BML-284 (Wnt agonist 1)

製品コードS8178 バッチS817804

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.000mg/ml (2.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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^[1]. 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)^[2].
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^[1]. 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, improves renal regeneration and function while attenuating inflammation and oxidative stress in the kidneys after IR^[3].

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 with 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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