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MS417

CAS No. : 916489-36-6

MCE 站：MS417

产品活性：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。

研究领域：Epigenetics  |  Anti-infection

作用靶点：Epigenetic Reader Domain  |  HIV

In Vitro: MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC₅₀s of 30, 46 nM and K_ds 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.

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.

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