目錄:MedChemExpress LLC>>信號(hào)通路>> Taladegib | MedChemExpress (MCE)
| 參考價(jià) | ￥ 1240 |
| 參考價(jià) | ￥ 1240 |
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| CAS | 1258861-20-9 | 純度 | 99.57% |
|---|---|---|---|
| 分子量 | 512.5 | 分子式 | C??H??F?N?O |
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
| 貨號(hào) | HY-13242 | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥 |
MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)。
CAS No. : 1258861-20-9
MCE 國(guó)際站：Taladegib
產(chǎn)品活性：Taladegib (LY2940680) 是一種 smoothened 受體拮抗劑。
研究領(lǐng)域：Stem Cell/Wnt
作用靶點(diǎn)：Smo
In Vitro: Taladegib, a small-molecule antagonist of the smoothened receptor, shows a slight inhibitory effect on cell proliferation without differences between mucin- (IC50: Taladegib=49.8±4.5 μM) and mixed- Cholangiocarcinoma (CCA) (IC50: Taladegib=61.2±21.1 μM). The IC50 for Taladegib inhibition of [3H]MRT-92 binding is right shifted (3- to 100-fold) for the S387AECL2, L325F3.36f, and D473H6.54f mutants but did not differ from that of WT receptor for the other mutants. The ability of SANT-1 to inhibit [3H]MRT-92 binding to V329F3.40f and T466F6.47f mutants is abolished, and it is severely impaired for L325F3.40f, I408F5.51f, and M525G7.45f mutants (4- to 140-fold drop of the IC50), but is not modified for the S387AECL2 mutant. Taken together, these data confirm our docking hypothesis that MRT-92-binding mode differs from that of either Taladegib or SANT-1 by simultaneously occupying binding sites 1 and 2.
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