bms 986165

Deucravacitinib是一种高选择性、口服生物可利用的变构 TYK2 抑制剂，用于治疗自身免疫性疾病。它通过稳定调节 JH2 结构域来阻断受体介导的 Tyk2 激活，可抑制IL-12/23和 I 型IFN 途径。它选择性结合 TYK2 假激酶 (JH2)结构域，IC50为1.0 nM。

PF-303 is a covalent-reversible BTK inhibitor. Inhibitors of Bruton's tyrosine kinase (BTK) possess much promise for the treatment of oncologic and autoimmune indications.

Deucravacitinib hydrochloride is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12,IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM),and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-,IL-12-,and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM).

Deucravacitinib-13C,d3是具13C和氘代标记的Deucravacitinib。Deucravacitinib (BMS-986165) 是一种口服生物可利用且具有高效选择性的TYK2变构抑制剂，适用于自身免疫性疾病的研究。该化合物选择性结合并稳定TYK2假激酶 (JH2) 结构域 (IC50=1.0 nM)，阻断受体介导的Tyk2激活，并抑制IL-12/23与I型IFN途径。Deucravacitinib是FDA全球首款从头设计的氘代物，用于中度至重度斑块型银屑病研究。