2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride

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2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride manufacturers
2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride Basic information
Product Name:2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride
Synonyms:2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride;RU-SKI 43 HCL;HHAT INHIBITOR;RUSKI 43 hydrochloride,RU SKI 43 hydrochloride
CAS:1782573-67-4
MF:C22H31ClN2O2S
MW:423.01
EINECS:
Product Categories:
Mol File:1782573-67-4.mol
2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride Structure
2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride Chemical Properties
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
Safety Information
MSDS Information
2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride Usage And Synthesis
DescriptionHedgehog 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.
UsesRU-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 t1/2 of 17 min in mouse plasma after IV administration[1].

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
2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride Preparation Products And Raw materials
Tag:2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride(1782573-67-4) Related Product Information
Ethanone, 1-[6,7-dihydro-4-[(3-Methylphenoxy)Methyl]thieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-Methylbutyl)aMino]- 2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride Ethanone, 1-[4-[(4-chlorophenoxy)methyl]-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-hydroxybutyl)(2-methoxyethyl)amino]- NA Ethanone, 1-[4-[(3-fluorophenoxy)methyl]-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-hydroxypentyl)(3-methoxypropyl)amino]- Ethanone, 1-[6,7-dihydro-4-(6-methyl-2-pyridinyl)thieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-methylbutyl)amino]-, hydrochloride (1:2)