別名

2,6-Dimethylphenyl N-(2,4-dimethoxyphenyl)-N-[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]carbamate,KIN112

生化/生理作用

WH-4-023 (KIN112) is a potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src. WH-4-023 is a somewhat less potent inhibitor of salt-inducible kinases (SIKs) with IC50 values of 10, 22 and 60 nM for SIK 1, 2 and 3 respectively. WH-4-023 was found to support self-renewal of naive human embryonic stem cells, in particular in combination with PD 0325901 (PZ0162), CHIR99021 (SML1046), and SB-590885 (SML0501). WH-4-023 belongs to the Src kinase family. It stimulates apoptosis in GC-resistant T-acute lymphoblastic leukemia (T-ALL) cells.

其他說明

WH-4-023 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the WH-4-023 probe summary on the Chemical Probes Portal website.