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Merck
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Key Documents

5.04521

Sigma-Aldrich

Hhat Inhibitor, RU-SKI 43

同義詞:

Hhat Inhibitor, RU-SKI 43, Hedgehog Acyltransferase Inhibitor, RU-SKI43, 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, RU-SKI43, 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

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About This Item

經驗公式(希爾表示法):
C22H30N2O2S
CAS號碼:
分子量::
386.55
分類程式碼代碼:
12352200

化驗

≥98% (HPLC)

品質等級

形狀

semisolid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

off-white

溶解度

DMSO: 100 mg/mL

儲存溫度

2-8°C

InChI

1S/C22H30N2O2S/c1-4-16(2)13-23-14-22(25)24-10-8-21-19(9-11-27-21)20(24)15-26-18-7-5-6-17(3)12-18/h5-7,9,11-12,16,20,23H,4,8,10,13-15H2,1-3H3

InChI 密鑰

AEENEMOEBJOKGN-UHFFFAOYSA-N

一般說明

A cell-permeable dihydrothienopyridinyl-ethanone compound that acts as an effective inhibitor against MBOAT (membrane-bound O-acyltranferase) family member Hhat/hedgehog acyltransferase-catalyzed ShhN palmitoylation in cell-free assays (by 70% at 12.5 µM) in a palmitoyl CoA-noncompetitive (Ki = 6,9 µM; [ShhN] = 38 µM) and ShhN-uncompetitive (Ki = 7.4 µM; [palmitoyCoA] = 30 µM) manner. Effectively prevents Shh- & Hhat-transfected COS-1 cells from activating hedgehog signaling in co-cultured C3H10T1/2 cells (~80% inhibition of AP production in 30 min with10 µM inhibitor) by inhibiting COS-1 intracellular ShhN palmitoylation (by 52% and 80%, respectively, with 10 or 20 µM drug treatment and serum withdrawal 1 h before 4 h [125I]-palmitate incubation). RU-SKI 43 is shown not to interfere with 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.).
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 = 6,9 µM; [ShhN] = 38 µM) and ShhN-uncompetitive (Ki = 7.4 µM; [palmitoyCoA] = 30 µM) manner. Effectively prevents Shh- & Hhat-transfected COS-1 cells from activating hedgehog signaling in co-cultured C3H10T1/2 cells (~80% inhibition with10 µM inhibitor) by inhibiting COS-1 intracellular ShhN palmitoylation (by 52% and 80%, respectively, with 10 or 20 µM 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.).

生化/生理作用

Cell permeable: yes
Primary Target
Hhat
Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他說明

Petrova, E., et al. 2013. Nat. Chem. Biol.9, 247.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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