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T0070907

Name: T0070907
Brand: Selleck Chemicals
SKU: S2871
Rating: 5 (66 reviews)

Catalog No.S2871

For research use only.

T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.

CAS No. 313516-66-4

Selleck's T0070907 has been cited by 66 publications

Purity & Quality Control

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PPAR Signaling Pathway Map

Biological Activity

Description

Targets

PPARγ ^[1]
(Cell-free assay)

1 nM

In vitro

T0070907 is a potent and selective PPARγ antagonist. With an apparent binding affinity (concentration at 50% inhibition of [³H] rosiglitazone binding or IC50) of 1 nM, T0070907 covalently modifies PPARγ on cysteine 313 in helix 3 of human PPARγ2. T0070907 blocks PPARγ function in both cell-based reporter gene and adipocyte differentiation assays. Consistent with its role as an antagonist of PPARγ, T0070907 blocks agonist-induced recruitment of coactivator-derived peptides to PPARγ in a homogeneous time-resolved fluorescence-based assay and promotes recruitment of the transcriptional corepressor NCoR to PPARγ in both glutathione S-transferase pull-down assays and a PPARγ/retinoid X receptor (RXR) α-dependent gel shift assay. Studies with mutant receptors suggest that T0070907 modulates the interaction of PPARγ with these cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain. Interestingly, whereas the T0070907-induced NCoR recruitment to PPARγ/RXRα heterodimer can be almost completely reversed by the simultaneous treatment with RXRα agonist LGD1069, T0070907 treatment has only modest effects on LGD1069-induced coactivator recruitment to the PPARγ/RXRα heterodimer. ^[1] T0070907 treatment inhibits proliferation, invasion and migration but does not significantly affect apoptosis. Molecular inhibition using a dominant negative (Δ462) receptor yields similar results. T007 also mediates a dose-dependent decrease in phosphorylation of PPARγ, and its ability to bind to DNA, and may directly affect mitogen-activated protein kinase signaling. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

OR6	MU\DfZRwfG:6aXPpeJkh[XO\|YYm=		NYnUO3dRPzJiaILz		MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBi\nKrY3HuJIdz\WWwIH3vcotmgSCRUk[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFeVVEGgZZN{[XluIFPDOVA:Oi55zszNMi=>	NELKbYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i5NVE5Oyd-MkO4PVEyQDN:L3G+
OR6	MYTBcpRqfmm{YXygZZN{[Xl?		NWKxTIE4PzJiaILz		NVSwSJc1SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHnu[oVkfGWmIHnuJIFnemmlYX6g[5Jm\W5ibX;ub4V6KE:UNjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJHJPSSC{ZYDsbYNifGmxbjDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG\|ZTDy[ZBwenSncjDn[Y5mKGG\|c3H5MEBGTDVyPUSuPe69VS5?	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh7MUG4N{c,OjN6OUGxPFM9N2F-

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In vivo

Lipopolysaccharide preconditioning significantly attenuates the development of renal dysfunction, hepatocellular injury, and circulatory failure as well as the increase in the plasma levels of interleukin-1 [beta] caused by severe endotoxemia. T0070907 can attenuate all of these beneficial effects afforded by preconditioning with lipopolysaccharide ^[3]

Protocol (from reference)

Kinase Assay:^[1]	Ligand Binding Assay: To determine the binding affinity of T0070907 to the PPARs, scintillation proximity assay (SPA) is performed with the following modifications. A 90-μl reaction contains SPA buffer (10 mm KH₂PO₄, 10 mm KH₂PO₄, 2 mm EDTA, 50 mm NaCl, 1 mm dithiothreitol, 2 mmCHAPS, 10% (v/v) glycerol, pH 7.1), 50 ng of GST-PPARγ (or 150 ng of GST-PPARα, GST-PPARδ), 5 nm ³H-labeled radioligands, and 5 μl of T0070907 in Me₂SO. After incubation for 1 h at room temperature, 10 μl of polylysine-coated SPA beads (at 20 mg/ml in SPA buffer) are added, and the mixtureis incubated for 1 h before reading in Packard Topcount. [³H]Rosiglitazone is used for PPARγ, and [³H]GW2433 is used for PPARα and PPARδ.
Cell Research:^[2]	Cell lines: MCF-7 cells Concentrations: 20 μM and higher concentrations Incubation Time: 48 h Method: MTS assay
Animal Research:^[3]	Animal Models: Preconditioning is performed by administering a low dose (1 mg/kg) of Escherichia coli LPS (serotype 0.127:B8) intraperitoneally 24 hr before the induction of severe endotoxemia. Dosages: 1 mg/kg Administration: intraperitoneally

References

Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 5% DMSO+45% PEG 300+ddH2O For best results, use promptly after mixing. Click to purchase: PEG300	9mg/mL

Chemical Information

Molecular Weight	277.66
Formula	C₁₂H₈ClN₃O₃
CAS No.	313516-66-4
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1=CC(=C(C=C1[N+](=O)[O-])C(=O)NC2=CC=NC=C2)Cl

Download T0070907 SDF

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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