MS-436

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Catalog #

82061

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Description

MS-436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated Ki of 30-50 nM) with preference for the first bromodomain over the second. MS-436 effectively blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC₅₀ values are 3.8 and 4.9 μM, respectively). MS-436 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.

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Synonyms

MS436, MS 436

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Chemical Structure

Product Info

Storage and Usage

Citations

Purity

98%

Format

Solid

Formula

C₁₈H₁₇N₅O₃S

383.4 Da

CAS Registry #

1395084-25-9

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MS-436

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