622855-37-2

WEE1-IN-4 (Compound 15) is a potent checkpoint Wee1 kinase inhibitor with an IC50 of 0.011 μM. Wee1 inhibitors can abrogate the G2/M checkpoint[1].

Wee1 inhibitor is an inhibitor of the checkpoint kinase Wee1 (IC50 = 11 nM).1 It is selective for Wee1 over checkpoint kinase 1 (Chk1; IC50 = 440 nM). Wee1 inhibitor also inhibits the ATPase activity of LptB, an enzyme involved in the transport and assembly of LPS (IC50 = 25 μM for the E. coli enzyme).2

1.Palmer, B.D., Thompson, A.M., Booth, R.J., et al.4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitutionJ. Med. Chem.49(16)4896-4911(2006) 2.Gronenberg, L.S., and Kahne, D.Development of an activity assay for discovery of inhibitors of lipopolysaccharide transportJ. Am. Chem. Soc.132(8)2518-2519(2010)