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T0070907
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
T0070907图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
25mg电议
50mg电议

产品介绍
T0070907 是一种有效的 PPARγ 拮抗剂,Ki 为 1 nM。

Cell lines

HeLa, SiHa, and Me180 cell lines

Preparation method

The solubility of this compound in DMSO is >13.9 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

50 μM

Applications

Three cervical cancer cell lines (HeLa, SiHa, and Me180) were treated with a PPARγ inhibitor, T0070907, and/or radiation. T0070907 has significantly decreased the tubulin levels in a time-dependent manner in ME180 cells. The decrease in the tubulin levels after T0070907 in ME180 and SiHa cells was associated with significant increase in the cells at the G2/M phase. The changes in the tubulin and G2/M phase were not evident in HeLa cells. T0070907 reduced the protein levels of PPARγ; however, PPARγ silencing had no effect on the α-tubulin level in ME180 cells suggesting the PPARγ-dependent and -independent actions of T0070907.

产品描述

T0070907 is a selective antagonist of peroxisome proliferator-activated receptor γ (PPARγ) with IC50 value of 1nM [1].

T0070907 shows high affinity to PPARγ with Ki of 1nM. The Ki values of it to PPARα and PPARδ are 0.85 and 1.8μM, respectively, demonstrating the high selectivity of T0070907. It is found that T0070907 binds PPARγ within the cysteine 313 in helix 3 of human PPARγ2, subsequently blocks PPARγ function. In transient transfection assay, T0070907 inhibits the transactivation of PPARγ in the presence of rosiglitazone (a PPARγ agonist) with IC50 value in the nM range. T0070907 can block the induction of adipogenesis of the adipogenic cell line 3T3-L1. Additionally, T0070907 is found to suppress the interaction between PPARγ and the coactivator derived peptide, while promoting the recruitment of the NCoR-derived peptide to PPARγ. Furthermore, T0070907 can also promote a significant increase in the recruitment of NCoR to the PPARγ/RXRα heterodimer [1].

References:
[1] Lee G, Elwood F, McNally J, Weiszmann J, Lindstrom M, Amaral K, Nakamura M, Miao S, Cao P, Learned RM, Chen JL, Li Y. 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.