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ESK-001 hydrochloride

Chemical Structure : ESK-001 hydrochloride

CAS No.: 3009133-87-0

ESK-001 hydrochloride (Envudeucitinib hydrochloride)

Catalog No.: PC-25063Not For Human Use, Lab Use Only.

Envudeucitinib hydrochloride (ESK-001 hydrochloride) is a novel allosteric, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 104-149 nM in human whole blood, binds to JH2 domain of TYK2.

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Biological Activity

Envudeucitinib hydrochloride (ESK-001 hydrochloride) is a novel allosteric, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 104-149 nM in human whole blood, binds to JH2 domain of TYK2.
ESK-001 (Envudeucitinib) has no off-target effects on other kinases (IC50 of >30,000 nM for JAK1-3).
ESK-001 (Envudeucitinib) significantly inhibited STAT phosphorylation and downstream IFNγ production stimulated by IL-12, IL-23, and IFNα in human whole blood and peripheral blood mononuclear cells in a concentration-dependent manner.

Physicochemical Properties

M.Wt 462.97
Formula C22H19D6ClN6O3
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

N-(4-((2-methoxy-3-(1-(methyl-d3)-1H-1,2,4-triazol-3-yl)phenyl)amino)-5-(propanoyl-3,3,3-d3)pyridin-2-yl)cyclopropanecarboxamide hydrochloride

References

1. Ucpinar S, et al. Clin Transl Sci. 2024 Dec;17(12):e70094.

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