GW6471

GW6471 是 PPARα 的拮抗剂,IC50 为 0.24 μM。它增强 PPAR α 配体结合结构域与共抑制蛋白 SMRT 和 NCoR 的结合亲和力。

CAS号

880635-03-0

分子式

C35H36F3N3O4

主要靶点

PPAR

仅限科研使用

Cat No : CM06124

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Synonyms

GW 6471



产品信息

GW6471 is an antagonist of PPARα with IC50 of 0.24 μ M. GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.

CAS号 880635-03-0
分子式 C35H36F3N3O4
主要靶点 PPAR
主要通路 DNA损伤和修复|代谢
分子量 619.67
纯度 98.38%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GW 6471

体外活性

A specific PPARα antagonist, GW6471, induced both apoptosis and cell cycle arrest at G0/G1 in VHL(+) and VHL(-) RCC cell lines (786-O and Caki-1) associated with attenuation of the cell cycle regulatory proteins c-Myc, Cyclin D1, and CDK4;?this data was confirmed as specific to PPARα antagonism by siRNA methods.

溶解度

DMSO:120 mg/mL (193.65 mM),Sonification is recommended.

参考文献

1.Abu Aboud O, et al. Inhibition of PPARα induces cell cycle arrest and apoptosis, and synergizes with glycolysisinhibition in kidney cancer cells. PLoS One. 2013 Aug 7;8(8):e71115.
2.Xu HE, et al. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha. Nature. 2002 Feb 14;415(6873):813-7.
3.Abu Aboud O, et al. PPARα inhibition modulates multiple reprogrammed metabolic pathways in kidney cancer and attenuates tumor growth. Am J Physiol Cell Physiol. 2015 Jun 1;308(11):C890-8.

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