MS417 (GTPL7512)

MS417 (GTPL7512) 是一种选择性 BET 特异性 BRD4 抑制剂，与 BRD4-BD1 和 BRD4-BD2 结合，IC50 分别为 30、46 nM 和 Kds 分别为 36.1、25.4 nM，对 CBP BRD 的选择性较弱 (IC50, 32.7 &#956 ;M)。

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库存: 现货

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5mg

￥987.00

790.00

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10mg

￥1525.00

1220.00

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50mg

￥3987.00

3190.00

- +
100mg

￥6687.00

5350.00

- +

已选 0 种 0 瓶

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Background

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 weak selectivity at CBP BRD (IC50, 32.7 μM).

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[1].

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[1].

[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.