CDK

CDK製品

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S1116 Palbociclib (PD-0332991) HCl パルボシクリブ塩酸塩 (Palbociclib (PD-0332991) HCl) は選択性の高い CDK4/6 阻害剤であり、cell-free assay における IC50 はそれぞれ 11 nM/ 16 nM です。CDK1/2/5, EGFR, FGFR, PDGFR, InsR その他のターゲットに対しては活性を有しません。臨床第3相試験中
Cancer Cell, 2024, S1535-6108(24)00037-0
Nat Commun, 2024, 15(1):775
Cell Mol Life Sci, 2024, 81(1):29
S1579 Palbociclib Isethionate Palbociclib 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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Cell Mol Life Sci, 2024, 81(1):29
Gastroenterology, 2023, S0016-5085(23)05008-4
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.
Haematologica, 2024, 109(1):231-244
bioRxiv, 2024, 2024.01.17.575938
Nat Commun, 2023, 14(1):6322
S2768 Dinaciclib Dinaciclib 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.
Cancers (Basel), 2024, 16(2)370
Research Square, 2024, 10.21203/rs.3.rs-3857577/v1
Mol Cell, 2023, 83(5):803-818.e8
S1153 Roscovitine 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.
Cell, 2023, 186(21):4694-4709.e16
Nat Commun, 2023, 14(1):6322
Nat Commun, 2023, 14(1):6322
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) 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.
Nat Commun, 2024, 15(1):35
Elife, 2024, 13e80684
Nat Genet, 2023, 55(10):1721-1734
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.
Nat Commun, 2023, 14(1):6270
Cell Death Dis, 2023, 14(2):135
Cell Rep, 2023, 42(5):112529
S4482 Palbociclib Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
Cancer Cell, 2024, S1535-6108(24)00037-0
Nat Commun, 2024, 15(1):775
Clin Cancer Res, 2024, 30(4):703-718
S5716 Abemaciclib Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Cancer Cell, 2024, S1535-6108(24)00037-0
Clin Cancer Res, 2024, 30(4):703-718
Cell Mol Life Sci, 2024, 81(1):29
S7440 Ribociclib Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.
Gastroenterology, 2023, S0016-5085(23)05008-4
Nat Commun, 2023, 14(1):3851
Mol Cell, 2023, 83(1):121-138.e7
S7158 Abemaciclib mesylate Abemaciclib mesylate 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.
Cell Mol Life Sci, 2024, 81(1):29
Nature, 2023, 620(7973):374-380
Cell, 2023, 186(3):528-542.e14
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.
Int J Mol Sci, 2024, 25(2)886
Cancer Cell, 2022, S1535-6108(22)00312-9
Nat Commun, 2022, 13(1):2725
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.
Viruses, 2024, 16(2)282
Cell Rep, 2023, 42(7):112792
Cells, 2023, 12(7)1038
S2679 Flavopiridol (Alvocidib) HCl Flavopiridol (Alvocidib) HClcompetes 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.
Elife, 2024, 13e80684
Int J Biol Macromol, 2023, 258(Pt 1):128776
Mol Cell Biol, 2023, 43(1):1-21
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 decrease GSK3β phosphorylation. AT7519 induces apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
J Cell Biol, 2022, 221-11e202202100
Cell Death Discov, 2022, 8(1):139
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, 2024, 187(3):642-658.e19
Nucleic Acids Research, 2023, 4341–4362
Nucleic Acids Res, 2023, gkad172
S2742 PHA-767491 HCl PHA-767491 (CAY10572, NMS 1116354) HCl 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, 2023, 10.1016/j.molcel.2023.10.011
Cell Rep, 2023, 42(7):112792
Breast Cancer Res, 2023, 25(1):51
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.
Adv Sci (Weinh), 2023, 10(12):e2206542
Bone Res, 2023, 11(1):18
J Transl Med, 2023, 21(1):530
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.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
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.
Signal Transduct Target Ther, 2023, 8(1):302
Transl Oncol, 2023, 35:101729
bioRxiv, 2023, 10.1101/2023.04.03.535285
S2670 A-674563 HCl A-674563 HCl 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.
J Biol Chem, 2024, 300(2):105641
Nat Commun, 2023, 14(1):886
Exp Gerontol, 2023, 173:112091
S7547 XL413 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.
Transl Oncol, 2024, 39:101825
Nat Genet, 2023, 55(8):1311-1323
Nat Commun, 2023, 10.1038/s41467-023-43274-3
S2672 PF-562271 Besylate PF-562271 Besylate 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.
Elife, 2023, 12RP89141
bioRxiv, 2023, 2023.06.02.543509
Front Immunol, 2022, 13:837180
S1249 JNJ-7706621 JNJ-7706621 is a 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.
Microbiol Spectr, 2023, 11(1):e0194322
Cancer Cell, 2022, S1535-6108(22)00312-9
Curr Biol, 2022, 32(19):4314-4324.e7
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.
Nat Commun, 2023, 14(1):505
Curr Biol, 2022, 32(19):4314-4324.e7
Cancers (Basel), 2022, 14(6)1575
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.
Cancers (Basel), 2023, 10.3390/cancers15225424
Cancer Res, 2022, canres.1707.2021
Oncogene, 2022, 41(31):3859-3875
S2751 Milciclib 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, it's also an inhibitor of TRKA with IC50 of 53nM. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
Nat Commun, 2022, 13(1):2725
Eur J Pharm Sci, 2021, 159:105740
Eur J Pharm Sci, 2021, S0928-0987(21)00042-7
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.
Biomed Pharmacother, 2022, 149:112888
Cancers (Basel), 2020, 12(12)E3845
Cancers (Basel), 2020, 12(12)3845
S8100 K03861 (AUZ454) K03861 (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.
Microbiol Spectr, 2023, 11(2):e0491922
Nature, 2022, 604(7904):146-151
Science, 2022, 375(6581):eabl8876
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.
Sci Rep, 2023, 13(1):13763
Sci Rep, 2023, 13(1):13763
Nat Cardiovasc Res, 2022, 1(2):142-156
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.
Nat Commun, 2023, 10.1038/s41467-023-43274-3
Curr Biol, 2022, 32(19):4314-4324.e7
J Cell Biol, 2022, 221-11e202202100
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.
Cell Death Discov, 2022, 8(1):139
Glycobiology, 2022, cwac038
Immun Inflamm Dis, 2022, 10(6):e631
S5187 Ribociclib hydrochloride Ribociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Cancer Res, 2023, 83(1):141-157
Anal Chem, 2023, 95(13):5661-5670
Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8
S5188 Ribociclib succinate Ribociclib (LEE011) succinate is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Anal Chem, 2023, 95(13):5661-5670
Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8
Cell Death Dis, 2022, 13(2):163
S1949 Menadione (Vitamin K3) Menadione (Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
Med -N Y, 2022, S2666-6340-2200365-8
Mol Cell, 2021, S1097-2765(21)00269-0
DNA Repair (Amst), 2021, 105:103152
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.
Cell, 2024, 187(3):642-658.e19
J Pathol, 2023, 261(3):256-268
Cell Rep, 2022, 39(2):110673
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.
Adv Healthc Mater, 2022, e2102345
Sci Adv, 2022, 8(14):eabj3887
Nat Biomed Eng, 2021, 10.1038/s41551-021-00757-2
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
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
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.
Cancer Cell Int, 2023, 10.1186/s12935-023-03079-2
Cancer Cell Int, 2023, 23(1):248
Cell Rep, 2022, 40(7):111218
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.
Cancers (Basel), 2022, 14(19)4695
Nat Commun, 2020, 22;11(1):1931
Mol Cell, 2020, 80(6):1104-1122.e9
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 Commun Signal, 2023, 21(1):94
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
S8727 Atuveciclib (BAY-1143572) Atuveciclib (BAY-1143572) is a 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.
Int Immunopharmacol, 2024, 129:111652
Nat Commun, 2021, 12(1):7213
Bulletin of the Korean Chemical Society, 2021, 42(3):416-419
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.
J Adv Res, 2024, S2090-1232(24)00025-0
Theranostics, 2023, 13(11):3856-3871
Mol Cell Biol, 2023, 10.1080/10985549.2023.2253131
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.
Nucleic Acids Res, 2023, gkad001
Cancer Lett, 2022, 544:215812
Cell Death Dis, 2022, 13(5):450
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.
Clin Cancer Res, 2022, clincanres.3523.2021
EMBO Mol Med, 2022, e14990
Genes Dev, 2022, 36(17-18):956-969
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).
EMBO Mol Med, 2022, e14990
Cell Commun Signal, 2022, 20(1):96
Mol Cell, 2021, S1097-2765(20)30956-4
S8730 Enitociclib (BAY 1251152) Enitociclib (BAY 1251152) 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 Transl Med, 2024, 14(1):e1531
Cancers (Basel), 2023, 16(1)107
Cell Rep, 2022, 41(13):111865
S8816 PF-06873600 PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (CDK2), CDK4, and CDK6 with Ki values of 0.1, 1.2, and 0.1 nM, respectively, blocks the phosphorylation of retinoblastoma protein (RB1), and limits the proliferation of OVCAR-3 ovarian cancer cells with EC50s of 19 and 45 nM, respectively. 
Nat Commun, 2023, 14(1):6796
Nat Commun, 2023, 10.1038/s41467-023-42504-y
PLoS One, 2022, 17(9):e0273182
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.
Cancers -Basel, 2022, 14-174200
J Surg Res, 2021, 263:236-244
Exp Ther Med, 2015, 10(3):1066-1070
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.
Science, 2022, 378(6620):eabn5647
Pathol Oncol Res, 2022, 28:1610273
Front Cell Dev Biol, 2020, 8:408
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.
Mol Cell, 2022, S1097-2765(22)01064-4
Cell Chem Biol, 2019, 26(1):121-130
Biotechnol Lett, 2017, 39(7):951-957
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.
Exp Hematol Oncol, 2023, 12(1):28
Breast Cancer, 2021, 10.1007/s12282-021-01242-z
Prostate, 2021, 10.1002/pros.24257
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.
Sci Adv, 2023, 9(40):eadi3821
Science, 2022, 378(6620):eabn5647
Viruses, 2022, 14(5)1021
S6595 THZ531 THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively.
EMBO Mol Med, 2022, e14990
Cancers (Basel), 2022, 14(11)2755
Neuroendocrinology, 2020, 10.1159/000509865
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.
Nucleic Acids Res, 2023, gkad001
Breast Cancer Res, 2022, 24(1):41
S8722 Samuraciclib (ICEC0942) hydrochloride Samuraciclib (ICEC0942) hydrochloride 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.
Nat Commun, 2023, 14(1):4003
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
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).
Front Immunol, 2023, 14:1196731
Cancers (Basel), 2021, 13(15)3906
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
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
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.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
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.
Int J Biol Sci, 2023, 19(14):4511-4524
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.
Adv Sci (Weinh), 2022, e2202528
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
S8963 HLM006474 HLM006474 is a small molecule pan-E2F inhibitor that inhibits DNA binding to E2F4 with IC50 of 29.8 µM in A375 cells. HLM006474 induces a reduction in cell proliferation and an increase in apoptosis. The CDK/Rb/E2F pathway is commonly disrupted in lung cancer, and HLM006474 is shown to have efficacy in lung cancer.
Cell Death Differ, 2022, 10.1038/s41418-021-00926-5
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.
Science, 2022, 378(6620):eabn5647
S5953 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
S9742 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.
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Pharmaceutics, 2023, 15(3)977
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.
Int J Mol Sci, 2022, 23(18)10597
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
S8925 Simurosertib Simurosertib (TAK-931), an oral cell division cycle 7 (CDC7)-selective inhibitor with an IC50<0.3 nM, induces S phase delay and replication stress and causes mitotic aberrations through centrosome dysregulation and chromosome missegregation, resulting in irreversible antiproliferative effects in cancer cells.
Mol Oncol, 2023, 10.1002/1878-0261.13537
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.
Phytomedicine, 2022, 104:154283
E4578New Trilaciclib dihydrochloride Trilaciclib dihydrochloride(G1T28 dihydrochloride) is a potent inhibitor of CDK4/cyclin D1 and CDK6/cyclin D3 with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride regulates cell proliferation and protects against chemotherapy toxicity in murine and canine bone marrow cells.
E1520New NSC 663284 NSC 663284(DA-3003-10) is a potent, cell-permeable, and irreversible dual specificity phosphatase inhibitor of Cdc25, and exhibits an IC50 of 0.21 μM for Cdc25B2 and is 20 and 450-fold highly selective against Cdc25B2. NSC 663284 also inhibits NSD2 with an IC50 of 170 nM via a direct interaction with the catalytic SET domain.
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.
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.
E2668New Cirtuvivint Cirtuvivint (SM08502) is a potent and orally active inhibitor of CDC-like kinase (CLK) and a DYRK (dual-specificity tyrosine kinase) that targets mRNA splicing and is optimized for Wnt pathway inhibition. Cirtuvivint inhibits serine and arginine-rich splicing factor (SRSF) phosphorylation and disrupts spliceosome activity. Cirtuvivint can be used for solid tumor research.
S0734 Aminopurvalanol A Aminopurvalanol A, a selective,cell permeable and competitive inhibitor of cyclins/Cdk complexes, causes the reduction of in vitro fertilizing ability of boar spermatozoa, by negatively affecting the capacitation-dependent actin polymerization.
S9901 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.
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.
E2504New Toyocamycin Toyocamycin(Vengicide), an adenosine analog, acts as an inhibitor of XBP1. Toyocamycin is also a specific inhibitor of CDK9 with an IC50 value of 79 nM.
S7371 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.
E0474 7BIO 7-bromoindirubin-3-oxime (7BIO), an indirubin derivative derived from indirubin-3-oxime, possesses inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β), also potently inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, and activation of astrocytes and microglia.
E2642 CGP60474 CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively).
JID Innov, 2024, 4(2):100248
E2404 NVP-LCQ195 NVP-LCQ195 (AT9311, LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.
E2370 CDK-IN-2 CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM.
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.
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.
E1495New PF-07220060 (CDK4/6-IN-6) PF-07220060 (CDK4/6-IN-6) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.
S7969 THZ2 Bufalin is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.
E2821 RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
S1058 BI-1347 BI-1347 is a small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM.
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.
S9650 LY3143921 hydrate LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
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.
E0647 (R)-CR8 trihydrochloride (R)-CR8 trihydrochloride, one of CR8 isomers, is a potent inhibitor CDK1/2/5/7/9 with antiproliferative effect and proapoptotic effect on CML cell lines.
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.
S8389 Trilaciclib Trilaciclib 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.
E0072 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.
S8783 JSH-150 JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
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.
Theranostics, 2024, 14(4):1371-1389
E2914New 5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside 5,6-Dichlorobenzimidazole riboside(DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. It trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
S6884 LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.
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.
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).
Gastroenterology, 2024, S0016-5085(24)00062-3
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.
E2202 1-Naphthyl PP1 hydrochloride 1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.
E2658 FN-1501 FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively.
E2640 M2N12 M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09 μM, also shows promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively.
E1605New Avotaciclib trihydrochloride Avotaciclib trihydrochloride(BEY1107 trihydrochloride) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). It can be used for the research of locally advanced or metastatic pancreatic cancer.
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.
S8815 BSJ-03-123 BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC)
S6383 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.
S9878 Tagtociclib (PF-07104091) Tagtociclib (PF-07104091) inhibits CDK2, which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation.
S6768 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.
E0951 Dalpiciclib Dalpiciclib (SHR-6390), a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 and CDK6, exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest. This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
E2373 CAN508 CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM, exhibits a 38-fold selectivity for CDK9/cyclin T1 over other CDK/cyclin complexes.
S1116 Palbociclib (PD-0332991) HCl パルボシクリブ塩酸塩 (Palbociclib (PD-0332991) HCl) は選択性の高い CDK4/6 阻害剤であり、cell-free assay における IC50 はそれぞれ 11 nM/ 16 nM です。CDK1/2/5, EGFR, FGFR, PDGFR, InsR その他のターゲットに対しては活性を有しません。臨床第3相試験中
Cancer Cell, 2024, S1535-6108(24)00037-0
Nat Commun, 2024, 15(1):775
Cell Mol Life Sci, 2024, 81(1):29
S1579 Palbociclib Isethionate Palbociclib 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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Cell Mol Life Sci, 2024, 81(1):29
Gastroenterology, 2023, S0016-5085(23)05008-4
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.
Haematologica, 2024, 109(1):231-244
bioRxiv, 2024, 2024.01.17.575938
Nat Commun, 2023, 14(1):6322
S2768 Dinaciclib Dinaciclib 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.
Cancers (Basel), 2024, 16(2)370
Research Square, 2024, 10.21203/rs.3.rs-3857577/v1
Mol Cell, 2023, 83(5):803-818.e8
S1153 Roscovitine 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.
Cell, 2023, 186(21):4694-4709.e16
Nat Commun, 2023, 14(1):6322
Nat Commun, 2023, 14(1):6322
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) 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.
Nat Commun, 2024, 15(1):35
Elife, 2024, 13e80684
Nat Genet, 2023, 55(10):1721-1734
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.
Nat Commun, 2023, 14(1):6270
Cell Death Dis, 2023, 14(2):135
Cell Rep, 2023, 42(5):112529
S4482 Palbociclib Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
Cancer Cell, 2024, S1535-6108(24)00037-0
Nat Commun, 2024, 15(1):775
Clin Cancer Res, 2024, 30(4):703-718
S5716 Abemaciclib Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
Cancer Cell, 2024, S1535-6108(24)00037-0
Clin Cancer Res, 2024, 30(4):703-718
Cell Mol Life Sci, 2024, 81(1):29
S7440 Ribociclib Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.
Gastroenterology, 2023, S0016-5085(23)05008-4
Nat Commun, 2023, 14(1):3851
Mol Cell, 2023, 83(1):121-138.e7
S7158 Abemaciclib mesylate Abemaciclib mesylate 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.
Cell Mol Life Sci, 2024, 81(1):29
Nature, 2023, 620(7973):374-380
Cell, 2023, 186(3):528-542.e14
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.
Int J Mol Sci, 2024, 25(2)886
Cancer Cell, 2022, S1535-6108(22)00312-9
Nat Commun, 2022, 13(1):2725
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.
Viruses, 2024, 16(2)282
Cell Rep, 2023, 42(7):112792
Cells, 2023, 12(7)1038
S2679 Flavopiridol (Alvocidib) HCl Flavopiridol (Alvocidib) HClcompetes 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.
Elife, 2024, 13e80684
Int J Biol Macromol, 2023, 258(Pt 1):128776
Mol Cell Biol, 2023, 43(1):1-21
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 decrease GSK3β phosphorylation. AT7519 induces apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
J Cell Biol, 2022, 221-11e202202100
Cell Death Discov, 2022, 8(1):139
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, 2024, 187(3):642-658.e19
Nucleic Acids Research, 2023, 4341–4362
Nucleic Acids Res, 2023, gkad172
S2742 PHA-767491 HCl PHA-767491 (CAY10572, NMS 1116354) HCl 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, 2023, 10.1016/j.molcel.2023.10.011
Cell Rep, 2023, 42(7):112792
Breast Cancer Res, 2023, 25(1):51
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.
Adv Sci (Weinh), 2023, 10(12):e2206542
Bone Res, 2023, 11(1):18
J Transl Med, 2023, 21(1):530
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.
Front Immunol, 2022, 13:837180
Cancers (Basel), 2022, 14(6)1537
J Biol Chem, 2022, S0021-9258(22)00119-3
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.
Signal Transduct Target Ther, 2023, 8(1):302
Transl Oncol, 2023, 35:101729
bioRxiv, 2023, 10.1101/2023.04.03.535285
S2670 A-674563 HCl A-674563 HCl 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.
J Biol Chem, 2024, 300(2):105641
Nat Commun, 2023, 14(1):886
Exp Gerontol, 2023, 173:112091
S7547 XL413 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.
Transl Oncol, 2024, 39:101825
Nat Genet, 2023, 55(8):1311-1323
Nat Commun, 2023, 10.1038/s41467-023-43274-3
S2672 PF-562271 Besylate PF-562271 Besylate 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.
Elife, 2023, 12RP89141
bioRxiv, 2023, 2023.06.02.543509
Front Immunol, 2022, 13:837180
S1249 JNJ-7706621 JNJ-7706621 is a 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.
Microbiol Spectr, 2023, 11(1):e0194322
Cancer Cell, 2022, S1535-6108(22)00312-9
Curr Biol, 2022, 32(19):4314-4324.e7
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.
Nat Commun, 2023, 14(1):505
Curr Biol, 2022, 32(19):4314-4324.e7
Cancers (Basel), 2022, 14(6)1575
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.
Cancers (Basel), 2023, 10.3390/cancers15225424
Cancer Res, 2022, canres.1707.2021
Oncogene, 2022, 41(31):3859-3875
S2751 Milciclib 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, it's also an inhibitor of TRKA with IC50 of 53nM. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
Nat Commun, 2022, 13(1):2725
Eur J Pharm Sci, 2021, 159:105740
Eur J Pharm Sci, 2021, S0928-0987(21)00042-7
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.
Biomed Pharmacother, 2022, 149:112888
Cancers (Basel), 2020, 12(12)E3845
Cancers (Basel), 2020, 12(12)3845
S8100 K03861 (AUZ454) K03861 (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.
Microbiol Spectr, 2023, 11(2):e0491922
Nature, 2022, 604(7904):146-151
Science, 2022, 375(6581):eabl8876
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.
Sci Rep, 2023, 13(1):13763
Sci Rep, 2023, 13(1):13763
Nat Cardiovasc Res, 2022, 1(2):142-156
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.
Nat Commun, 2023, 10.1038/s41467-023-43274-3
Curr Biol, 2022, 32(19):4314-4324.e7
J Cell Biol, 2022, 221-11e202202100
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.
Cell Death Discov, 2022, 8(1):139
Glycobiology, 2022, cwac038
Immun Inflamm Dis, 2022, 10(6):e631
S5187 Ribociclib hydrochloride Ribociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Cancer Res, 2023, 83(1):141-157
Anal Chem, 2023, 95(13):5661-5670
Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8
S5188 Ribociclib succinate Ribociclib (LEE011) succinate is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively.
Anal Chem, 2023, 95(13):5661-5670
Sci China Life Sci, 2022, 10.1007/s11427-021-2140-8
Cell Death Dis, 2022, 13(2):163
S1949 Menadione (Vitamin K3) Menadione (Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement.
Med -N Y, 2022, S2666-6340-2200365-8
Mol Cell, 2021, S1097-2765(21)00269-0
DNA Repair (Amst), 2021, 105:103152
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.
Cell, 2024, 187(3):642-658.e19
J Pathol, 2023, 261(3):256-268
Cell Rep, 2022, 39(2):110673
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.
Adv Healthc Mater, 2022, e2102345
Sci Adv, 2022, 8(14):eabj3887
Nat Biomed Eng, 2021, 10.1038/s41551-021-00757-2
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
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
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.
Cancer Cell Int, 2023, 10.1186/s12935-023-03079-2
Cancer Cell Int, 2023, 23(1):248
Cell Rep, 2022, 40(7):111218
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.
Cancers (Basel), 2022, 14(19)4695
Nat Commun, 2020, 22;11(1):1931
Mol Cell, 2020, 80(6):1104-1122.e9
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 Commun Signal, 2023, 21(1):94
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
S8727 Atuveciclib (BAY-1143572) Atuveciclib (BAY-1143572) is a 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.
Int Immunopharmacol, 2024, 129:111652
Nat Commun, 2021, 12(1):7213
Bulletin of the Korean Chemical Society, 2021, 42(3):416-419
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.
J Adv Res, 2024, S2090-1232(24)00025-0
Theranostics, 2023, 13(11):3856-3871
Mol Cell Biol, 2023, 10.1080/10985549.2023.2253131
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.
Nucleic Acids Res, 2023, gkad001
Cancer Lett, 2022, 544:215812
Cell Death Dis, 2022, 13(5):450
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.
Clin Cancer Res, 2022, clincanres.3523.2021
EMBO Mol Med, 2022, e14990
Genes Dev, 2022, 36(17-18):956-969
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).
EMBO Mol Med, 2022, e14990
Cell Commun Signal, 2022, 20(1):96
Mol Cell, 2021, S1097-2765(20)30956-4
S8730 Enitociclib (BAY 1251152) Enitociclib (BAY 1251152) 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 Transl Med, 2024, 14(1):e1531
Cancers (Basel), 2023, 16(1)107
Cell Rep, 2022, 41(13):111865
S8816 PF-06873600 PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (CDK2), CDK4, and CDK6 with Ki values of 0.1, 1.2, and 0.1 nM, respectively, blocks the phosphorylation of retinoblastoma protein (RB1), and limits the proliferation of OVCAR-3 ovarian cancer cells with EC50s of 19 and 45 nM, respectively. 
Nat Commun, 2023, 14(1):6796
Nat Commun, 2023, 10.1038/s41467-023-42504-y
PLoS One, 2022, 17(9):e0273182
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.
Cancers -Basel, 2022, 14-174200
J Surg Res, 2021, 263:236-244
Exp Ther Med, 2015, 10(3):1066-1070
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.
Mol Cell, 2022, S1097-2765(22)01064-4
Cell Chem Biol, 2019, 26(1):121-130
Biotechnol Lett, 2017, 39(7):951-957
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.
Exp Hematol Oncol, 2023, 12(1):28
Breast Cancer, 2021, 10.1007/s12282-021-01242-z
Prostate, 2021, 10.1002/pros.24257
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.
Sci Adv, 2023, 9(40):eadi3821
Science, 2022, 378(6620):eabn5647
Viruses, 2022, 14(5)1021
S6595 THZ531 THZ531 is a selective covalent inhibitor of CDK12 and CDK13 with IC50 values of 158 and 69 nM, respectively.
EMBO Mol Med, 2022, e14990
Cancers (Basel), 2022, 14(11)2755
Neuroendocrinology, 2020, 10.1159/000509865
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.
Nucleic Acids Res, 2023, gkad001
Breast Cancer Res, 2022, 24(1):41
S8722 Samuraciclib (ICEC0942) hydrochloride Samuraciclib (ICEC0942) hydrochloride 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.
Nat Commun, 2023, 14(1):4003
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
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).
Front Immunol, 2023, 14:1196731
Cancers (Basel), 2021, 13(15)3906
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
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
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.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
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.
Int J Biol Sci, 2023, 19(14):4511-4524
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.
Adv Sci (Weinh), 2022, e2202528
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
S8963 HLM006474 HLM006474 is a small molecule pan-E2F inhibitor that inhibits DNA binding to E2F4 with IC50 of 29.8 µM in A375 cells. HLM006474 induces a reduction in cell proliferation and an increase in apoptosis. The CDK/Rb/E2F pathway is commonly disrupted in lung cancer, and HLM006474 is shown to have efficacy in lung cancer.
Cell Death Differ, 2022, 10.1038/s41418-021-00926-5
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.
Science, 2022, 378(6620):eabn5647
S5953 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
S9742 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.
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Pharmaceutics, 2023, 15(3)977
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.
Int J Mol Sci, 2022, 23(18)10597
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
S8925 Simurosertib Simurosertib (TAK-931), an oral cell division cycle 7 (CDC7)-selective inhibitor with an IC50<0.3 nM, induces S phase delay and replication stress and causes mitotic aberrations through centrosome dysregulation and chromosome missegregation, resulting in irreversible antiproliferative effects in cancer cells.
Mol Oncol, 2023, 10.1002/1878-0261.13537
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.
Phytomedicine, 2022, 104:154283
E4578New Trilaciclib dihydrochloride Trilaciclib dihydrochloride(G1T28 dihydrochloride) is a potent inhibitor of CDK4/cyclin D1 and CDK6/cyclin D3 with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride regulates cell proliferation and protects against chemotherapy toxicity in murine and canine bone marrow cells.
E1520New NSC 663284 NSC 663284(DA-3003-10) is a potent, cell-permeable, and irreversible dual specificity phosphatase inhibitor of Cdc25, and exhibits an IC50 of 0.21 μM for Cdc25B2 and is 20 and 450-fold highly selective against Cdc25B2. NSC 663284 also inhibits NSD2 with an IC50 of 170 nM via a direct interaction with the catalytic SET domain.
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.
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.
E2668New Cirtuvivint Cirtuvivint (SM08502) is a potent and orally active inhibitor of CDC-like kinase (CLK) and a DYRK (dual-specificity tyrosine kinase) that targets mRNA splicing and is optimized for Wnt pathway inhibition. Cirtuvivint inhibits serine and arginine-rich splicing factor (SRSF) phosphorylation and disrupts spliceosome activity. Cirtuvivint can be used for solid tumor research.
S0734 Aminopurvalanol A Aminopurvalanol A, a selective,cell permeable and competitive inhibitor of cyclins/Cdk complexes, causes the reduction of in vitro fertilizing ability of boar spermatozoa, by negatively affecting the capacitation-dependent actin polymerization.
S9901 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.
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.
E2504New Toyocamycin Toyocamycin(Vengicide), an adenosine analog, acts as an inhibitor of XBP1. Toyocamycin is also a specific inhibitor of CDK9 with an IC50 value of 79 nM.
S7371 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.
E0474 7BIO 7-bromoindirubin-3-oxime (7BIO), an indirubin derivative derived from indirubin-3-oxime, possesses inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β), also potently inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, and activation of astrocytes and microglia.
E2642 CGP60474 CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively).
JID Innov, 2024, 4(2):100248
E2404 NVP-LCQ195 NVP-LCQ195 (AT9311, LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.
E2370 CDK-IN-2 CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM.
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.
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.
E1495New PF-07220060 (CDK4/6-IN-6) PF-07220060 (CDK4/6-IN-6) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.
S7969 THZ2 Bufalin is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.
E2821 RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
S1058 BI-1347 BI-1347 is a small molecule inhibitor of Cyclin-dependent kinase 8(CDK8) with IC50 of 1.1 nM.
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.
S9650 LY3143921 hydrate LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
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.
E0647 (R)-CR8 trihydrochloride (R)-CR8 trihydrochloride, one of CR8 isomers, is a potent inhibitor CDK1/2/5/7/9 with antiproliferative effect and proapoptotic effect on CML cell lines.
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.
S8389 Trilaciclib Trilaciclib 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.
E0072 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.
S8783 JSH-150 JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.
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.
Theranostics, 2024, 14(4):1371-1389
E2914New 5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside 5,6-Dichlorobenzimidazole riboside(DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. It trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
S6884 LY3405105 LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.
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.
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).
Gastroenterology, 2024, S0016-5085(24)00062-3
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.
E2202 1-Naphthyl PP1 hydrochloride 1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.
E2658 FN-1501 FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively.
E2640 M2N12 M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09 μM, also shows promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively.
E1605New Avotaciclib trihydrochloride Avotaciclib trihydrochloride(BEY1107 trihydrochloride) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). It can be used for the research of locally advanced or metastatic pancreatic cancer.
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.
S8815 BSJ-03-123 BSJ-03-123 is a phthalimide-based degrader of cyclin-dependent kinase 6 (CDK6). (PROTAC)
S6383 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.
S9878 Tagtociclib (PF-07104091) Tagtociclib (PF-07104091) inhibits CDK2, which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation.
S6768 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.
E0951 Dalpiciclib Dalpiciclib (SHR-6390), a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 and CDK6, exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest. This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
E2373 CAN508 CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM, exhibits a 38-fold selectivity for CDK9/cyclin T1 over other CDK/cyclin complexes.
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.
Science, 2022, 378(6620):eabn5647
Pathol Oncol Res, 2022, 28:1610273
Front Cell Dev Biol, 2020, 8:408
E4578New Trilaciclib dihydrochloride Trilaciclib dihydrochloride(G1T28 dihydrochloride) is a potent inhibitor of CDK4/cyclin D1 and CDK6/cyclin D3 with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride regulates cell proliferation and protects against chemotherapy toxicity in murine and canine bone marrow cells.
E1520New NSC 663284 NSC 663284(DA-3003-10) is a potent, cell-permeable, and irreversible dual specificity phosphatase inhibitor of Cdc25, and exhibits an IC50 of 0.21 μM for Cdc25B2 and is 20 and 450-fold highly selective against Cdc25B2. NSC 663284 also inhibits NSD2 with an IC50 of 170 nM via a direct interaction with the catalytic SET domain.
E2668New Cirtuvivint Cirtuvivint (SM08502) is a potent and orally active inhibitor of CDC-like kinase (CLK) and a DYRK (dual-specificity tyrosine kinase) that targets mRNA splicing and is optimized for Wnt pathway inhibition. Cirtuvivint inhibits serine and arginine-rich splicing factor (SRSF) phosphorylation and disrupts spliceosome activity. Cirtuvivint can be used for solid tumor research.
E2504New Toyocamycin Toyocamycin(Vengicide), an adenosine analog, acts as an inhibitor of XBP1. Toyocamycin is also a specific inhibitor of CDK9 with an IC50 value of 79 nM.
E1495New PF-07220060 (CDK4/6-IN-6) PF-07220060 (CDK4/6-IN-6) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.
E2914New 5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside 5,6-Dichlorobenzimidazole riboside(DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. It trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
E1605New Avotaciclib trihydrochloride Avotaciclib trihydrochloride(BEY1107 trihydrochloride) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). It can be used for the research of locally advanced or metastatic pancreatic cancer.

CDK阻害剤の選択性比較

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