BML-284

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Chemical Structure| 853220-52-7 同义名 : Wnt Agonist I
CAS号 : 853220-52-7
货号 : A149492
分子式 : C19H18N4O3
纯度 : 99%+
分子量 : 350.371
MDL号 : MFCD09908087
存储条件:

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(299.68 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 The Wnt signaling pathway plays an important role in a variety of physiological and pathological processes by regulating genes involved in cellular adhesion, proliferation, and differentiation. Many of the key components of the signaling pathway have been elucidated. The Wnt ligand activates downstream signal transduction through interaction with its receptor, Frizzled[3]. BML-284 induces β‐catenin‐ and TCF‐dependent transcriptional activity in a dose‐dependent manner with an EC50 value of 0.7 μM[3]. β‐catenin‐ and TCF‐dependent reporter gene expression induced by BML-284 was blocked in the presence of the dominant negative TCF4, thus suggesting that the active compound functions in the canonical Wnt pathway through the TCFs. In a Xenopus model, embryos treated with BML-284 (n=36) had substantial head defects that ranged from significantly diminished heads and complete loss of eyes, to reduced eyes and heads; the posterior structures of tadpoles remained largely intact. These results suggest that the small‐molecule Wnt agonist indeed mimics the effects of Wnt at the whole‐organism level[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.54mL

5.71mL

2.85mL

参考文献

[1]Wang H, Graves MW 2nd, et al. 2-Amino-4-(3,4-(methylenedioxy)benzylamino)-6-(3-methoxyphenyl)pyrimidine is an anti-inflammatory TLR-2, -4 and -5 response mediator in human monocytes. Inflamm Res. 2016 Jan;65(1):61-9.

[2]Liu J, Wu X, et al. A small-molecule agonist of the Wnt signaling pathway. Angew Chem Int Ed Engl. 2005 Mar 18;44(13):1987-90.

[3]Liu J, Wu X, Mitchell B, Kintner C, Ding S, Schultz PG. A small-molecule agonist of the Wnt signaling pathway. Angew Chem Int Ed Engl. 2005 Mar 18;44(13):1987-90. doi: 10.1002/anie.200462552. PMID: 15724259.