HP661 | OXPHOS inhibitor | Probechem Biochemicals

Chemical Structure : HP661

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HP661 (HP 661, HP-661)

货号: PC-20779Not For Human Use, Lab Use Only.

HP661 is a potent, and selective oral complex I OXPHOS inhibitor with 76% inhibition at 1u M in H460 cells using electron flow assays, inhibits high-OXPHOS H460 cell viability with IC50 of 5 nM.

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生物&药学活性

HP661 is a potent, and selective oral complex I OXPHOS inhibitor with 76% inhibition at 1u M in H460 cells using electron flow assays, inhibits high-OXPHOS H460 cell viability with IC50 of 5 nM.
HP661 displays no inhibitory rates against complexes II-IV.
HP661 potently and preferentially blocked the mitochondrial OXPHOS function in high-OXPHOS cancer cells.
HP661 effectively inhibited MEKi tolerance-meditated mitochondrial OXPHOS, indicating the potential of HP661 to sensitize MEKi in KRAS-mutant lung cancer.
HP661 efficiently induced apoptosis of H460 and H441 cells, sensitizes KRAS-mutant NSCLC cells to MEKi therapy.
HP661 not only significantly suppressed tumor growth but also augmented the therapeutic efficacy of trametinib by impairing tumor mitochondrial respiration in mouse model of high-OXPHOS lung cancer.

物理化学性质&存储条件

分子量	661.61
分子式	C31H29F6N7O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-((5-methyl-4-(4-(4-(2,2,2-trifluoroethoxy)benzyl)piperazine-1-carbonyl)-1H-1,2,3-triazol-1-yl)methyl)-N-(4-(trifluoromethyl)phenyl)picolinamide

参考文献

1. Peng He, et al. Journal of Medicinal Chemistry, May 2, 2023

HP661 (HP 661, HP-661)

生物&药学活性

物理化学性质&存储条件

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HP661 (HP 661, HP-661)

生物&药学活性

物理化学性质&存储条件

参考文献

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