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Chemical Structure : GSK761
Catalog No.: 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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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.
| M.Wt | 646.832 | |
| Formula | C40H46N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ghiboub M, et al. BMC Biol. 2022 Aug 19;20(1):182.
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