Wee1 Inhibitor

What are the applications of Application

Wee1 Inhibitor is a pyrrolocarbazole compound that acts as a potent, ATP-binding site-targeting inhibitor of Wee1

Biological Activity

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

References

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)