mitochondrial protease clpp

TR-107 (Anticancer agent 230) is a selective and potent activator of the mitochondrial protease ClpP that inhibits tumor growth in the MDA-MB-231 xenograft model.

THX6 is an activator of human mitochondrial protease ClpP, with an EC50 of 1.18 μM. It displays cytotoxicity in ONC201-resistant SU-DIPG-VI cells, with an IC50 of 0.13 μM. THX6 inhibits the expression of mitochondria-related proteins (such as parkin, TFAM, NRF1, SDHA), leading to impaired mitochondrial function. Additionally, THX6 affects cell membrane lipid metabolism and exhibits antitumor potential.

MS6076 is a mitochondrial protease ClpP activator. It specifically triggers the activation of ClpP protease within the mitochondrial matrix, significantly disrupting the mitochondrial electron transport chain (ETC) by accelerating the degradation of unfolded proteins. MS6076 exhibits strong cytotoxicity against various breast cancer cell lines, including triple-negative breast cancer cells (MDA-MB-468, MDA-MB-231), as well as other subtypes (SK-BR-3, MCF-7, BT-474). This compound is applicable in breast cancer research.

ZG36, a human Caseinolytic protease P (ClpP) agonist, non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, causing mitochondrial dysfunction and inducing leukemic cell death. Additionally, it inhibits the development of acute myeloid leukemia in a xenograft mouse model [1].