az 32

AZ32 是一种口服生物利用度和血脑屏障穿透性 ATM 抑制剂，对 ATM 酶的 IC50 <6.2 nM，对细胞内 ATM 的 IC50 为 0.31 μM。

Ac32Az19 是一种有效、无毒、高选择性的 BCRP 抑制剂，在BCRP 过度表达的HEK293 R2细胞中，EC50值为13 nM。

AZ3246是一种口服有效的选择性HPK1抑制剂，IC50< 3 nM。它可诱导T细胞分泌IL-2，EC50为90 nM。作为一种低容量、低清除率的抗肿瘤化合物，AZ3246展现出显著的药理特性。

AZ-Tak1 is a potent and a relatively selective inhibitor of TAK1 kinase activity, with an IC50 of 0.009 mM. AZ-Tak1 treatment decreased the level of p38 and ERK in mantle cell lymphoma cells, and induced apoptosis in a dose and time dependent manner, with an IC50 of 0.1–0.5 mM. Using the annexin-V and PI staining and FACS analysis, After 48 hours of incubation, AZ-Tak1 (0.1 mM) induced apoptosis in 28%, 34% and 86% of Mino, SP53, and Jeko cells, respectively, which was increased to 32%, 42%, and 86% when 0.5 mM concentration was used.