MS417 是一种选择性的 BET 特异性蛋白 BRD4 的抑制剂，能够与 BRD4-BD1 和 BRD4-BD2 结合，IC₅₀ 值分别为 30，46 nM，K_d 值分别为 36.1，25.4 nM; MS417 对 CBP BRD 的选择性较低，IC₅₀ 值为 32.7 μM。

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).

Solid

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)

MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with less selectivity at CBP BrD (IC50, 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[1]. Zhang G, et al. Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem. 2012 Aug 17;287(34):28840-51.

In Vitro: Ethanol : 50 mg/mL (120.51 mM; Need ultrasonic)配制储备液