DY131

DY131(GSK 9089) is a novel selective agonist of ERRβ and ERRγ; displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.IC50 value:Target: ERRβ/γDY131, a selective ERRγ agonist, could potentiate the ERRγ-induced growth inhibition in LNCaP- ERRγ and DU145- ERRγ cells in a dose-dependent manner compared with respective parental cells. DY131 inhibited the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells. DY131 had no effect on the structurally related receptors ERRα or the estrogen receptors alpha and beta (ERalpha/beta). DY131 appears to inhibit Smo signaling through a common binding site shared by previously reported Smo agonists and antagonists.

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

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