Taladegib,1258861-20-9

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Taladegib

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 S387A^ECL2, L325F^3.36f, and D473H^6.54f 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 V329F^3.40f and T466F^6.47f mutants is abolished, and it is severely impaired for L325F^3.40f, I408F^5.51f, and M525G^7.45f mutants (4- to 140-fold drop of the IC₅₀), but is not modified for the S387A^ECL2 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  |  SAG  |  Cyclopamine  |  Purmorphamine  |  Sonidegib  |  SANT-1  |  Glasdegib  |  DY131  |  20(S)-Hydroxycholesterol  |  BMS-833923  |  KAAD-Cyclopamine  |  Halcinonide  |  PF-5274857  |  Jervine  |  Saridegib  |  GSA-10  |  Saikosaponin B1  |  ALLO-2  |  CUR61414  |  HhAntag  |  LEQ506  |  MK-4101  |  MRT-81  |  MRT-83  |  AZD7254  |  AZD8542

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds