CLPP-1071 | ClpP agonist | Probechem Biochemicals

Chemical Structure : CLPP-1071

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CLPP-1071 (CLPP1071)

货号: PC-23501Not For Human Use, Lab Use Only.

CLPP-1071 is a potent, orally efficacious activator of human sapiens caseinolytic protease P (ClpP) with EC50 of 23.5 nM, exhibits HL60 cell growth inhibition with IC50 of 4.6 nM.

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生物&药学活性

CLPP-1071 is a potent, orally efficacious activator of human sapiens caseinolytic protease P (ClpP) with EC50 of 23.5 nM, exhibits HL60 cell growth inhibition with IC50 of 4.6 nM.
CLPP-1071 binds to ClpP (Kd=26.9 nM) and activates with mitochondrial ClpP.
CLPP-1071 has significantly stronger ClpP activation than ONC212, decreases SDHB and NDUFA12 proteins at 1 nM and both proteins even mostly disappeared at 10 nM in HL60 and MOLM13 cells.
CLPP-1071 causes significant mitochondrial damage, induces cell cycle arrest and apoptosis in HL60 and MOLM13.
CLPP-1071 (5-10 mg/kg, p.o, qd) dose-dependently extended the survival of female NSG mice, exerted antitumor activity in vivo.

物理化学性质&存储条件

分子量	490.41
分子式	C25H24BrN5O
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	(R)-3-((4-(4-Bromobenzyl)-8-methyl-5-oxo-1,2,4,5,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-7(6H)-yl)methyl)benzonitrile

参考文献

1. Beijing Chen, et al. J Med Chem. 2024 Nov 22. doi: 10.1021/acs.jmedchem.4c01605.

CLPP-1071 (CLPP1071)

生物&药学活性

物理化学性质&存储条件

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CLPP-1071 (CLPP1071)

生物&药学活性

物理化学性质&存储条件

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