Description
MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC 50 s of 30, 46 nM and K d s of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD ( IC 50, 32.7 µM).In VitroMS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC 50 s of 30, 46 nM and K d s of 36.1, 25.4 nM, respectively, with less selectivity at CBP BrD (IC 50, 32.7 µM). MS417 effectively blocks BRD4 binding to NF-κB, almost completely suppresses TNFα-induced NF-κB transcription activation in human embryonic kidney 293T cells at 1 µM and also reduces NF-κB p65 acetylation in the HIV-infected RTECs. MS417 (1 µM) modulation of gene transcription in HIV-infected human primary renal tubular epithelial cells. In addition, MS417 suppresses NF-κB-targeted cytokines and chemokines. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoMS417 (0.08 mg/kg) markedly improves renal function, reduces proteinuria and decreases glomerulosclerosis, tubular injury, and infiltration of inflammatory cells in the kidney of Tg26 mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 30 nM (BRD4-BD1), 46 nM (BRD4-BD2), 32.7 µM (CBP BRD), Kd: 36.1 nM (BRD4-BD1), 25.4 nM (BRD4-BD2)