Chemical Structure : ESK-001
CAS No.:
2417135-66-9
ESK-001
(Envudeucitinib)
Catalog No.: PC-25062Not For Human Use, Lab Use Only.
ESK-001 (Envudeucitinib) 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ESK-001 (Envudeucitinib) 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
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M.Wt
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426.51
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Formula
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C22H18D6N6O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Ucpinar S, et al. Clin Transl Sci. 2024 Dec;17(12):e70094.
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