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RU-SKI 43 is an inhibitor of Hhat (IC50 = 0.85 µM).1 It blocks palmitoylation of Shh without affecting palmitoylation of H-Ras or Fyn, myristoylation of c-Src, or acylation of Wnt3a.1 RU-SKI 43 is cell-permeable and inhibits both autocrine and paracrine Shh-induced activation of Gli-mediated transcription.1 In pancreatic cancer cells, RU-SKI 43 reduces both Gli1 activation and proliferation.2
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1. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling. Nat. Chem. Biol. 9(4), 247-249 (2013).
2. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. Oncogene 34, 263-268 (2015).