Powder: -20°C for 3 years | In solvent: -80°C for 1 year
THZ-P1-2 is a novel, specific inhibitor of PI5P4K that effectively targets PI5P4Kα. With an IC 50 of 190 nM, THZ-P1-2 selectively inhibits PI5P4Kα by forming covalent bonds with cysteine residues located on a disordered loop present in PI5P4Kα/β/γ. This mechanism not only disrupts autophagy but also elevates TFEB signaling. Moreover, THZ-P1-2 exhibits potent anticancer effects in leukemia cell lines, making it a promising candidate for therapeutic applications.
Pack Size | Availability | Price/USD | Quantity |
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5 mg | 5 days | $ 427.00 |
Description | THZ-P1-2 is a novel, specific inhibitor of PI5P4K that effectively targets PI5P4Kα. With an IC 50 of 190 nM, THZ-P1-2 selectively inhibits PI5P4Kα by forming covalent bonds with cysteine residues located on a disordered loop present in PI5P4Kα/β/γ. This mechanism not only disrupts autophagy but also elevates TFEB signaling. Moreover, THZ-P1-2 exhibits potent anticancer effects in leukemia cell lines, making it a promising candidate for therapeutic applications. |
In vitro | THZ-P1-2 (0.2-11.4 μM) exhibits approximately 75% inhibition of PI-4,5-P2 formation by PI5P4Kα and PI5P4Kγ and 50% inhibition by PI5P4Kβ at a concentration of 0.7 μM[1]. THZ-P1-2 (10-100000 nM; 72 hours) shows modest anti-proliferative activity in all six AML/ALL cell lines with IC 50 values in the low micromolar range[1]. Cell Proliferation Assay[1]Cell Line: THP1, SEMK2, OCI/AML-2, HL60, SKM1, NOMO1 cells Concentration: 10-100000 nM Incubation Time: 72 hours Result: Showed anti-proliferative activity in all six AML/ALL cell lines with IC 50 values ranging from 0.87 to 3.95 μM. |
Synonyms | THZ-P1-2 |
Molecular Weight | 531.62 |
Formula | C31H29N7O2 |
CAS No. | 2058075-45-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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THZ-P1-2 2058075-45-7 THZ P1 2 THZ-P-1-2 THZP12 inhibitor inhibit