1609392-28-0
Chemical Structure
Deucravacitinib (hydrochloride)
Synonym(s): BMS-986165 (hydrochloride)
- CAS No.: 1609392-28-0
- Formula:C20H20D3ClN8O3
- Molecular Weight:461.92
InChIKey: LILQGPVDQZORJG-NIIDSAIPSA-N
SMILES: COC1=C(C2=NN(C)C=N2)C=CC=C1NC3=C(N=NC(NC(C4CC4)=O)=C3)C(NC([2H])([2H])[2H])=O.Cl
Biological Activity: Deucravacitinib (BMS-986165) hydrochloride is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib hydrochloride blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib hydrochloride can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus[1][2].
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Deucravacitinib (hydrochloride) | Deucravacitinib (BMS-986165) hydrochloride is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib hydrochloride blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib hydrochloride can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus. | |||||||||||||||||||||
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- [1]. Armstrong AW, et al. Deucravacitinib versus placebo and apremilast in moderate to severe plaque psoriasis: Efficacy and safety results from the 52-week, randomized, double-blinded, placebo-controlled phase 3 POETYK PSO-1 trial. J Am Acad Dermatol. 2023;88(1):29-39. [Content Brief]
- [2]. Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019;62(20):8973-8995. [Content Brief]
Keywords
