activity. KSQ-4279 also exhibits synergistic activity in combination with PARP inhibitors. |
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| S0519 | BYK204165 | BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). This compound inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively. |
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| E0111 | BRM/BRG1 ATP Inhibitor-1 (BRM014) | BRM/BRG1 ATP Inhibitor-1 (Compound 14) is an orally active inhibitors of Brahma Homolog (BRM)/SMARCA2 (BRG1) with IC50s below 0.005 µM. |
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| E2147 | AZD9574 (Palacaparib) | AZD9574 is a novel PARP inhibitor which combines PARP1 selectivity, trapping and high CNS penetration in a single molecule. |
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| S4710 | Picolinamide | Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
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| E1425 | Nesuparib | Nesuparib (JPI-547, NOV140201) is a potential inhibitor of both PARP and tankyrases, with IC50 of 0.005 μM, 0.001 μM, 0.002 μM, and ND for TNKS1, TNKS2, PARP1, and PARP2, respectively. This compound exhibits anti-tumor activity in BRCA-deficient xenograft models. | ||
| S6899 | Licochalcone D | Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. This compound inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. It inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. This chemical also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. | ||
| E1411 | Tuvusertib | Tuvusertib (M1774, ATR inhibitor 1) is a potent ATR inhibitor, which exhibits anti-proliferative and anti-tumor effects in cancer cell lines. | ||
| S6977 | DR2313 | DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. | ||
| S6739 | MN 64 | MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. | ||
| S0913 | 4',5,7-Trimethoxyflavone | 4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. This compound increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein. | ||
| S3224 | Cinobufagin | Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. This compound increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. It inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, this chemical induces cell cycle arrest at the G2/M phase and apoptosis. | ||
| E1485 | IDE397 (GSK-4362676) | IDE397 (GSK-4362676) is a potent inhibitor of MAT2A(methionine adenosyltransferase 2A) and exhibits anti-tumor activity in MTAP-deleted PDX models. | ||
| E5842New | Nudifloramide | Nudifloramide (2PY, N-methyl-2-pyridone-5- carboxamide) is a pyridine derivative of nicotinamide that inhibits PARP-1 (poly (ADP-ribose) polymerase-1) activity in vitro, with an IC50 of 8 µM. | ||
| E1007 | BRD0639 |
BRD0639 is a first-in-class PBM-competitive small molecule inhibitor that disrupts the PRMT5-RIOK1 complex with IC50s of 7.5 μM and 16 μM in permeabilized and living cells, respectively. |
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| E1069 | M2912 | M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity. | ||
| E5945New | Wu-5 | Wu-5 is an inhibitor of USP10 that blocks its activity in vitro with an IC50 of 8.3 µM. It also promotes FLT3-ITD degradation and synergistically enhances crenolanib-induced apoptosis. | ||
| S0732 | GeA-69 | GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM. | ||
| E1108 | Camonsertib (RP-3500) | Camonsertib (RP-3500) is a highly potent and selective inhibitor of ATR kinase with an IC50 of 1 nM. | ||
| E1633 | BAY-805 | BAY-805 is a potent, selective, and cell-active inhibitor that non-covalently targets the catalytic activity of USP21, a member of the ubiquitin-specific protease (USP) subfamily of deubiquitinating enzymes (DUBs). | ||
| E8297New | Myt1-IN-1 | Myt1-IN-1 is a potent and selective inhibitor of membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1)(Gene: PKMYT1) with an IC50 of <10 nM. It exhibits anticancer activity and can be used in research on cancers with CCNE1 amplification or FBXW7 mutations that rely on Myt1 activity. | ||
| E1908 | HRO761 | HRO761 is a potent, selective, allosteric inhibitor of Werner syndrome RecQ helicase (WRN). It binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation, and demonstrates anti-proliferative effects specifically in microsatellite instability (MSI) cancer cells. | ||
| E1912 | B102(PARP/HDAC-IN-1) | B102(PARP/HDAC-IN-1) is a dual inhibitor of PARP and HDAC, with IC50 of 19.01 nM, 2.13 nM, 1.69 μM, > 10 μM for PARP1, PARP2, HDAC1, HDAC6, respectively, in an enzymatic assay. It exhibits anti-proliferative and anti-tumor effects. It also induces DNA damage and apoptosis in vitro. | ||
| E1614 | OUL232 | OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies. | ||
| S9893 | Venadaparib(IDX-1197) | Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells. | ||
| E8293New | YD54 | YD54 is a potent, selective and orally bioavailable PROTAC and a degrader of SMARCA2 with DC50 of 8.1 nM at 24 hours. It exhibits antitumor activity in SMARCA4-mutant lung cancer xenograft models and can be used in research on non-small cell lung cancer. | ||
| E8294New | YDR1 | YDR1 is a potent, selective and orally bioavailable Cereblon-based PROTAC and a degrader of SMARCA2 with DC50 of 60 nM at 48 hours. It exhibits antitumor activity in SMARCA4-mutant lung cancer xenograft models and can be used in research on non-small cell lung cancer. | ||
| E1985 | YD23 | YD23 is a PROTAC which induces the degradation of SMARCA2. It reduces chromatin accessibility in SMARCA4-deficient cells, affecting gene enhancers related to cell cycle and growth regulation, which leads to the downregulation of several cell cycle genes. It also selectively inhibits the growth of SMARCA4 mutant lung cancer cells in vitro. | ||
| S0056 | (E/Z)-BCI | (E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells. | ||
| S8479 | LLY-284 | LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. This compound is much less active than LLY-283 and can be used as a negative control for it. | ||
| E1871 | TNG-462 | TNG-462 is an orally active, potent and selective inhibitor of methylthioadenosine (MTA)-cooperative PRMT5. It exhibits significant antitumor activity, including durable regressions and complete responses, against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation solid tumors. | ||
| E1600 | AMG 193 | AMG-193 is an orally active and MTA-cooperative inhibitor of PRMT5 with potent biochemical and cellular activity. AMG-193, in combination with MTA, selectively targets and inhibits the growth of MTAP-deficient tumor cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumor activity. | ||
| E4942New | Talazoparib tosylate | Talazoparib tosylate (BMN 673ts) is a potent, orally bioavailable PARP1/2 inhibitor exhibiting an IC50 of 0.57 nM against PARP1. | ||
| S6882 | HI-TOPK-032 | HI-TOPK-032 is a potent and specific inhibitor of TOPK. This compound also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. | ||
| E4869 | Niraparib hydrochloride | Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity. | ||
| S9360 | 4-Hydroxyquinazoline | 4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM. | ||
| E0636 | GSK-1520489A | GSK-1520489A(EX-A5430) is an active Protein Kinase, Membrane Associated Tyrosine/Threonine 1 (PKMYT1) inhibitor. | ||
| E1955New | TNG348 | TNG348 is an orally bioavailable allosteric inhibitor targeting the ubiquitin-specific protease USP1. It selectively and potently blocks USP1 activity, preventing deubiquitination of proliferative PCNA and FANCD2, which disrupts DNA repair mechanisms. TNG348 demonstrates inhibitory effects against BRCA1/2-mutated and homologous recombination-deficient (HRD) breast and ovarian cancers . | ||
| E0947 | Iu1-248 | Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM. | ||
| E1118New | SJB3-019A | SJB3-019A is a potent inhibitor of USP1 that significantly suppresses cell proliferation and induces apoptosis in B-cell acute lymphoblastic leukemia (B-ALL) cells. It also promotes DNA-binding-1 (ID1) degradation in K562 cells. | ||
| E4719 | XYL-1 | XYL-1 is a highly potent inhibitor of PARP7 with and IC50 of 0.6 nM. It could enhance the type-Ⅰinterferon signaling in vitro, and can be a potential candidate for developing cancer immunotherapy agents. | ||
| E1481New | AM-9747 | AM-9747 (PRMT5-IN-25) is a potent inhibitor of PRMT5 with a Ki of 0.06 nM. It exhibits antiproliferative activity and a significant oral antitumor effect in mouse models employing patient-derived xenografts (PDX). | ||
| E5851New | T26 | T26( PARP1-IN-35) is a potent, selective, orally active, inhibitor of PARP1 capable of crossing the blood-brain barrier, with IC50 values of 0.2 nM. It exhibits significant antitumor efficacy and holds potential as a research treatment for breast cancer metastases. | ||
| E7366 | Veliparib dihydrochloride | Veliparib dihydrochloride is an orally active and potent inhibitor of both PARP-1 and PARP-2 with Kis of 5.2 nM and 2.9 nM, respectively. It exhibit ability to cross the blood-brain barrier and potentiate DNA-damaging agents in preclinical tumor model. | ||
| E1529 | ART812 | ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. | ||
| E1989 | ART0380 (Alnodesertib) | ART0380 (IACS-030380) is a potent and selective, orally bioavailable inhibitor of ATR kinase, with an IC50 of 51.7 nM effectively inhibiting the enzyme activity of the ATR-ATRIP complex. It functions as an ATP-competitive inhibitor, binding to the ATP pocket of ATR, where ATP would typically bind. It interacts with the hinge through its morpholine oxygen and occupies the ribose pocket with a sulfoximine group. It also exhibits antitumor activity. | ||
| E1518 | DPQ | DPQ is a potent inhibitor of Poly (ADP-ribose) polymerase (PARP), with an IC50 of 40 nM for PARP1. It also suppresses macrophage-mediated inflammation and mitigates acute lung injury (ALI) induced by lipopolysaccharide (LPS) challenge in mice. | ||
| E1136 | SKLB-197 | SKLB-197 exerts selectively inhibition against ataxia telangiectasia mutated and Rad3-related (ATR) kinase with IC50 of 0.013 μM, also displays potent antitumor activity against ATM-deficent tumors both in vitro and in vivo. | ||
| E1806 | AGI-24512 | AGI-24512 is an inhibitor of MAT2A with an IC50 of 8 nM. It increases R-Loop formation and DNA damage in MTAP-deleted and WT cell models. It also exhibits anti-proliferative activity in vitro. | ||
| S6943 | IU1-47 | IU1-47 is a potent and specific inhibitor of USP14 with an IC50 of 0.6 μM. This compound shows ∼33-fold selectivity for USP14 over USP5 (IsoT). | ||
| S8876 | RK-287107 | RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. This compound inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. | ||
| E7768 | C527 | C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM). | ||
| E1512 | M3541 | M3541 is a potent and selective inhibitor of ATM kinase activity with an IC50 value of 0.25 nM in cell-free assays. This compound suppresses double-strand breaks (DSB) repair, clonogenic cancer cell growth and potentiates antitumor activity of ionizing radiation in cancer cell lines. | ||
| E4701 | CMP-5 | CMP5 is a potent and selective small molecule inhibitor of PRMT5. It is found to selectively block S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. It also exhibit potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes. | ||
| E6541New | PolQi2 | PolQi2 is a PolΘ inhibitor that specifically targets the N-terminal helicase domain of PolΘ, thereby suppressing alt-EJ (alternative end-joining) repair. This compound improves the accuracy and integration efficiency of gene editing across multiple loci and diverse cell lines. Additionally, PolQi2 demonstrates synergistic effects with DNA-PK inhibitors in reducing Cas9-mediated off-target activity. Its application is suitable for gene editing studies. | ||
| E4737 | Potrasertib | Potrasertib (IMP7068, WEE1-IN-10) is a potent and selective inhibitor of WEE1 Kinase. It displays antitumor activity and is well-tolerated in patients with advanced solid tumors. | ||
| E1658 | PRT543 | PRT543 is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) with broad antitumor activity in vitro and in vivo. It also inhibits the methyltransferase activity of the PRMT5/MEP50 complex with an IC50 of 10.8 nM. | ||
| E8059 | VH032-cyclopropane-F | VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4. | ||
| E0449 | SGC-SMARCA-BRDVIII |
SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor. |
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| S9872 | AG-270 | AG-270 is a potent and non-competitive methionine adenosyltransferase 2A (MAT2A) inhibitor which lessens the intracellular SAM levels and MTAP-null–selective antiproliferative activity. | ||
| E1711 | FHT-1015 | FHT-1015 is a potent, small-molecule, allosteric inhibitor of SMARCA4/SMARCA2 ATPase with IC50 values ≤10 nM. FHT-1205 decreases PD1+TIM3+ cells and cytokine expression in vivo. | ||
| E1429 | T1-44 | T1-44 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits anti-tumor activity in pancreatic cancers. |
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