1609392-27-9
Chemical Structure
Deucravacitinib
Synonym(s): BMS-986165
- CAS No.: 1609392-27-9
- Formula:C20H19D3N8O3
- Molecular Weight:425.46
IUPAC Name: 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide
InChIKey: BZZKEPGENYLQSC-FIBGUPNXSA-N
SMILES: O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]
Biological Activity: Deucravacitinib (BMS-986165) 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 blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Deucravacitinib | 99.93% | Deucravacitinib (BMS-986165) 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 blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus. | ||||||||||||||||||||
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Fadeucravacitinib | 98.04% | Fadeucravacitinib (Tyk2-IN-8) is an orally active selective TYK2 inhibitor with an IC50 of 5.7 nM against the JH2 pseudokinase domain. Fadeucravacitinib specifically binds to the TYK2 JH2 domain to exert allosteric inhibition, reduces JH1 kinase activity, and thereby blocks the TYK2/STAT pathway and pro-inflammatory signaling cascades. Fadeucravacitinib can be used in research related to inflammatory bowel disease. | ||||||||||||||||||||
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Deucravacitinib-13C,d3 | Deucravacitinib-13C,d3 is the 13C- and deuterium labeled Deucravacitinib. Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis. | |||||||||||||||||||||
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Tyk2-IN-25 | Tyk2-IN-25 is a TYK2 inhibitor that binds to the JH2 domain of TYK2. Tyk2-IN-25 inhibits p-STAT4 and p-STAT3 in human peripheral blood mononuclear cells. Tyk2-IN-25 is applicable to research related to multiple diseases such as immune and inflammatory diseases, and neurological diseases. | |||||||||||||||||||||
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References
- [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]
