XMD8-92

XMD8-92 is a potent and selective dual inhibitor of Extracellular Signal-Regulated Kinase 5 (ERK5, also known as BMK1 or MAPK7) and Bromodomain-containing protein 4 (BRD4). It demonstrates binding affinities (Kd) of 80 nM for ERK5 and 170-190 nM for BRD4, with additional lower-potency activity against DCAMKL2, PLK4, and TNK1. Preclinical research indicates that XMD8-92 possesses anti-cancer properties, specifically inhibiting tumor cell proliferation and tumor-associated angiogenesis in models of lung, cervical, pancreatic, and melanoma cancers. Its mechanism of action involves the modulation of promyelocytic leukemia protein (PML). Although the compound is orally bioavailable with a half-life of approximately 2 hours, it has not advanced to clinical trials and is currently utilized as a research tool.

Other names

2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one