BML-284 (Wnt agonist 1)

Synonyms: AMBMP

BML-284 (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.

BML-284 (Wnt agonist 1) Chemical Structure

BML-284 (Wnt agonist 1) Chemical Structure

CAS: 2095432-75-8

Selleck's BML-284 (Wnt agonist 1) has been cited by 27 Publications

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Purity & Quality Control

Batch: Purity: 99.91%
99.91

BML-284 (Wnt agonist 1) Related Products

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Biological Activity

Description BML-284 (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
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].
Cell Research 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.

In Vivo
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].
Animal Research Animal Models Male adult Sprague-Dawley rats
Dosages 5 mg/kg BW
Administration i.v.

Chemical Information & Solubility

Molecular Weight 386.83 Formula

C19H18N4O3·HCl

CAS No. 2095432-75-8 SDF Download BML-284 (Wnt agonist 1) SDF
Smiles COC1=CC=CC(=C1)C2=CC(=NC(=N2)N)NCC3=CC4=C(C=C3)OCO4.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 77 mg/mL ( (199.05 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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.

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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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