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T0070907

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Chemical Structure| 313516-66-4 同义名 : -
CAS号 : 313516-66-4
货号 : A227971
分子式 : C12H8ClN3O3
纯度 : 98%
分子量 : 277.663
MDL号 : MFCD00121849
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(216.09 mM)，配合低频超声，并水浴加热至45℃助溶，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：

5% DMSO+45% PEG 300+water 9 mg/mL

生物活性
靶点

  • PPARγ

    PPARγ, IC50:1 nM
描述 T0070907 is a potent and selective PPARγ antagonist with Ki value of 1nM, with >800-fold preference for PPARγ over PPARα and PPARδ with Ki values of 0.85μM and 1.8 μM. T0070907 at concentration ranging in 1nM-1μM dose-dependently antagonized the effects of rosiglitazone at concentration 1μM in HTRF assays, blocking agonist-induced recruitment of coactivator-derived peptides to PPARγ. It promoted recruitment of the transcriptional corepressor NCoR to PPARγ/RXR heterodimer[1]. Treatment with 50μM T0070907 for 24h led loss of 70% cell adherence in trypsinized HepG2 cells, associated with reductions in phosphorylated FAK[2].
作用机制 T0070907 covalently modifies PPARγ on cysteine 313 in helix 3 of human PPARγ2. T0070907 modulates the interaction of PPARγ with cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
african green monkey OR6 cells Cytotoxic assay Cytotoxicity against african green monkey OR6 cells after 72 hrs by WST1 assay, CC50=2.7 μM 23891183
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.60mL

0.72mL

0.36mL

18.01mL

3.60mL

1.80mL

36.01mL

7.20mL

3.60mL
参考文献

[1]Lee G, Elwood F, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 2002 May 31;277(22):19649-57. Epub 2002 Mar 4.

[2]Schaefer KL, Wada K, et al. Peroxisome proliferator-activated receptor gamma inhibition prevents adhesion to the extracellular matrix and induces anoikis in hepatocellular carcinoma cells. Cancer Res. 2005 Mar 15;65(6):2251-9.