PD173952

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[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl

Lyn:0.3 nM (IC50)

Abl:1.7 nM (IC50)

Csk:6.6 nM (IC50)

Myt1:8.1 nM (Ki)

PD173952 (0-1000 nM; 12 h) 以浓度依赖方式抑制 K562 细胞中 p210Bcr-Abl 和 CrkL 的酪氨酸磷酸化[1]。 PD173952 (0.5 μM; 1-4 days) 抑制 K562 细胞活力[1]。 PD173952 (0.5 μM; 24 and 48 h) 诱导 K562 和 MEG-01 细胞凋亡[1]。 Western Blot Analysis[1] Cell Line: K562 cells Concentration: 0, 25, 50, 100, 200, 500 and 1000 nM Incubation Time: 12 h Result: Inhibited tyrosine phosphorylation of p210Bcr-Abl and CrkL. Cell Viability Assay[1] Cell Line: K562 cells Concentration: 0.5 μM Incubation Time: 1-4 days Result: Caused cell death in a time-dependent manner. Western Blot Analysis[1] Cell Line: K562 and MEG-01 cells Concentration: 0.5 μM Incubation Time: 24 and 48 h Result: 85-kDa PARP fragment was detected.

[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.