1018673-42-1
Chemical Structure
GSK3117391
Synonym(s): ESM-HDAC391; CHR-5154; HDAC-IN-3
- CAS No.: 1018673-42-1
- Formula:C22H33N3O4
- Molecular Weight:403.52
IUPAC Name: cyclopentyl (S)-2-cyclohexyl-2-(((6-(3-(hydroxyamino)-3-oxopropyl)pyridin-3-yl)methyl)amino)acetate
InChIKey: AFDPFLDWOXXHQM-NRFANRHFSA-N
SMILES: O=C([C@@H](NCC1=CN=C(CCC(NO)=O)C=C1)C2CCCCC2)OC3CCCC3
Biological Activity: GSK3117391 (ESM-HDAC391; CHR-5154; HDAC-IN-3) is an orally active HDAC inhibitor with a IC50 of 55 nM. Using esterase-sensitive motif technology, GSK3117391 is selectively converted into its active acid metabolite HDAC189 in cells expressing carboxylesterase-1. GSK3117391 induces sustained global protein acetylation in monocytes, inhibits the production of proinflammatory cytokines, depletes circulating monocytes, downregulates the expression of CSF1R, and inhibits monocyte adhesion and differentiation. GSK3117391 can be used in the research of chronic inflammatory diseases[1].
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GSK3117391 | 99.40% | GSK3117391 (ESM-HDAC391; CHR-5154; HDAC-IN-3) is an orally active HDAC inhibitor with a IC50 of 55 nM. Using esterase-sensitive motif technology, GSK3117391 is selectively converted into its active acid metabolite HDAC189 in cells expressing carboxylesterase-1. GSK3117391 induces sustained global protein acetylation in monocytes, inhibits the production of proinflammatory cytokines, depletes circulating monocytes, downregulates the expression of CSF1R, and inhibits monocyte adhesion and differentiation. GSK3117391 can be used in the research of chronic inflammatory diseases. | ||||||||||||||||||||
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Keywords
