deucravacitinib

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。

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).

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.