THZ-P1-2 |
カタログ番号GC39823 |
THZ-P1-2 は、クラス初の選択的 PI5P4K 阻害剤であり、PI5P4Kα の IC50 は 190 nM です。 THZ-P1-2 は、PI5P4Kα/β/γ の無秩序なループ上のシステインを共有結合で標的にします。 THZ-P1-2 はオートファジーの混乱を引き起こし、TFEB シグナル伝達をアップレギュレートします。 THZ-P1-2 は、白血病細胞株で抗がん活性を示します。
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Cas No.: 2058075-45-7
Sample solution is provided at 25 µL, 10mM.
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.
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