Deucravacitinib

SKU: orb1308545

Description

Deucravacitinib (BMS-986165) is an oral, allosteric inhibitor that selectively targets the TYK2 pseudokinase (JH2) domain with high potency (IC50 = 1.0 nM). It functions by stabilizing this regulatory domain, thereby blocking IL-12, IL-23, and type I interferon signaling pathways. This mechanism supports its research application in studying autoimmune disease models, both in vitro and in vivo.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Immunology & Inflammation, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1609392-27-9
• MW: 425.46
• Purity: 99.43% (May vary between batches)
• Formula: C₂₀H₁₉D₃N₈O₃
• SMILES: [2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncn(C)n2)c1OC
• Target: Tyrosine Kinases|||JAK|||Interleukin|||IFNAR
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (7.76 mM);DMSO:84.2 mg/mL (197.9 mM)

Bioactivity

• Target IC50:
  IL-12:2–19 nM|Tyk2 JH2:0.2 nM|IFN-α:2–19 nM|IL-23:2–19 nM|JAK1 JH2:1 nM
• In Vivo:
  METHODS: When mirdametinib was used in combination with Deucravacitinib (BMS-986165) (40 μM) in JW23.3 cells, cell growth was observed. RESULTS Both drugs synergistically inhibited cell proliferation and increased cell apoptosis compared to either drug alone.
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• In Vitro:
  METHODS: The mean daily percent inhibition of TYK2 was simulated by Deucravacitinib (BMS-986165) (6 mg/12 mg once daily) at clinically relevant concentrations. RESULTS Deucravacitinib (BMS-986165) had minimal effects on IL-2-induced STAT5 phosphorylation (JAK 1/3) and TPO-induced STAT3 phosphorylation (JAK 2/2).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Deucravacitinib, BMS 986165, BMS986165, BMS-986165, IFNAR, Inhibitor, Interleukin Related, Interleukin, Interferon-α/β receptor, Interferon-alpha/beta receptor, Janus kinase, JAK1-JH2, JAK1 JH2, JAK, inhibit, Tyk2 JH2, TyrosineKinases, Tyrosine Kinases

Compound Identifiers

PubChem CID

134821691