Copanlisib是一个高效的泛I型 PI3K抑制剂,其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3.
MoreTersolisib (STX-478) 是一种高效、突变选择性、变构抑制剂 PI3Kα,可选择性靶向 PI3Kα 的常见突变形式。它对常见的 PI3Kα 螺旋和激酶结构域突变(包括 H1047R 变体)具有很强的疗效,IC50 值为 9.4 nmol/L。与野生型相比,STX-478 对突变型 PI3Kα 的选择性高 14 倍。它可以避免代谢功能障碍并改善 PI3Kα 突变异种移植的治疗反应.
MoreClozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di.
MoreMK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.
MorePF-3084014 is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM.
More
