T0070907

Catalog No.S2871

T0070907 Chemical Structure

Molecular Weight(MW): 277.66

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.

Size Price Stock Quantity  
In DMSO USD 60 In stock
USD 50 In stock
USD 70 In stock
USD 170 In stock
USD 270 In stock
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1 Customer Review

  • PPARγ mRNA expression and activated PPARγ in nuclear extraction in monocytes after treatment with 10 μM atorvastatin for 24 h in the presence or absence of T0070907 (10 nM) or rosiglitazone (100 nM).§P<0.05 for atorvastatin versus vehicle. *P<0.05 for atorvastatin plus the indicated chemicals versus atorvastatin.

    Int Immunopharmacol, 2015, 26(1): 58-64. T0070907 purchased from Selleck.

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Biological Activity

Description 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.
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
african green monkey OR6 cells MXXDfZRwfG:6aXRCpIF{e2G7 MlPyR5l1d3SxeHnjbZR6KGGpYXnud5Qh[W[{aXPhckBoemWnbjDtc45s\XliT2K2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCZU2SxJIF{e2G7LDDDR|UxRTJwNzFOwG0> NHLrW2UzOzh7MUG4Ny=>

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • Cell lines: MCF-7 cells
  • Concentrations: 20 μM and higher concentrations
  • Incubation Time: 48 h
  • Method: MTS assay
    (Only for Reference)
Animal Research:[3]
+ Expand
  • 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.
  • Formulation: 10% v/v dimethylsulfoxide [DMSO], 20–25% v/v DMSO, or saline
  • Dosages: 1 mg/kg
  • Administration: intraperitoneally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 26 mg/mL (93.63 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+45% PEG 300+ddH2O
9mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 277.66
Formula

C12H8ClN3O3

CAS No. 313516-66-4
Storage powder
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID