Hippo signaling pathway, also known as the Salvador/Warts/Hippo (SWH) pathway, controls organ size in animals through the regulation of cell proliferationand apoptosis. The Hippo pathway consists of a core kinase cascade in which Hpo phosphorylates the protein kinase Warts (Wts) Hpo (MST1/2 in mammals) is a member of the Ste-20 family of protein kinases. This highly conserved group of serine/threonine kinases regulates several cellular processes, including cell proliferation, apoptosis, and various stress responses.
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A potent, selective, and ATP-competitive inhibitor of the mammalian Hippo orthologs, Sterile 20–like kinases MST1 and MST2 with IC50 of 71.1 nM and 38.1 nM, respectively; has a selectivity score of 0.05 against a panel of 468 diverse kinases; inhibits phosphorylation of MOB1 in a dose-dependent manner, activates the downstream effector Yes-associated protein (YAP) and promotes cell growth; attenuates acetaminophen-induced liver injury, promotes liver repair and regeneration in mice; a valuable chemical probe to study the Hippo signaling pathway
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