hsclpp

CLPP-2068 has oral activity and is an activator of human casein hydrolase P (HsClpP) (EC50=50.4 nM). CLPP-2068 exhibits anti proliferative effects (IC50=5.2 nM) in OCI-LY10 cells, and can also reduce mitochondrial membrane potential, increase mitochondrial ROS levels, and induce mitochondrial dysfunction. CLPP-2068 blocks the cell cycle in G1 phase and induces apoptosis in OCI-LY10 cells. CLPP-2068 exhibits anti-tumor activity in a mouse xenograft model.

(R)-ZG197 is a compound that acts as a highly selective activator for Staphylococcus aureus Caseinolytic protease P (Sa ClpP), exhibiting an effective concentration (EC50) of 1.5 μM. It also activates Homo sapiens ClpP (Hs ClpP) with an EC50 of 31.4 μM.

ZK53 is a selective and potent activator of mitochondrial casein hydrolase protease P (HsClpP).ZK53 induces apoptosis and inhibits the hydrolysis of alpha-casein by HsClpP.ZK53 inhibits tumour growth in xenografts and native mouse models.