产品描述:
XMD8-92 is an ERK5 inhibitor (Kd = 80 nM) that less potently inhibits DCAMKL2, TNK1, and Plk4 (Kds = 190, 890, and 600 nM, respectively) in a panel of 402 kinases.{31129} It blocks ERK5 autophosphorylation, ERK5-mediated phosphorylation of promyelocytic leukemia protein (PML), and PML-dependent activation of p21.{31129} XMD8-92 inhibits AP-1 transcriptional activity induced by MEK5-activated ERK5 but not that induced by Cdc37.{31128} It inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice and reduces tumor growth in a HeLa mouse xenograft model when administered at a dose of 50 mg/kg twice per day.{31129} XMD8-92 also binds bromodomain-containing protein 4 (BRD4; Kd = 170 nM for BRD4 bromodomain 1).{42864}