BML-284 (Wnt agonist 1)

製品コードS8178 バッチS817801

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 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].

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, 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.
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.

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：

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
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
Empagliflozin activates Wnt/β-catenin to stimulate FUNDC1-dependent mitochondrial quality surveillance against type-3 cardiorenal syndrome [ Mol Metab, 2022, 64:101553] PubMed: 35863636
Endothelial Shp2 deficiency controls alternative activation of macrophage preventing radiation-induced lung injury through notch signaling [ iScience, 2022, 25(3):103867] PubMed: 35243230
Zuogui Wan slowed senescence of bone marrow mesenchymal stem cells by suppressing Wnt/β-catenin signaling [ J Ethnopharmacol, 2022, 294:115323] PubMed: 35483559
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
ARL4C Regulates the Progression of Clear Cell Renal Cell Carcinoma by Affecting the Wnt/β-Catenin Signaling Pathway [ J Oncol, 2022, 2022:2724515] PubMed: 35774359

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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