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CDK Signaling Pathways

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Catalog No. Product Name Information Product Use Citations Product Validations
E0072New Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S0273 CDK2-IN-73 (CDK2-IN-4) CDK2-IN-73 (CDK2-IN-4, CDK2 inhibitor 73) is a potent and selective inhibitor of CDK2 with IC50 of 44 nM for CDK2/cyclin A.
S0354 Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S0500 Purvalanol B Purvalanol B (NG-95) is a potent and selective inhibitor of cyclin-dependent kinase (CDK) with IC50 of 6 nM, 6 nM, 9 nM and 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively.
S0771 BRD6989 BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA).
Infect Drug Resist, 2021, 14:3135-3143
S1058 BI-1347 BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM.
S1116 Palbociclib (PD-0332991) HCl Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Mol Cancer Ther, 2022, 21(1):48-57
Nat Med, 2021, 10.1038/s41591-020-01168-7
Cancer Cell, 2021, S1535-6108(21)00383-4
S1145 SNS-032 (BMS-387032) SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis. Phase 1.
Cancers (Basel), 2021, 13(15)3906
Cell Death Dis, 2021, 12(11):1048
Cells, 2021, 10(3)550
S1153 Roscovitine (CYC202) Roscovitine (CYC202, Seliciclib, R-roscovitine) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.
Nucleic Acids Res, 2021, 49(13):7492-7506
EMBO J, 2021, e99692
Front Cell Dev Biol, 2021, 9:662868
S1230 Flavopiridol (L86-8275) Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Nature, 2021, 10.1038/s41586-021-03445-y
Genome Res, 2021, 31(6):981-994
J Cell Biol, 2021, 220(7)e202008146
S1249 JNJ-7706621 JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Cancers (Basel), 2021, 13(6)1205
Gland Surg, 2020, 9(2):558-574
EMBO J, 2019, 38(19):e101704
S1487 PHA-793887 PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Mol Cell Biol, 2020, 40(4)
S1524 AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
S1572 BS-181 HCl BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
Cancers (Basel), 2020, 12(12)E3845
Neuroendocrinology, 2020, 10.1159/000509865
Epigenetics Chromatin, 2019, 12(1):11
S1579 Palbociclib (PD0332991) Isethionate Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Mol Cancer Ther, 2022, 21(1):48-57
Nature, 2021, 10.1038/s41586-021-03445-y
Nat Med, 2021, 10.1038/s41591-020-01168-7
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
S2009 Indirubin-3'-monoxime Indirubin-3'-monoxime (Indirubin-3'-oxime) is a selective CDK inhibitor with IC50 of 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM for CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35,respectively. Indirubin-3'-monoxime is a direct and selective 5-lipoxygenase inhibitor with IC50 of 7.8-10 µM.
S2014 BMS-265246 BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4.
Cancers (Basel), 2020, 12(6):E1637
Nature, 2019, 10.1038/s41586-019-1607-3
Nature, 2019, 574(7777):268-272
S2621 AZD5438 AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1.
Nat Commun, 2021, 12(1):3946
J Clin Invest, 2020, 10.1172/JCI122462
Nat Commun, 2020, 11(1):71
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S2670 A-674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.
Sci Signal, 2020, 13(619)
Cancers (Basel), 2020, 12(9)E2668
Biomolecules, 2020, 10(2)
S2672 PF-00562271 Besylate PF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Sci Adv, 2021, 7(40):eabh0363
J Nanobiotechnology, 2021, 19(1):175
Cells, 2021, 10(3)663
S2679 Flavopiridol (L86-8275) HCl Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Nature, 2021, 10.1038/s41586-021-03445-y
Genome Res, 2021, 31(6):981-994
EMBO Rep, 2021, e52023
S2688 R547 R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Cancer Res, 2019, 10.1158/0008-5472.CAN-18-2486
S2735 MK-8776 (SCH 900776) MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.
Nat Genet, 2021, 10.1038/s41588-021-00893-0
Mol Cell, 2021, 81(19):4041-4058.e15
Nat Commun, 2021, 12(1):6667
S2742 PHA-767491 PHA-767491 (CAY10572, NMS 1116354) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM in cell-free assays, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK1 and CHK2.
Mol Cell, 2021, 81(3):426-441.e8
Mol Cell, 2021, S1097-2765(21)00649-3
Mol Cell, 2021, S1097-2765(21)00683-3
S2751 Milciclib (PHA-848125) Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
Sci Rep, 2021, 11(1):7259
Eur J Pharm Sci, 2021, 159:105740
Eur J Pharm Sci, 2021, S0928-0987(21)00042-7
S2768 Dinaciclib (SCH727965) Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.
Cell, 2021, 184(25):6119-6137.e26
Gut, 2021, 70(5):890-899
Sci Adv, 2021, 7(7)eabd2645
S2890 PF-562271 PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Sci Adv, 2021, 7(40):eabh0363
Elife, 2021, 10e63093
J Nanobiotechnology, 2021, 19(1):175
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S4454New FIT-039 FIT-039 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), suppressing replication of a broad spectrum of DNA viruses through inhibition of mRNA transcription.
S4482New Palbociclib Palbociclib (Ibrance, PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.
Mol Cancer Ther, 2022, 21(1):48-57
Cell, 2021, 184(25):6119-6137.e26
Genome Biol, 2021, 22(1):176
S4743 Wogonin Wogonin (Vogonin), a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase.
J Surg Res, 2021, 263:236-244
Exp Ther Med, 2015, 10(3):1066-1070
S5187New Ribociclib hydrochloride Ribociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(7):119044
Mol Cancer Res, 2021, 19(6):1026-1039
Front Oncol, 2021, 11:681530
S5188New Ribociclib succinate Ribociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(7):119044
Mol Cancer Res, 2021, 19(6):1026-1039
Front Oncol, 2021, 11:681530
S5316 NU2058 NU2058 (O(6)-Cyclohexylmethylguanine) is an inhibitor of CDK2 with IC50 value of 17 μM in an isolated enzyme assay. It also potentiates melphalan (DMF 2.3), and monohydroxymelphalan (1.7), but not temozolomide or ionising radiation.
S5716 Abemaciclib (LY2835219) Abemaciclib (LY2835219) is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Nat Med, 2021, 10.1038/s41591-020-01212-6
Nat Commun, 2021, 12(1):5386
Cancers (Basel), 2021, 13(19)5025
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
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S6531 Bohemine Bohemine is a CDK inhibitor with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively.
S6537 CVT-313 CVT-313 is a potent CDK2 inhibitor with an IC50 of 0.5 microM in vitro. It has no effect on other, nonrelated ATP-dependent serine/threonine kinases.
Nucleic Acids Res, 2021, gkab643
S6540 NG 52 NG-52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p with IC50s of 7 and 2 μM, respectively.
S6595 THZ531 THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively.
Neuroendocrinology, 2020, 10.1159/000509865
S6768New CC-671 CC-671 is a selectively dual inhibitor of TTK (human protein kinase monopolar spindle 1 [hMps1]) and CDC like kinase 2 (CLK2) with IC50s of 5 nM and 3 nM for TTK and CLK2, respectively.
S6777 NSC95397 NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
S6871 Sodium oxamate Sodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH‑A. Sodium oxamate (SO) induces G2/M cell cycle arrest via downregulation of the CDK1/cyclin B1 pathway and promotes apoptosis through enhancement of mitochondrial ROS generation.
Aging (Albany NY), 2021, 13(24):25920-25930
Int J Biol Sci, 2021, 17(11):2756-2769
S6884New LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.
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. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone 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.
S7114 NU6027 NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.
Nucleic Acids Res, 2021, gkab584
S7158 Abemaciclib mesylate (LY2835219) Abemaciclib (LY2835219) is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.
Nat Med, 2021, 10.1038/s41591-020-01212-6
Cancer Cell, 2021, S1535-6108(20)30609-7
Nat Commun, 2021, 12(1):3356
S7198 BIO BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.
Mol Cell, 2021, 81(18):3803-3819.e7
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Front Cell Dev Biol, 2021, 9:662868
S7320 TG003 TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC.
Mol Cell, 2020, 80(6):1104-1122.e9
Nat Commun, 2020, 22;11(1):1931
Gastric Cancer, 2020, 24
S7357 PF-562271 HCl PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Sci Adv, 2021, 7(40):eabh0363
Elife, 2021, 10e63093
J Nanobiotechnology, 2021, 19(1):175
S7371New Fadraciclib (CYC065) Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.
S7440 Ribociclib (LEE011) Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.
Cancer Cell, 2021, S1535-6108(21)00492-X
Nat Commun, 2021, 12(1):3356
Cancers (Basel), 2021, 13(3)E372
S7461 LDC000067 LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.
Cell Rep, 2021, 35(11):109233
Autophagy, 2021, 1-19
Aging (Albany NY), 2021, 13(11):14892-14909
S7509 ML167 ML167 (CID 44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B.
SLAS Discov, 2018, 23(8):850-861
S7511 LY2857785 LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM).
Cancers (Basel), 2021, 13(15)3906
S7547 XL413 (BMS-863233) XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2.
Nucleic Acids Res, 2021, gkab628
Mol Syst Biol, 2021, 17(11):e10396
Cell, 2020, 182(3):685-712.e19
S7549 THZ1 2HCl THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.
Nature, 2021, 10.1038/s41586-021-04116-8
ACS Nano, 2021, 10.1021/acsnano.1c04570
Sci Adv, 2021, 7(48):eabf6123
S7636 SU9516 SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.
Cell Chem Biol, 2019, 26(1):121-130
Biotechnol Lett, 2017, 39(7):951-957
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Mol Imaging Biol, 2019, 21(4):705-712
S7747 Ro-3306 RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
Science, 2021, 371(6535)eabc5386
Cancer Cell, 2021, S1535-6108(21)00659-0
Mol Cell, 2021, S1097-2765(20)30951-5
S7773 CDKI-73 CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.
S7793 Purvalanol A Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Cancer Lett, 2021, 526:53-65
Mol Neurobiol, 2021, 10.1007/s12035-021-02581-w
Aging (Albany NY), 2020, 12(19):19022-19044
S7808 AT7519 HCl AT7519 HCl is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM in cell-free assays. It is less potent to CDK3 and little active to CDK7. Phase 2.
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
Exp Mol Med, 2020, 10.1038/s12276-020-00537-z
S7917 Kenpaullone Kenpaullone (9-Bromopaullone, NSC-664704) is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Antiviral Res, 2019, 170:104572
S7969 THZ2 THZ2, a THZ1 analog, is a selective inhibitor of CDK7 with IC50 of 13.9 nM. THZ2 efficiently suppresses the clonogenic growth of TNBC cells with IC50 of ~10 nM.
S7992 LDC4297 (LDC044297) LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs).
Mol Cell, 2021, S1097-2765(20)30956-4
Mol Cell, 2019, 74(4):674-687
S8058 Riviciclib hydrochloride (P276-00) Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3.
Arthritis Res Ther, 2021, 23(1):47
BMC Genomics, 2021, 22(1):160
Mol Cell, 2020, 77(6):1322-1339
S8100 K03861 K03861 (AUZ 454,AUZ454) is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely.
Bone, 2021, 145:115837
Cancers (Basel), 2020, 12(6):E1637
Mol Oncol, 2020, 14(12):3153-3168
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S8387 MSC2530818 MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable.
Cell Stem Cell, 2021, 28(6):1105-1124.e19
Nat Biomed Eng, 2021, 10.1038/s41551-021-00757-2
STAR Protoc, 2021, 2(4):100913
S8389 Trilaciclib (G1T28) Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively.
S8520 Senexin A Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.
S8568 G1T38 G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.
S8719 AZD4573 AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.
Cancers (Basel), 2021, 13(15)3906
Front Cell Dev Biol, 2021, 9:641271
Cell Chem Biol, 2020, S2451-9456(20)30380-9
S8722 Samuraciclib (ICEC0942) Samuraciclib (ICEC0942, CT7001) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
S8727 Atuveciclib (BAY-1143572) Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
Nat Commun, 2021, 12(1):7213
Bulletin of the Korean Chemical Society, 2021, 42(3):416-419
Cell Chem Biol, 2020, S2451-9456(20)30380-9
S8730 BAY 1251152 BAY1251152 is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
S8783 JSH-150 JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
S8809 MC180295 MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs.
S8815 BSJ-03-123 BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC)
S8840 SEL120 (SEL120-34A) hydrochloride SEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively.
S8863 YKL-5-124 YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13.
Cell, 2021, 184(25):6119-6137.e26
Cell Rep, 2021, 35(4):109013
S8894 SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors.
S8903 AS2863619 AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells.
S8979 THAL-SNS-032 THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
S8981 NVP-2 NVP-2, a potent, selective, non-neurotoxic and ATP-competitive cyclin dependent kinase 9 (CDK9) inhibitor with IC50 of 0.514 nM for CDK9/CycT activity and induces cell apoptosis.
S9605 Apcin Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.
Prostate, 2021, 10.1002/pros.24257
Breast Cancer, 2021, 10.1007/s12282-021-01242-z
S9650New LY3143921 hydrate LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
S9665 Motixafortide (BL-8040) Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
S9742New Indisulam Indisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition.
S9859New BSJ-4-116 BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.
S9880New MS140 MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC).
S9901New KB-0742 Dihydrochloride

KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.

A5016 Cyclin B1 Rabbit Recombinant mAb

Cyclin B1 Rabbit Recombinant mAb detects endogenous levels of total Cyclin B1.

Arch Biochem Biophys, 2021, 700:108774
Gastric Cancer, 2019, 10.1007/s10120-019-00977-1
Gastric Cancer, 2019, 10.1007/s10120-019-00977-1
A5053 p27 KIP1 Rabbit Recombinant mAb p27 KIP1 Rabbit Recombinant mAb detects endogenous levels of total p27 KIP 1.
Aging (Albany NY), 2020, 12(16):16390-16409
A5081 Cdk8 Rabbit Recombinant mAb Cdk8 Rabbit Recombinant mAb detects endogenous levels of CDK8.
A5127 Cyclin B2 Rabbit Recombinant mAb Cyclin B2 Rabbit Recombinant mAb detects endogenous level of total Cyclin B2.
A5128 Cdk9 Rabbit Recombinant mAb Cdk9 Rabbit Recombinant mAb detects endogenous level of total Cdk9.
A5129 Cdk6 Rabbit Recombinant mAb Cdk6 Rabbit Recombinant mAb detects endogenous level of total Cdk6.
A5197 Cdc16/APC6 Rabbit Recombinant mAb Cdc16/APC6 Rabbit Recombinant mAb detects endogenous level of total Cdc16/APC6.
A5198 CDC34 Rabbit Recombinant mAb CDC34 Rabbit Recombinant mAb detects endogenous level of total CDC34.
A5200 Cdc37 Rabbit Recombinant mAb Cdc37 Rabbit Recombinant mAb detects endogenous level of total Cdc37.
A5268 p57 Kip2 Rabbit Recombinant mAb p57 Kip2 Rabbit Recombinant mAb detects endogenous level of total p57 Kip2.
S7981 CCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Front Cell Dev Biol, 2020, 8:408
E0072New Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S0273 CDK2-IN-73 (CDK2-IN-4) CDK2-IN-73 (CDK2-IN-4, CDK2 inhibitor 73) is a potent and selective inhibitor of CDK2 with IC50 of 44 nM for CDK2/cyclin A.
S0354 Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S0500 Purvalanol B Purvalanol B (NG-95) is a potent and selective inhibitor of cyclin-dependent kinase (CDK) with IC50 of 6 nM, 6 nM, 9 nM and 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively.
S0771 BRD6989 BRD6989 is a selective inhibitor of CDK8 and CDK19. BRD6989 upregulates IL-10. BRD6989 is an analog of the natural product cortistatin A (dCA).
Infect Drug Resist, 2021, 14:3135-3143
S1058 BI-1347 BI-1347 is small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM.
S1116 Palbociclib (PD-0332991) HCl Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Mol Cancer Ther, 2022, 21(1):48-57
Nat Med, 2021, 10.1038/s41591-020-01168-7
Cancer Cell, 2021, S1535-6108(21)00383-4
S1145 SNS-032 (BMS-387032) SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis. Phase 1.
Cancers (Basel), 2021, 13(15)3906
Cell Death Dis, 2021, 12(11):1048
Cells, 2021, 10(3)550
S1153 Roscovitine (CYC202) Roscovitine (CYC202, Seliciclib, R-roscovitine) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.
Nucleic Acids Res, 2021, 49(13):7492-7506
EMBO J, 2021, e99692
Front Cell Dev Biol, 2021, 9:662868
S1230 Flavopiridol (L86-8275) Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Nature, 2021, 10.1038/s41586-021-03445-y
Genome Res, 2021, 31(6):981-994
J Cell Biol, 2021, 220(7)e202008146
S1249 JNJ-7706621 JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Cancers (Basel), 2021, 13(6)1205
Gland Surg, 2020, 9(2):558-574
EMBO J, 2019, 38(19):e101704
S1487 PHA-793887 PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Mol Cell Biol, 2020, 40(4)
S1524 AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
S1572 BS-181 HCl BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
Cancers (Basel), 2020, 12(12)E3845
Neuroendocrinology, 2020, 10.1159/000509865
Epigenetics Chromatin, 2019, 12(1):11
S1579 Palbociclib (PD0332991) Isethionate Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Mol Cancer Ther, 2022, 21(1):48-57
Nature, 2021, 10.1038/s41586-021-03445-y
Nat Med, 2021, 10.1038/s41591-020-01168-7
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
S2009 Indirubin-3'-monoxime Indirubin-3'-monoxime (Indirubin-3'-oxime) is a selective CDK inhibitor with IC50 of 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM for CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35,respectively. Indirubin-3'-monoxime is a direct and selective 5-lipoxygenase inhibitor with IC50 of 7.8-10 µM.
S2014 BMS-265246 BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4.
Cancers (Basel), 2020, 12(6):E1637
Nature, 2019, 10.1038/s41586-019-1607-3
Nature, 2019, 574(7777):268-272
S2621 AZD5438 AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1.
Nat Commun, 2021, 12(1):3946
J Clin Invest, 2020, 10.1172/JCI122462
Nat Commun, 2020, 11(1):71
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S2670 A-674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.
Sci Signal, 2020, 13(619)
Cancers (Basel), 2020, 12(9)E2668
Biomolecules, 2020, 10(2)
S2672 PF-00562271 Besylate PF-00562271 Besylate (PF-562271) is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Sci Adv, 2021, 7(40):eabh0363
J Nanobiotechnology, 2021, 19(1):175
Cells, 2021, 10(3)663
S2679 Flavopiridol (L86-8275) HCl Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Nature, 2021, 10.1038/s41586-021-03445-y
Genome Res, 2021, 31(6):981-994
EMBO Rep, 2021, e52023
S2688 R547 R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Cancer Res, 2019, 10.1158/0008-5472.CAN-18-2486
S2735 MK-8776 (SCH 900776) MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.
Nat Genet, 2021, 10.1038/s41588-021-00893-0
Mol Cell, 2021, 81(19):4041-4058.e15
Nat Commun, 2021, 12(1):6667
S2742 PHA-767491 PHA-767491 (CAY10572, NMS 1116354) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM in cell-free assays, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK1 and CHK2.
Mol Cell, 2021, 81(3):426-441.e8
Mol Cell, 2021, S1097-2765(21)00649-3
Mol Cell, 2021, S1097-2765(21)00683-3
S2751 Milciclib (PHA-848125) Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
Sci Rep, 2021, 11(1):7259
Eur J Pharm Sci, 2021, 159:105740
Eur J Pharm Sci, 2021, S0928-0987(21)00042-7
S2768 Dinaciclib (SCH727965) Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.
Cell, 2021, 184(25):6119-6137.e26
Gut, 2021, 70(5):890-899
Sci Adv, 2021, 7(7)eabd2645
S2890 PF-562271 PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Sci Adv, 2021, 7(40):eabh0363
Elife, 2021, 10e63093
J Nanobiotechnology, 2021, 19(1):175
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S4454New FIT-039 FIT-039 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), suppressing replication of a broad spectrum of DNA viruses through inhibition of mRNA transcription.
S4482New Palbociclib Palbociclib (Ibrance, PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.
Mol Cancer Ther, 2022, 21(1):48-57
Cell, 2021, 184(25):6119-6137.e26
Genome Biol, 2021, 22(1):176
S4743 Wogonin Wogonin (Vogonin), a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase.
J Surg Res, 2021, 263:236-244
Exp Ther Med, 2015, 10(3):1066-1070
S5187New Ribociclib hydrochloride Ribociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(7):119044
Mol Cancer Res, 2021, 19(6):1026-1039
Front Oncol, 2021, 11:681530
S5188New Ribociclib succinate Ribociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(7):119044
Mol Cancer Res, 2021, 19(6):1026-1039
Front Oncol, 2021, 11:681530
S5316 NU2058 NU2058 (O(6)-Cyclohexylmethylguanine) is an inhibitor of CDK2 with IC50 value of 17 μM in an isolated enzyme assay. It also potentiates melphalan (DMF 2.3), and monohydroxymelphalan (1.7), but not temozolomide or ionising radiation.
S5716 Abemaciclib (LY2835219) Abemaciclib (LY2835219) is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Nat Med, 2021, 10.1038/s41591-020-01212-6
Nat Commun, 2021, 12(1):5386
Cancers (Basel), 2021, 13(19)5025
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
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S6531 Bohemine Bohemine is a CDK inhibitor with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively.
S6537 CVT-313 CVT-313 is a potent CDK2 inhibitor with an IC50 of 0.5 microM in vitro. It has no effect on other, nonrelated ATP-dependent serine/threonine kinases.
Nucleic Acids Res, 2021, gkab643
S6540 NG 52 NG-52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p with IC50s of 7 and 2 μM, respectively.
S6595 THZ531 THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively.
Neuroendocrinology, 2020, 10.1159/000509865
S6768New CC-671 CC-671 is a selectively dual inhibitor of TTK (human protein kinase monopolar spindle 1 [hMps1]) and CDC like kinase 2 (CLK2) with IC50s of 5 nM and 3 nM for TTK and CLK2, respectively.
S6777 NSC95397 NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
S6871 Sodium oxamate Sodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH‑A. Sodium oxamate (SO) induces G2/M cell cycle arrest via downregulation of the CDK1/cyclin B1 pathway and promotes apoptosis through enhancement of mitochondrial ROS generation.
Aging (Albany NY), 2021, 13(24):25920-25930
Int J Biol Sci, 2021, 17(11):2756-2769
S6884New LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.
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. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone 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.
S7114 NU6027 NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.
Nucleic Acids Res, 2021, gkab584
S7158 Abemaciclib mesylate (LY2835219) Abemaciclib (LY2835219) is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.
Nat Med, 2021, 10.1038/s41591-020-01212-6
Cancer Cell, 2021, S1535-6108(20)30609-7
Nat Commun, 2021, 12(1):3356
S7198 BIO BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.
Mol Cell, 2021, 81(18):3803-3819.e7
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Front Cell Dev Biol, 2021, 9:662868
S7320 TG003 TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC.
Mol Cell, 2020, 80(6):1104-1122.e9
Nat Commun, 2020, 22;11(1):1931
Gastric Cancer, 2020, 24
S7357 PF-562271 HCl PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.
Sci Adv, 2021, 7(40):eabh0363
Elife, 2021, 10e63093
J Nanobiotechnology, 2021, 19(1):175
S7371New Fadraciclib (CYC065) Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.
S7440 Ribociclib (LEE011) Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.
Cancer Cell, 2021, S1535-6108(21)00492-X
Nat Commun, 2021, 12(1):3356
Cancers (Basel), 2021, 13(3)E372
S7461 LDC000067 LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.
Cell Rep, 2021, 35(11):109233
Autophagy, 2021, 1-19
Aging (Albany NY), 2021, 13(11):14892-14909
S7509 ML167 ML167 (CID 44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B.
SLAS Discov, 2018, 23(8):850-861
S7511 LY2857785 LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM).
Cancers (Basel), 2021, 13(15)3906
S7547 XL413 (BMS-863233) XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2.
Nucleic Acids Res, 2021, gkab628
Mol Syst Biol, 2021, 17(11):e10396
Cell, 2020, 182(3):685-712.e19
S7549 THZ1 2HCl THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.
Nature, 2021, 10.1038/s41586-021-04116-8
ACS Nano, 2021, 10.1021/acsnano.1c04570
Sci Adv, 2021, 7(48):eabf6123
S7636 SU9516 SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.
Cell Chem Biol, 2019, 26(1):121-130
Biotechnol Lett, 2017, 39(7):951-957
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Mol Imaging Biol, 2019, 21(4):705-712
S7747 Ro-3306 RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
Science, 2021, 371(6535)eabc5386
Cancer Cell, 2021, S1535-6108(21)00659-0
Mol Cell, 2021, S1097-2765(20)30951-5
S7773 CDKI-73 CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.
S7793 Purvalanol A Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Cancer Lett, 2021, 526:53-65
Mol Neurobiol, 2021, 10.1007/s12035-021-02581-w
Aging (Albany NY), 2020, 12(19):19022-19044
S7808 AT7519 HCl AT7519 HCl is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM in cell-free assays. It is less potent to CDK3 and little active to CDK7. Phase 2.
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
Exp Mol Med, 2020, 10.1038/s12276-020-00537-z
S7917 Kenpaullone Kenpaullone (9-Bromopaullone, NSC-664704) is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Antiviral Res, 2019, 170:104572
S7969 THZ2 THZ2, a THZ1 analog, is a selective inhibitor of CDK7 with IC50 of 13.9 nM. THZ2 efficiently suppresses the clonogenic growth of TNBC cells with IC50 of ~10 nM.
S7992 LDC4297 (LDC044297) LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs).
Mol Cell, 2021, S1097-2765(20)30956-4
Mol Cell, 2019, 74(4):674-687
S8058 Riviciclib hydrochloride (P276-00) Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3.
Arthritis Res Ther, 2021, 23(1):47
BMC Genomics, 2021, 22(1):160
Mol Cell, 2020, 77(6):1322-1339
S8100 K03861 K03861 (AUZ 454,AUZ454) is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely.
Bone, 2021, 145:115837
Cancers (Basel), 2020, 12(6):E1637
Mol Oncol, 2020, 14(12):3153-3168
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S8387 MSC2530818 MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable.
Cell Stem Cell, 2021, 28(6):1105-1124.e19
Nat Biomed Eng, 2021, 10.1038/s41551-021-00757-2
STAR Protoc, 2021, 2(4):100913
S8389 Trilaciclib (G1T28) Trilaciclib (G1T28, G1T28-1) is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively.
S8520 Senexin A Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.
S8568 G1T38 G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.
S8719 AZD4573 AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.
Cancers (Basel), 2021, 13(15)3906
Front Cell Dev Biol, 2021, 9:641271
Cell Chem Biol, 2020, S2451-9456(20)30380-9
S8722 Samuraciclib (ICEC0942) Samuraciclib (ICEC0942, CT7001) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
S8727 Atuveciclib (BAY-1143572) Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
Nat Commun, 2021, 12(1):7213
Bulletin of the Korean Chemical Society, 2021, 42(3):416-419
Cell Chem Biol, 2020, S2451-9456(20)30380-9
S8730 BAY 1251152 BAY1251152 is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
S8783 JSH-150 JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
S8809 MC180295 MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs.
S8815 BSJ-03-123 BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC)
S8840 SEL120 (SEL120-34A) hydrochloride SEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively.
S8863 YKL-5-124 YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for inhibiting CDK7/Mat1/CycH, CDK2 and CDK9 respectively. It displays biochemical and cellular selectivity for CDK7 over CDK12/13.
Cell, 2021, 184(25):6119-6137.e26
Cell Rep, 2021, 35(4):109013
S8894 SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors.
S8903 AS2863619 AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells.
S8979 THAL-SNS-032 THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
S8981 NVP-2 NVP-2, a potent, selective, non-neurotoxic and ATP-competitive cyclin dependent kinase 9 (CDK9) inhibitor with IC50 of 0.514 nM for CDK9/CycT activity and induces cell apoptosis.
S9605 Apcin Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.
Prostate, 2021, 10.1002/pros.24257
Breast Cancer, 2021, 10.1007/s12282-021-01242-z
S9650New LY3143921 hydrate LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
S9665 Motixafortide (BL-8040) Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
S9742New Indisulam Indisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition.
S9859New BSJ-4-116 BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.
S9880New MS140 MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC).
S9901New KB-0742 Dihydrochloride

KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.

A5016 Cyclin B1 Rabbit Recombinant mAb

Cyclin B1 Rabbit Recombinant mAb detects endogenous levels of total Cyclin B1.

Arch Biochem Biophys, 2021, 700:108774
Gastric Cancer, 2019, 10.1007/s10120-019-00977-1
Gastric Cancer, 2019, 10.1007/s10120-019-00977-1
A5053 p27 KIP1 Rabbit Recombinant mAb p27 KIP1 Rabbit Recombinant mAb detects endogenous levels of total p27 KIP 1.
Aging (Albany NY), 2020, 12(16):16390-16409
A5081 Cdk8 Rabbit Recombinant mAb Cdk8 Rabbit Recombinant mAb detects endogenous levels of CDK8.
A5127 Cyclin B2 Rabbit Recombinant mAb Cyclin B2 Rabbit Recombinant mAb detects endogenous level of total Cyclin B2.
A5128 Cdk9 Rabbit Recombinant mAb Cdk9 Rabbit Recombinant mAb detects endogenous level of total Cdk9.
A5129 Cdk6 Rabbit Recombinant mAb Cdk6 Rabbit Recombinant mAb detects endogenous level of total Cdk6.
A5197 Cdc16/APC6 Rabbit Recombinant mAb Cdc16/APC6 Rabbit Recombinant mAb detects endogenous level of total Cdc16/APC6.
A5198 CDC34 Rabbit Recombinant mAb CDC34 Rabbit Recombinant mAb detects endogenous level of total CDC34.
A5200 Cdc37 Rabbit Recombinant mAb Cdc37 Rabbit Recombinant mAb detects endogenous level of total Cdc37.
A5268 p57 Kip2 Rabbit Recombinant mAb p57 Kip2 Rabbit Recombinant mAb detects endogenous level of total p57 Kip2.
S7981 CCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Front Cell Dev Biol, 2020, 8:408
E0072New Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S4454New FIT-039 FIT-039 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9), suppressing replication of a broad spectrum of DNA viruses through inhibition of mRNA transcription.
S4482New Palbociclib Palbociclib (Ibrance, PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.
Mol Cancer Ther, 2022, 21(1):48-57
Cell, 2021, 184(25):6119-6137.e26
Genome Biol, 2021, 22(1):176
S5187New Ribociclib hydrochloride Ribociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(7):119044
Mol Cancer Res, 2021, 19(6):1026-1039
Front Oncol, 2021, 11:681530
S5188New Ribociclib succinate Ribociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Biochim Biophys Acta Mol Cell Res, 2021, 1868(7):119044
Mol Cancer Res, 2021, 19(6):1026-1039
Front Oncol, 2021, 11:681530
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
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S6768New CC-671 CC-671 is a selectively dual inhibitor of TTK (human protein kinase monopolar spindle 1 [hMps1]) and CDC like kinase 2 (CLK2) with IC50s of 5 nM and 3 nM for TTK and CLK2, respectively.
S6884New LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.
S7371New Fadraciclib (CYC065) Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.
S9650New LY3143921 hydrate LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
S9742New Indisulam Indisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition.
S9859New BSJ-4-116 BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.
S9880New MS140 MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC).
S9901New KB-0742 Dihydrochloride

KB-0742 Dihydrochloride is a potent, selective, and orally bioavailable small molecule inhibitor of the transcription elongation cofactor CDK9 with IC50 of 6 nM for CDK9/cyclin T1 inhibition at 10 μM ATP.

Tags: CDK inhibition | CDK and cancer | CDK phosphorylation | CDK activity | CDK activation | CDK assay | CDK inhibitors in clinical trials | CDK inhibitor drugs | CDK inhibitor review