MS-436
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 (IC50values 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.
Product Specifications
Purity
98%
Format
Solid
Molecular Formula
C18H17N5O3S
Shipping Conditions
Room Temperature
Storage Conditions
At least 6 months at -20°C.
Calculated Molecular Weight
383.4 Da
CAS Number
1395084-25-9
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