Wnt agonist 1

Catalog No.S8178 Synonyms: BML-284 HCL, BML-284 hydrochloride, AMBMP hydrochloride, AMBMP HCL

For research use only.

Wnt agonist 1 (BML-284 HCL, AMBMP HCL) is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.

Wnt agonist 1 Chemical Structure

CAS No. 2095432-75-8

Selleck's Wnt agonist 1 has been cited by 21 publications

Purity & Quality Control

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Biological Activity

Description Wnt agonist 1 (BML-284 HCL, AMBMP HCL) 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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[3]

  • Animal Models: Male adult Sprague-Dawley rats
  • Dosages: 5 mg/kg BW
  • Administration: i.v.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

9mg/mL

Chemical Information

Molecular Weight 386.83
Formula

C19H18N4O3·HCl

CAS No. 2095432-75-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=CC(=C1)C2=CC(=NC(=N2)N)NCC3=CC4=C(C=C3)OCO4.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What’s the formulation of S8178 for in vivo studies?

Answer:
The IP formula of S8178 is "2% DMSO+40% PEG 300+2% Tween 80+ddH2O", which can up to 9mg/ml.

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