BML-284 Hydrochloride (Wnt agonist 1, AMBMP)

製品コードS8178 バッチS817803

印刷

化学情報

Chemical Structure Synonyms AMBMP Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H18N4O3·HCl
分子量 386.83 CAS No. 2095432-75-8
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
in vitro BML-284 (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. Exposure of human brain endothelial hCMEC/D3 cells to this compound 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).
in vivo BML-284 (Wnt agonist 1) mimics the effects of Wnt at the whole-organism level in a Xenopus model (10 μM), and affects Xenopus embryonic head specification. In animal model (Rat renal IR model), this compound significantly lowered serum levels of creatinine, AST, and LDH, inhibited the production of IL-6 and IL-1β, and MPO activities. It reduced iNOS, nitrotyrosine proteins and 4-hydroxynonenal in the kidneys, improving renal regeneration and function while attenuating inflammation and oxidative stress in the kidneys after IR.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 293T cells
濃度 10 μM
反応時間 24 h
実験の流れ

For high-throughput screening of BML-284 (Wnt agonist 1), 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, this compound solution (1 mM, 500 nL) is added to each well. After incubation for another 24 h, luciferase activity is measured with BrightGlo.
動物実験 動物モデル Male adult Sprague-Dawley rats
投薬量 5 mg/kg BW
投与方法 i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15724259/
  • https://pubmed.ncbi.nlm.nih.gov/18624906/
  • https://pubmed.ncbi.nlm.nih.gov/25514428/

カスタマーフィードバック

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

NRF2 modulates WNT signaling pathway to enhance photodynamic therapy resistance in oral leukoplakia [ EMBO Mol Med, 2025, 17(7):1794-1824] PubMed: 40494896
Stress induces behavioral disorders by promoting microglial phagocytosis via decreasing neuronal Dkk3 [ Mol Psychiatry, 2025, 30(12):5731-5748] PubMed: 41136744
Huaier promotes sensitivity of colorectal cancer to oxaliplatin by inhibiting METTL3 to regulate the Wnt/β‑catenin signaling pathway [ Oncol Rep, 2025, 53(1)7] PubMed: 39513580
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
Radiation-induced morphea of the breast - characterization and treatment of fibroblast dysfunction with repurposed mesalazine [ Sci Rep, 2024, 14(1):26132] PubMed: 39477958
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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