CDK

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
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
S8387 MSC2530818 <1 mg/mL 68 mg/mL 68 mg/mL
S8520 Senexin A <1 mg/mL 54 mg/mL 54 mg/mL
S7992 LDC4297 (LDC044297) 27 mg/mL 86 mg/mL 86 mg/mL
S7511 LY2857785 <1 mg/mL 23 mg/mL 42 mg/mL
S4743 Wogonin <1 mg/mL 56 mg/mL 3 mg/mL
S7549 THZ1 2HCl <1 mg/mL 100 mg/mL <1 mg/mL
S1524 AT7519 <1 mg/mL 10 mg/mL <1 mg/mL
S2679 Flavopiridol HCl <1 mg/mL 88 mg/mL <1 mg/mL
S1249 JNJ-7706621 <1 mg/mL 79 mg/mL <1 mg/mL
S2621 AZD5438 <1 mg/mL 74 mg/mL 74 mg/mL
S2735 MK-8776 (SCH 900776) <1 mg/mL 3 mg/mL <1 mg/mL
S1487 PHA-793887 <1 mg/mL 72 mg/mL 72 mg/mL
S1572 BS-181 HCl 3 mg/mL 83 mg/mL 22 mg/mL
S1579 Palbociclib (PD0332991) Isethionate 10 mg/mL <1 mg/mL <1 mg/mL
S2670 A-674563 72 mg/mL 72 mg/mL 18 mg/mL
S7158 abemaciclib (LY2835219) 100 mg/mL 83 mg/mL 24 mg/mL
S2014 BMS-265246 <1 mg/mL 20 mg/mL <1 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
S2688 R547 <1 mg/mL 60 mg/mL <1 mg/mL
S7440 Ribociclib (LEE011) <1 mg/mL 7 mg/mL <1 mg/mL
S7114 NU6027 <1 mg/mL 50 mg/mL 3 mg/mL
S8058 P276-00 88 mg/mL 88 mg/mL 7 mg/mL
S7320 TG003 <1 mg/mL 6 mg/mL <1 mg/mL
S7747 Ro-3306 <1 mg/mL 13 mg/mL <1 mg/mL
S7793 Purvalanol A <1 mg/mL 60 mg/mL 13 mg/mL
S8100 K03861 <1 mg/mL 100 mg/mL 15 mg/mL
S7509 ML167 <1 mg/mL 67 mg/mL 13 mg/mL
S7917 Kenpaullone <1 mg/mL 65 mg/mL <1 mg/mL
S8161 ON123300 <1 mg/mL 29 mg/mL <1 mg/mL
S7461 LDC000067 <1 mg/mL 74 mg/mL <1 mg/mL
S7636 SU9516 <1 mg/mL 48 mg/mL 12 mg/mL
S7808 AT7519 HCl 43 mg/mL 52 mg/mL 28 mg/mL
S7547 XL413 (BMS-863233) 46 mg/mL <1 mg/mL <1 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

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.

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.

S8387New

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.

S8520New

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.

S7992New

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).

S7511New

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).

S4743New

Wogonin

Wogonin, 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.

S7549New

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.

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.

S2679

Flavopiridol 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.

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.

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.

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.

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.

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.

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.

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.

S7158

abemaciclib (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.

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.

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.

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.

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.

S7440

Ribociclib (LEE011)

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.

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.

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.

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.

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.

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.

S8100

K03861

K03861 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.

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.

S7917

Kenpaullone

Kenpaullone is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.

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, PDGFRβ, FGFR1, RET, and Fyn, respectively.

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.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
A5035New

Cyclin D1 Rabbit Recombinant mAb

A5016New

Cyclin B1 Rabbit Recombinant mAb

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