MRL20 is a PPARγ constitutive and allosteric agonist that enhances the interaction between PPARγ and the co-activating peptide TRAP220, exhibiting an EC50 of 10 nM. Notably, even when covalently inhibited in its constitutive pocket by GW9662 or T0070907, MRL20 can maintain its ability to facilitate the PPARγ-TRAP220 interaction, with subsequent EC50 values of 176 nM and 440 nM, respectively. This compound does not completely inhibit cell activation, making MRL20 a valuable tool for investigating the allosteric regulatory mechanisms of PPARγ in various biological contexts.
MRL20 is a PPARγ constitutive and allosteric agonist that enhances the interaction between PPARγ and the co-activating peptide TRAP220, exhibiting an EC50 of 10 nM. Notably, even when covalently inhibited in its constitutive pocket by GW9662 or T0070907, MRL20 can maintain its ability to facilitate the PPARγ-TRAP220 interaction, with subsequent EC50 values of 176 nM and 440 nM, respectively. This compound does not completely inhibit cell activation, making MRL20 a valuable tool for investigating the allosteric regulatory mechanisms of PPARγ in various biological contexts.
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