BML-284 (Wnt agonist 1)

Catalog No.S8178 Batch:S817801

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Technical Data

Formula

C19H18N4O3·HCl
Molecular Weight 386.83 CAS No. 2095432-75-8
Solubility (25°C)* In vitro DMSO 77 mg/mL (199.05 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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 Assay:

[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 Study:

[3]
  • Animal Models

    Male adult Sprague-Dawley rats

  • Dosages

    5 mg/kg BW

  • Administration

    i.v.

Customer Product Validation

Data from [Data independently produced by , , Int J Oncol, 2017, 51(4):1077-1088]

Selleck's BML-284 (Wnt agonist 1) has been cited by 32 publications

MEN1 Deficiency-Driven Activation of the β-Catenin-MGMT Axis Promotes Pancreatic Neuroendocrine Tumor Growth and Confers Temozolomide Resistance [ Adv Sci (Weinh), 2024, 11(35):e2308417] PubMed: 39041891
Colchicine Blocks Abdominal Aortic Aneurysm Development by Maintaining Vascular Smooth Muscle Cell Homeostasis [ Int J Biol Sci, 2024, 20(6):2092-2110] PubMed: 38617538
β-catenin inhibition disrupts the homeostasis of osteogenic/adipogenic differentiation leading to the development of glucocorticoid-induced osteonecrosis of the femoral head [ Elife, 2024, 12RP92469] PubMed: 38376133
IL-33 regulates adipogenesis via Wnt/β-catenin/PPAR-γ signaling pathway in preadipocytes [ J Transl Med, 2024, 22(1):363] PubMed: 38632591
Exosome-based bone-targeting drug delivery alleviates impaired osteoblastic bone formation and bone loss in inflammatory bowel diseases [ Cell Rep Med, 2023, 4(1):100881] PubMed: 36603578
Restoring Wnt signaling in a hormone-simulated postpartum depression model remediated imbalanced neurotransmission and depressive-like behaviors [ Mol Med, 2023, 29(1):101] PubMed: 37491227
Restoring Wnt signaling in a hormone-simulated postpartum depression model remediated imbalanced neurotransmission and depressive-like behaviors [ Mol Med, 2023, 29(1):101] PubMed: 37491227
Identification and Expression Analysis of Wnt2 Gene in the Sex Differentiation of the Chinese Soft-Shelled Turtle (Pelodiscus sinensis) [ Life (Basel), 2023, 13(1)188] PubMed: 36676139
Identification and Expression Analysis of Wnt2 Gene in the Sex Differentiation of the Chinese Soft-Shelled Turtle (Pelodiscus sinensis) [ Life (Basel), 2023, 13(1)188] PubMed: 36676139
Empagliflozin activates Wnt/β-catenin to stimulate FUNDC1-dependent mitochondrial quality surveillance against type-3 cardiorenal syndrome [ Mol Metab, 2022, 64:101553] PubMed: 35863636

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.