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.). Synonyms: 2-(2-Methylbutylamino)-1-(4-(m-tolyloxymethyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl) ethanone, 2-((2-Methylbutyl)amino)-1-(4-((3-methylphenoxy)methyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)ethanone, Hedgehog Acyltransferase Inhibitor, RU-SKI43 CAS No: 1043797-53-1 Molecular Formula: C22H30N2O2S Primary Target: Hhat Solubility: DMSO Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. 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.
Purity:
98% (HPLC)
Form:
Supplied as an off-white semi-solid.
CAS Number:
[1043797-53-1]
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