THZ-P1-2 是一种首创的，选择性的 PI5P4K 抑制剂，对 PI5P4Kα 的 IC50 为 190 nM。THZ-P1-2 共价靶向 PI5P4Kα/β/γ 中无序环上的半胱氨酸。THZ-P1-2 引起自噬破坏，上调 TFEB 信号传导。THZ-P1-2 在白血病细胞系中显示抗癌活性。
货号:ajcx17370
CAS:2058075-45-7
分子式:C31H29N7O2
分子量：531.61
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines[1].

[1]. Sivakumaren SC, et al. Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. Cell Chem Biol. 2020;27(5):525‐537.e6.