T0070907

説明

The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARγ receptor agonists with antidiabetic actions in vivo. There are many PPARγ agonists, including 15-deoxy-Δ^12,14-prostaglandin J₂ and azelaoyl PAF, which are naturally derived. However, only a few antagonists have been reported. T0070907 is a potent and selective antagonist of the human PPARγ with an apparent IC₅₀ of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys³¹³ of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.

化学的特性

Off-White Solid

使用

T0070907 has been used to reduce peroxisome proliferator-activated receptor gamma (PPAR-γ) expression in lipopolysaccharide (LPS)-induced leukemia RAW264.7 cell line. It also has been used to evaluate the involvement of wogonin in alleviating EtOH (ethanol)-induced inflammation in RAW264.7 cell line.

一般的な説明

T0070907 has antimicrotubule, antitumor and radiosensitizing properties. It decreases tubulin protein levels, which is associated with cell cycle arrest, apoptosis and also reduces metastasis of colorectal carcinoma cells. T0070907 is used as a therapeutic target in breast cancer. It stimulates proteasome-dependent degradation of tubulin.

生物活性

Potent and selective PPAR γ antagonist (IC 50 = 1 nM). Displays > 800-fold selectivity for PPAR γ over PPAR α and PPAR δ . In vitro, blocks transcriptional activity of PPAR γ and inhibits rosiglitazone-induced adipogenesis.