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T0070907

现货
Catalog No.
A4301
有效的人类PPARγ选择性拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
10mg
¥ 500.00
现货
25mg
¥ 1,200.00
现货
50mg
¥ 1,900.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt277.66
Cas No.313516-66-4
FormulaC12H8ClN3O3
Solubility≥27.8 mg/mL in DMSO, ≥4.77 mg/mL in EtOH with ultrasonic and warming, <2.29 mg/mL in H2O
Chemical Name2-chloro-5-nitro-N-pyridin-4-ylbenzamide
SDFDownload SDF
Canonical SMILESC1=CC(=C(C=C1[N+](=O)[O-])C(=O)NC2=CC=NC=C2)Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HeLa, SiHa和Me180细胞系

溶解方法

在DMSO中的溶解度> 13.9 mg/ml。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

50 μM

应用

用PPARγ抑制剂T0070907和/或辐射治疗三种宫颈癌细胞系(HeLa,SiHa和Me180)。 T0070907在ME180细胞中以时间依赖的方式显著降低微管蛋白水平。 经T0070907处理后ME180和SiHa细胞的微管蛋白水平的降低与G2 / M期细胞显著增加有关,但是微管蛋白和G2 / M期的变化在HeLa细胞中不明显。 T0070907也可以降低PPARγ的蛋白水平, 然而,PPARγ抑制对ME180细胞中的α-微管蛋白水平没有影响,表明T0070907同时具有PPARγ依赖和非依赖作用。

References:

[1] An Z, et al. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61.

生物活性

Description T0070907是一种有效的人类PPARγ选择性拮抗剂,IC50值为1 nM。
靶点 human PPARγ          
IC50 1 nM          

质量控制