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 (Ki = 6,9uM; [ShhN] = 38uM) and ShhN-uncompetitive (Ki = 7.4uM; [palmitoyCoA] = 30uM) manner. Effectively prevents Shh- & Hhat-transfected COS-1 cells from activating hedgehog signaling in co-cultured C3H10T1/2 cells (~80% inhibition with10uM inhibitor) by inhibiting COS-1 intracellular ShhN palmitoylation (by 52% and 80%, respectively, with 10 or 20uM 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 (t1/2 = 17 min; i.v.).
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.