PD173952 is a tyrosine kinases inhibitor with IC50s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively. PD173952 is also a potent Myt1 kinase inhibitor with a Ki of 8.1 nM. PD173952 induces apoptosis.
PD173952 (0-1000 nM; 12 h) inhibits tyrosine phosphorylation of p210Bcr-Abl and CrkL in K562 cells in a concentration-dependent manner[1].PD173952 (0.5 μM; 1-4 days) inhibits K562 cell viability[1].PD173952 (0.5 μM; 24 and 48 h) induces apoptosis of K562 and MEG-01 cells[1].
References:
[1]. Dorsey JF, et al. Interleukin-3 protects Bcr-Abl-transformed hematopoietic progenitor cells from apoptosis induced by Bcr-Abl tyrosine kinase inhibitors. Leukemia. 2002 Sep;16(9):1589-95.
[2]. Wichapong K, et al. Application of docking and QM/MM-GBSA rescoring to screen for novel Myt1 kinase inhibitors. J Chem Inf Model. 2014 Mar 24;54(3):881-93.