MS417

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 Vitro MS417 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 Vivo MS417 (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:Solid IC50& 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)

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