GSK761 | SP140 inhibitor | Probechem Biochemicals

Chemical Structure : GSK761

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GSK761 (GSK-761)

货号: PC-49278Not For Human Use, Lab Use Only.

GSK761 (GSK-761) is the first small molecule inhibitor of bromodomain-containing protein SP140, inhibits macrophage inflammatory function.

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生物&药学活性

GSK761 (GSK-761) is the first small molecule inhibitor of bromodomain-containing protein SP140, inhibits macrophage inflammatory function.
GSK761 reduced monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation in macrophages.
GSK761 specifically reduces SP140 chromatin binding and thereby expression of SP140-regulated genes.
GSK761 inhibits the expression of cytokines, including TNF, by CD14+ macrophages isolated from Crohn's disease (CD) intestinal mucosa.
SP140 is a bromodomain-containing protein expressed predominantly in immune cells.
SP140 preferentially occupies transcriptional start sites in inflammatory macrophages, with enrichment at gene loci encoding pro-inflammatory cytokines/chemokines and inflammatory pathways.

物理化学性质&存储条件

分子量	646.832
分子式	C40H46N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3-(2-(tert-butoxy)ethyl)phenyl)-2-(4-((3-(2-(tert-butoxy)ethyl)phenyl)carbamoyl)phenyl)-1-methyl-1H-benzo[d]imidazole-5-carboxamide

参考文献

1. Ghiboub M, et al. BMC Biol. 2022 Aug 19;20(1):182.

GSK761 (GSK-761)

生物&药学活性

物理化学性质&存储条件

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GSK761 (GSK-761)

生物&药学活性

物理化学性质&存储条件

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