Tyk2-IN-7 (Compound 48) 是 TYK2 JH2 抑制剂，与 TYK2 JH2 结构域结合，IC50 和 Ki.app 分别为 0.00053 μM 和 0.00007 μM。Tyk2-IN-7 (Compound 48) 是常规 TYK2 正构抑制剂的高选择性替代，抑制 TYK2/JAK1/JAK2 激酶结构域。Tyk2-IN-7 (Compound 48) 抑制小鼠 IL-12 诱导的 IFNγ 药效学模型中以及抑制在 IL-23 和 IL-12 依赖性小鼠结肠炎模型中的功效。
Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 (Compound 48) provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 (Compound 48) provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1]. Tyk2 JH2|0.00053 μM (IC50)|Tyk2 JH2|0.00007 μM (Ki app)
[1]. Moslin R, et al. Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2). J Med Chem. 2019 Jul 17.
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