CDK

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CDK Inhibitors (30)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • P Natl Acad Sci USA, 2011, 108(20):8414-9
  • AIDS, 2014, 28(15):2213-22
  • Int J Cancer, 2013, 133(10):2341-50
S1153 Roscovitine (Seliciclib,CYC202) Roscovitine (Seliciclib, CYC202) 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.
  • Circ Res, 2012, 111(2):201-11
  • J Neurosci, 2012, 32(32):11050-66
  • Cancer Lett, 2014, 356(2 Pt B):656-68
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. Phase 1.
  • Proc Natl Acad Sci USA, 2013, 110(33):13588-93
  • Leukemia, 2015, 10.1038/leu.2015.99
  • Cell Death Differ, 2014, 21(3):491-502
S2768 Dinaciclib (SCH727965) Dinaciclib (SCH727965) 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. Phase 3.
  • Leukemia, 2015, 10.1038/leu.2015.99
  • ACS Chem Biol, 2014, 9(5):1160-71
  • ACS Chem Biol, 2013, 8(11):2360-5
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.
  • Nat Med, 2015, 10.1038/nm.3855
  • Leukemia, 2014, 28(3):629-41
  • P Natl Acad Sci USA, 2011, 108(20):8414-9
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.
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.
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.
  • J Cell Biol, 2015, 209(2):221-34
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.
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.
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. Phase 2.
  • Nat Biotechnol, 2014, 32(1):92-6
  • Cancer Lett, 2014, 342(1):159-66
  • AIDS, 2014, 28(15):2213-22
S2679 Flavopiridol (Alvocidib) HCl Flavopiridol HCl 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. Phase 1/2.
  • Leukemia, 2014, 28(3):629-41
  • Proc Natl Acad Sci USA, 2011, 108(20):8414-9
  • Mol Cancer Ther, 2012, 11(11):2321-30
S7461 LDC000067 LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.
S7509 ML167 ML167 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.
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.
S7158 LY2835219 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.
  • Biochem J, 2014, 459(3):513-24
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.
S8058 P276-00 P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3.
S7440 Ribociclib (LEE011) Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
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, 2014, 5:3561
  • Mol Cancer Ther, 2014, 13(3):662-74
  • Antimicrob Agents Chemother, 2014, 58(8):4486-94
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. Phase 1.
  • Mol Cancer Ther, 2014, 13(3):662-74
  • Anticancer Agents Med Chem, 2011, 11(5):418-26
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.
  • Oncogene, 2014, 10.1038/onc.2014.351
  • Mol Cancer Ther, 2014, 13(3):662-74
  • Breast Cancer Res Tr, 2015, 149(3):715-26
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.
  • Arthritis Rheumatol, 2014, 66(6):1537-46
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.
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.
  • Hum Cell, 2015, 28(3):114-21
S2742 PHA-767491 PHA-767491 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.
  • Leukemia, 2015, 10.1038/leu.2015.99
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. Phase 2.
  • Mol Cancer Ther, 2014, 13(3):662-74
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.
  • Proc Natl Acad Sci USA, 2013, 110(10):4015-20
  • Nucleic Acids Res, 2013, 41(22):10334-44
  • Cell Death Dis, 2013, 4:e973
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.
S2688 R547 R547 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.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1116 Palbociclib (PD-0332991) HCl 30 mg/mL 3 mg/mL <1 mg/mL
S1153 Roscovitine (Seliciclib,CYC202) <1 mg/mL 71 mg/mL 6 mg/mL
S1145 SNS-032 (BMS-387032) <1 mg/mL 76 mg/mL <1 mg/mL
S2768 Dinaciclib (SCH727965) <1 mg/mL 26 mg/mL 8 mg/mL
S1230 Flavopiridol (Alvocidib) <1 mg/mL 15 mg/mL 8 mg/mL
S7808 AT7519 HCl 1 mg/mL 52 mg/mL 28 mg/mL
S7793 Purvalanol A <1 mg/mL 60 mg/mL 13 mg/mL
S7747 Ro-3306 <1 mg/mL 13 mg/mL <1 mg/mL
S7636 SU9516 <1 mg/mL 48 mg/mL 12 mg/mL
S7547 XL413 (BMS-863233) 46 mg/mL <1 mg/mL <1 mg/mL
S1524 AT7519 <1 mg/mL 10 mg/mL <1 mg/mL
S2679 Flavopiridol (Alvocidib) HCl <1 mg/mL 88 mg/mL <1 mg/mL
S7461 LDC000067 <1 mg/mL 74 mg/mL <1 mg/mL
S7509 ML167 <1 mg/mL 67 mg/mL 13 mg/mL
S7114 NU6027 <1 mg/mL 50 mg/mL 3 mg/mL
S7158 LY2835219 100 mg/mL 83 mg/mL 24 mg/mL
S7320 TG003 <1 mg/mL 6 mg/mL <1 mg/mL
S8058 P276-00 88 mg/mL 88 mg/mL 7 mg/mL
S7440 Ribociclib (LEE011) <1 mg/mL 7 mg/mL <1 mg/mL
S2621 AZD5438 <1 mg/mL 74 mg/mL 74 mg/mL
S1487 PHA-793887 <1 mg/mL 72 mg/mL 72 mg/mL
S1249 JNJ-7706621 <1 mg/mL 79 mg/mL <1 mg/mL
S1572 BS-181 HCl 3 mg/mL 83 mg/mL 22 mg/mL
S2014 BMS-265246 <1 mg/mL 20 mg/mL <1 mg/mL
S2670 A-674563 72 mg/mL 72 mg/mL 18 mg/mL
S2742 PHA-767491 <1 mg/mL 24 mg/mL <1 mg/mL
S2751 Milciclib (PHA-848125) <1 mg/mL 92 mg/mL <1 mg/mL
S1579 Palbociclib (PD0332991) Isethionate 50 mg/mL <1 mg/mL <1 mg/mL
S2735 MK-8776 (SCH 900776) <1 mg/mL 3 mg/mL <1 mg/mL
S2688 R547 <1 mg/mL 60 mg/mL <1 mg/mL
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