Chemical Structure : CLPP-1071
CAS No.:
CLPP-1071
(CLPP1071)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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490.41
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Formula
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C25H24BrN5O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Beijing Chen, et al. J Med Chem. 2024 Nov 22. doi: 10.1021/acs.jmedchem.4c01605.
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