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CAS No. : 1258861-20-9
MCE 国际站: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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Liver Cancer Compound Library | Rare Diseases Drug Library | Anti-Colorectal Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Purmorphamine (GMP) | IHR-1 | Sonidegib | Saikosaponin B1 | LEQ506 | RL-0070933 | ALLO-2 | GSA-10 | Cyclopamine | SMO-IN-3 | Saridegib | PF-5274857 | TPB15 | BMS-833923 | MRT-83 | SANT-1 | IHR-Cy3 | SMO-IN-2 | SAG hydrochloride | 20(S)-Hydroxycholesterol | Fluticasone | MK-4101 | AZD7254 | MRT-14 | DY131 | Halcinonide | MRT-81
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货号: HY-13242
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