| Identification | Back Directory | [Name]
Benzamide, 4-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-N-[3-[[6-(1H-indol-3-yl)-4-pyrimidinyl]amino]phenyl]- | [CAS]
2058075-45-7 | [Synonyms]
THZ-P1-2
Benzamide, 4-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-N-[3-[[6-(1H-indol-3-yl)-4-pyrimidinyl]amino]phenyl]- | [Molecular Formula]
C31H29N7O2 | [MOL File]
2058075-45-7.mol | [Molecular Weight]
531.61 |
| Chemical Properties | Back Directory | [Boiling point ]
765.2±60.0 °C(Predicted) | [density ]
1.334±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.94±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [References]
[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. DOI:10.1016/j.chembiol.2020.02.003 |
|
|