THZ-P1-2

• CAT Number: I015212
• CAS Number: 2058075-45-7
• Molecular Formula: C₃₁H₂₉N₇O₂
• Molecular Weight: 531.61
• Purity: ≥95%
• Target: Autophagy
• IUPAC Name: 4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]-N-[3-[[6-(1H-indol-3-yl)pyrimidin-4-yl]amino]phenyl]benzamide
• InChI: InChI=1S/C31H29N7O2/c1-38(2)16-6-11-30(39)36-22-14-12-21(13-15-22)31(40)37-24-8-5-7-23(17-24)35-29-18-28(33-20-34-29)26-19-32-27-10-4-3-9-25(26)27/h3-15,17-20,32H,16H2,1-2H3,(H,36,39)(H,37,40)(H,33,34,35)/b11-6+
• InChIKey: MJJJRRMQCUUKEO-IZZDOVSWSA-N
• SMILES: CN(C)CC=CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC(=C2)NC3=NC=NC(=C3)C4=CNC5=CC=CC=C54

THZ-P1-2（Cat No.:I015212） is a unique and selective inhibitor of PI5P4K (phosphatidylinositol 5-phosphate 4-kinase), specifically targeting PI5P4Kα with an IC50 of 190 nM. It forms a covalent bond with cysteines on a disordered loop present in PI5P4Kα, β, and γ. Through this mechanism, THZ-P1-2 disrupts autophagy and enhances TFEB signaling. Notably, THZ-P1-2 demonstrates anticancer activity in leukemia cell lines.

Reference

[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.