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Chemical Structure : THZ-P1-2
CAS No.: 2058075-45-7
Catalog No.: PC-38273Not For Human Use, Lab Use Only.
THZ-P1-2 is a potent, selective, covalent pan-PI5P4K inhibitor with IC50 of 190/700 nM for PI5P4Kα/β, respectively.
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|---|---|---|---|
| 5 mg | $328 | In stock | |
| 10 mg | $498 | In stock | |
| 25 mg | $798 | In stock | |
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| 100 mg | Get quote |
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THZ-P1-2 is a potent, selective, covalent pan-PI5P4K inhibitor with IC50 of 190/700 nM for PI5P4Kα/β, respectively.
THZ-P1-2 exhibited 75% inhibition of PI-4,5-P2 formation PI5P4K γ at 0.7 uM.
THZ-P1-2 binds covalently to all isoforms of the PI5P4K family on unique cysteine residues located on a disordered loop outside the kinase domain.
THZ-P1-2 demonstrates cellular on-target engagement with limited off-targets across the kinome. PIKfyve is an off-target (IC50=40 nM) when used the commercially available DiscoverX KINOMEScan profiling platform.
THZ-P1-2 causes autophagosome clearance defects and upregulation in TFEB nuclear localization and target genes, disrupting autophagy in a covalent-dependent manner and phenocopying the effects of PI5P4K genetic deletion.
THZ-P1-2 is a useful tool to further interrogate the therapeutic potential of PI5P4K inhibition.
| M.Wt | 531.62 | |
| Formula | C31H29N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(E)-N-(3-((6-(1H-Indol-3-yl)pyrimidin-4-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide |
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1. Sindhu Carmen Sivakumaren, et al. Cell Chem Biol. 2020 May 21;27(5):525-537.e6.
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