GSK-3117391 |CAS:1018673-42-1 Probechem Biochemicals

Chemical Structure : GSK-3117391

CAS No.: 1018673-42-1

GSK-3117391 (ESM-HDAC391;CHR-5154;GSK3117391;CHR5154)

Catalog No.: PC-63389Not For Human Use, Lab Use Only.

GSK-3117391 (ESM-HDAC391, CHR-5154) is an orally active, myeloid-targeted histone deacetylase (HDAC) inhibitor with IC50 of 55 nM in a HeLa cell nuclear extract fluorometric assay, potently inhibits Class I, Class IIb and Class IV members (HDAC 1/2/3/8, HDAC6/10, and HDAC 11, respectively), with Class IIa enzymes (HDAC4/5/7/9) unaffected.

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10 mg	$398	In stock
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Biological Activity

GSK-3117391 (ESM-HDAC391, CHR-5154) is an orally active, myeloid-targeted histone deacetylase (HDAC) inhibitor with IC50 of 55 nM in a HeLa cell nuclear extract fluorometric assay, potently inhibits Class I, Class IIb and Class IV members (HDAC 1/2/3/8, HDAC6/10, and HDAC 11, respectively), with Class IIa enzymes (HDAC4/5/7/9) unaffected.

GSK-3117391 (ESM-HDAC391, CHR-5154) increases global acetylation in monocytes in human whole blood with EC50 of 158 nM, with marked selectivity over other leucocyte populations.

GSK-3117391 (ESM-HDAC391, CHR-5154) inhibits TNFα production in LPS-stimulated blood (IC50=174 nM).

GSK-3117391 (ESM-HDAC391, CHR-5154) shows rapid conversion to acid metabolite HDAC189 in carboxylesterase-1-expressing cells.

GSK-3117391 (ESM-HDAC391, CHR-5154) is a novel targeted inhibitor demonstrating sustained potent mechanistic engagement and antiinflammatory activity.

Physicochemical Properties

M.Wt	389.496
Formula	C21H31N3O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	cyclopentyl (S)-2-cyclohexyl-2-((6-(3-(hydroxyamino)-3-oxopropyl)pyridin-3-yl)amino)acetate

References

1. Rebecca C Furze, et al. Br J Clin Pharmacol. 2022 Jun 2. doi: 10.1111/bcp.15428.

GSK-3117391 (ESM-HDAC391;CHR-5154;GSK3117391;CHR5154)

Biological Activity

Physicochemical Properties

References

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