Wnt agonist 1

Catalog No.S8178

Wnt agonist 1 Chemical Structure

Molecular Weight(MW): 386.83

Wnt agonist 1 is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.

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  • Both Wnt sinaling activators of agonist and recombinant protein, and therapeutic agents of fluorouracil and docetaxel stimulated TCF-4 promoter functions of wild-type (wt) could be blocked by Nano-Let-7b, compared with negative control group of mutant-type (mut). In detail, Let-7b alone affected the TCF-4 promoter activity effectively, and wnt signaling activators of either Wnt agonist-1 or Wnt protein attenuated the Let-7b functions significantly. Combined usage of therapeutic agent of either fluorouracil or docetaxel with Let-7b increased the TCF-4 activity when compared to groups treated with Let-7b alone, however, the TCF-4 activity when applying combination was still significantly lower than that of controlled group

    Int J Oncol, 2017, 51(4):1077-1088. Wnt agonist 1 purchased from Selleck.

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Biological Activity

Description Wnt agonist 1 is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.
Targets
Wnt/β-catenin [1]
(Cell-based assay)
In vitro

Wnt agonist 1 does not inhibit the activity of GSK-3β, and may be a useful tool in the study of physiological processes that involve the Wnt pathway[1]. Exposure human brain endothelial hCMEC/D3 cells to the Wnt agonist 1 led to an increase in the percentage of cells exhibiting nuclear or perinuclear β-catenin staining after exposure for 16 h to 10 μM (43 ± 2%, p < 0.01, n = 5) and 20 μM (48 ± 5%, p < 0.01, n = 5) compared with that of control (12 ± 1%, n = 5)[2].

In vivo In a Xenopus model, Wnt agonist 1 (10 μM) mimics the effects of Wnt at the whole-organism level, and affects Xenopus embryonic head specification[1]. In animal model (Rat renal IR model), Wnt agonist significantly lowered serum levels of creatinine, AST, and LDH, inhibited the production of IL-6 and IL-1β, and MPO activities. Wnt agonist reduced iNOS, nitrotyrosine proteins and 4-hydroxynonenal in the kidneys. Wnt agonist improves renal regeneration and function while attenuating inflammation and oxidative stress in the kidneys after IR[3].

Protocol

Cell Research:

[1]

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  • Cell lines: 293T cells
  • Concentrations: 10 μM
  • Incubation Time: 24 h
  • Method:

    For high-throughput screening, 293T cells are transiently transfected with the reporter construct in T75 cell culture flasks. After overnight culture, cells are harvested and replated onto 384-well plates with 1.5×103 cells in each well; 24 h later, compound solution (1 mM, 500 nL) is added to each well. After incubation for another 24 h, luciferase activity is measured with BrightGlo.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: Male adult Sprague-Dawley rats
  • Formulation: 20% DMSO in saline
  • Dosages: 5 mg/kg BW
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (199.05 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 386.83
Formula

C19H18N4O3·HCl

CAS No. 853220-52-7(free-base)
Storage powder
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID