RU-SKI 43

An inhibitor of hedgehog acyltransferase

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2mg

￥875.00

700.00

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5mg

￥1212.00

970.00

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10mg

￥1737.00

1390.00

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50mg

￥7450.00

5960.00

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Background

Hedgehog acyltransferase (Hhat) is an N-palmitoyltransferase that acylates Sonic hedgehog (Shh), which is critical for signaling through Shh. RU-SKI 43 is an inhibitor of Hhat (IC₅₀ = 0.85 ?M).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

1.Petrova, E., Rios-Esteves, J., Ourfelli, O., et al.Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signalingNat. Chem. Biol.9(4)247-249(2013) 2.Petrova, E., Matevossian, A., and Resh, M.D.Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinomaOncogene34263-268(2015)