MilliporeSigma™ Calbiochem™ Hhat Inhibitor, RU-SKI 43

Description

• A cell-permeable dihydrothienopyridinyl-ethanone compound that acts as an effective inhibitor against MBOAT family member Hhat/hedgehog acyltransferase-catalyzed ShhN palmitoylation in a palmitoyl CoA-noncompetitive ( K i = 6,9μM; [ShhN] = 38μM) and ShhN-uncompetitive ( K i = 7.4μM; [palmitoyCoA] = 30μM) manner
• Effectively prevents Shh- & Hhat-transfected COS-1 cells from activating hedgehog signaling in co-cultured C3H10T1/2 cells (∽80% inhibition with10μM inhibitor) by inhibiting COS-1 intracellular ShhN palmitoylation (by 52% and 80%, respectively, with 10 or 20μM drug treatment) without affecting cellular palmitoylation of H-ras & fyn, myristoylation of c-Src & Wnt3a, Shh autoprosessing, or the protein level and localization of Shh & Hhat
• Exhibits short plasma half-life in mice ( t 1/2 = 17 min; i.v.).