1782573-67-4

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1782573-67-4 Structure

Identification	Back Directory
[Name] 2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride
[CAS] 1782573-67-4
[Synonyms] RU-SKI 43 HCL;HHAT INHIBITOR 2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride
[Molecular Formula] C22H31ClN2O2S
[MDL Number] MFCD25371547
[MOL File] 1782573-67-4.mol
[Molecular Weight] 423.012

Chemical Properties	Back Directory
[storage temp. ] Store at -20°C
[solubility ] DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
[form ] A crystalline solid
[color ] White to off-white

Hazard Information	Back Directory
[Description] 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 μM). It blocks palmitoylation of Shh without affecting palmitoylation of H-Ras or Fyn, myristoylation of c-Src, or acylation of Wnt3a. RU-SKI 43 is cell-permeable and inhibits both autocrine and paracrine Shh-induced activation of Gli-mediated transcription. In pancreatic cancer cells, RU-SKI 43 reduces both Gli1 activation and proliferation.
[Uses] RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity[1].
[in vivo] RU-SKI 43 hydrochloride has a t_1/2 of 17 min in mouse plasma after IV administration^[1].
[storage] Store at -20°C
[References] [1] Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling.Nat Chem Biol. 2013 Apr;9(4):247-9. DOI:10.1038/nchembio.1184 [2] Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. Oncogene. 2014 Jan 27. doi: 10.1038/onc.2013.575. DOI:10.1038/onc.2013.575

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