A small molecule that blocks phosphorylation of PPARγ by Cdk5 (IC50 = 80 nM; Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor; demonstrates potent

SR 1664 – 1 mg

Brand:
Cayman
CAS:
1338259-05-4
Storage:
-20
UN-No:
Non-Hazardous - /

Apart from direct peroxisome proliferator-activated receptor γ (PPARγ) agonism, several PPARγ ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) at serine 273.{25001} This effect requires binding to the PPARγ ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor.{25002} It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.{25002}  

 

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Description

A small molecule that blocks phosphorylation of PPARγ by Cdk5 (IC50 = 80 nM; Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor; demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation

Formal name: 4′-[[2,3-dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-[1,1′-biphenyl]-2-carboxylic acid

Synonyms: 

Molecular weight: 547.6

CAS: 1338259-05-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cell Biology|Cell Signaling||Research Area|Endocrinology & Metabolism|Hormones & Receptors|PPARs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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