型号:
产品价格:电议      采购度:1628      原产地:美洲
发布时间:2021/7/24 1:01:30 所属地区:上海 上海市
简要描述:
Taladegib (LY2940680) 是一种 smoothened 受体拮抗剂。
标签:LY2940680
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CAS No. : 1258861-20-9
MCE 站:Taladegib
产品活性:Taladegib (LY2940680) 是一种 smoothened 受体拮抗剂。
研究领域:Stem Cell/Wnt
作用靶点: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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更新时间:2024/1/2 10:14:29
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