An inhibitor of dihydroceramide desaturase (IC50 = 2.32 µM); promotes the generation of ROS

Fenretinide – 25 mg

Brand:
Cayman
CAS:
65646-68-6
Storage:
-20
UN-No:
Non-Hazardous - /

Fenretinide is a synthetic derivative of retinoic acid (Item No. 11017) and an inhibitor of dihydroceramide desaturase (IC50 = 2.32 µM).{39681} It promotes the generation of reactive oxygen species (ROS), the degradation of anti-apoptotic MCL-1, and the cleavage of pro-apoptotic PKCδ.{22943} At 5-20 µM, fenretinide selectively activates retinoic acid receptor γ (RARγ) and is reported to inhibit the growth of Caov-3, OVCAR-3, and SKOV3 ovarian cancer cells with IC50 values of 3.7, 6.9, and 8.2 µM, respectively.{24737,17895} It also increases activity of serine palmitoyl transferase (SPT) by 1.75-fold and induces caspase-dependent apoptosis in BMEC cells (IC50 = 2.4 µM).{12547} Fenretinide prevents lipid-induced reductions in insulin-stimulated glucose uptake in isolated rat soleus muscle.{39682} In vivo, fenretinide (10 mg/ml in drinking water) reduces liver and soleus muscle neutral lipid content and inhibits high-fat diet-induced increases in dihydroceramide desaturase transcription.{39682}  

 

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Description

An inhibitor of dihydroceramide desaturase (IC50 = 2.32 µM); promotes the generation of ROS, degradation of MCL-1, and cleavage of PKCδ; selectively activates RARγ at 5-20 µM; inhibits the growth of Caov-3, OVCAR-3, and SKOV3 ovarian cancer cells (IC50s = 3.7, 6.9, and 8.2 µM, respectively); increases activity of SPT by 1.75-fold and induces caspase-dependent apoptosis in BMEC cells (IC50 = 2.4 µM); prevents lipid-induced reductions in insulin-stimulated glucose uptake in isolated rat soleus muscle; reduces liver and soleus muscle neutral lipid content and inhibits high-fat diet-induced increases in dihydroceramide desaturase transcription at 10 mg/ml,,

Formal name: N-(4-hydroxyphenyl)-retinamide

Synonyms:  4-HPR|4-Hydroxy(phenyl)retinamide|MK-4016|Retinoic Acid p-hydroxyphenylamide|Ro 22-4667

Molecular weight: 391.6

CAS: 65646-68-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Small Molecule Activators||Product Type|Biochemicals|Small Molecule Inhibitors|Fatty Acid Metabolism||Product Type|Biochemicals|Small Molecule Inhibitors|Sphingolipid Turnover||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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