CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.
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.
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.
Azathioprine(硫唑嘌呤) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
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.
Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor.
CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
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.