T0070907 313516-66-4

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Molecular Weight:

277.66 T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM, with a >800-fold selectivity over PPARα and PPARδ.






Biological Activity


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.


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.


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

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Product Categories : Metabolism > PPAR Inhibitor