VER-00158411

VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC50 values of 4.4 nM and 4.5 nM, respectively[1].

Research Areas >> Cancer

Chk1:4.4 nM (IC50)

Chk2:4.5 nM (IC50)

Cellular sensing of DNA damage, along with concomitant cell cycle arrest, is mediated by a great many proteins and enzymes. One focus of pharmaceutical development has been the inhibition of DNA damage signaling, and checkpoint kinases (CHKs). There have been a number of clinical trial of checkpoint kinase inhibits alone or as a combination therapy for example, as a means to sensitize proliferating tumor cells to chemotherapies that damage DNA. The development of checkpoint kinase inhibitors the treatment of cancer was a major objective in drug discovery[1].

[1]. Ann Gee Lisa OOI, et al. Combination therapy. 26 July 2018. WO2018136010A1