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MS436

CAS No. : 1395084-25-9

MCE 站：MS436

产品活性：MS436 是一种 bromodomain 抑制剂，有效作用于 BRD4 BrD1，K_i 为 30-50 nM，比作用于 BrD2 选择性高 10 倍。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: MS436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated K_i of 30-50 nM) with preference for the first bromodomain over the second. MS436 effectively inhibits BRD4 activity in NF-κB-directed production of NO and pro-inflammatory cytokine interleukin-6 in murine macrophages. MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression. MS436 exhibits potent affinity of an estimated K_i=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2, which is achieved through a unique set of water-mediated intermolecular interactions.

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