5.04521

Hhat Inhibitor, RU-SKI 43

• 別名: 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
• 実験式（ヒル表記法）: C₂₂H₃₀N₂O₂S
• CAS番号: 1043797-53-0
• 分子量: 386.55
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: semisolid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 100 mg/mL
• 保管温度: 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 Key: AEENEMOEBJOKGN-UHFFFAOYSA-N

詳細

詳細

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 (K_i = 6,9 µM; [ShhN] = 38 µM) and ShhN-uncompetitive (K_i = 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 (t_1/2 = 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 (K_i = 6,9 µM; [ShhN] = 38 µM) and ShhN-uncompetitive (K_i = 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 (t_1/2 = 17 min; i.v.).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Hhat

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable