cdk1/cyclinb

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.

PHA-793887 has been used in trials studying the treatment of Advanced Metastatic Solid Tumors.

KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.

MeBIO is an agonist of aryl hydrocarbon receptor, with IC50 of 44 and 55 μM for GSK-3 and CDK1 CyclinB, respectively. MeBIO does not affect GSK-3β.

Indirubin-3'-monoxime (Indirubin-3'-oxime) is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100 180 250 nM for Cdk5 p35, Cdk1 cyclin B, Cdk2 cyclin E).

JNJ-7706621 is a potent aurora kinase inhibitor that also inhibits CDK1 and CDK2.

Riviciclib hydrochloride (P276-00) is a novel inhibitor of CDK1, CDK4, and CDK9, with IC50 values of 79 nM, 63 nM, and 20 nM, respectively, currently in Phase 2 3.

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5 P25, and CDK1 cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 with an IC50 value of 2.1 μM against CDK1 cyclin B.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4 6, exhibiting IC50 values of 1.5 μM for CDK4 cyclin D1, 5.6 μM for CDK6 cyclin D1, and 25 μM for Cdk5 p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1 cyclinB, CDK2 cyclinA3, CDK1 CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.

NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).

GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α β and CDK1-cyclinB complex. It inhibits (GSK-3α β) CDK1 CDK5 activity with IC50 values of 5 nM 320 nM 83 nM, respectively.

BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1 2 4 5 6 9.

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

CVT-313 (NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor.

Milciclib (PHA-848125) (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.

AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.

CCT245737 is an orally active, selective Chk1 inhibitor with an IC50 of 1.3 nM, and is >1,000-fold selective over CHK2 and CDK1.

CAN508 is a potent ATP-competitive CDK9 cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9 cyclin T over other CDK cyclin complexes. [Antitumor activity.]

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.

(R)-Atuveciclib is an isomer of Atuveciclib. Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb CDK9 inhibitor with an IC50 value of 13 nm for CDK9 CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.

Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb CDK9 inhibitor with an IC50 value of 13 nm for CDK9 CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.

Indirubin-5-sulfonate shows inhibitory activity against GSK-3β. Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1 cyclin B, CDK2 cyclin A, CDK2 cyclin E, CDK4 cyclin D1,