EMD 638683 – 1 mg

Brand:
Cayman
CAS:
1181770-72-8
Storage:
-20
UN-No:
Non-Hazardous - /

EMD 638683 is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) that inhibits SGK1 by 85% when used at a concentration of 1 µM.{59340} It is greater than 27-fold selective for SGK1 over a panel of 11 kinases but does inhibit SGK2, SGK3, PRK2, and MSK1 by greater than 50% at 1 µM. EMD 638683 inhibits phosphorylation of the SGK1 target NDRG1 in HeLa cells (IC50 = 3.35 µM). It increases radiation-induced apoptosis of Caco-2 colon carcinoma cells when used at a concentration of 50 µM.{59341} Dietary administration of EMD 638683 (600 mg/kg) reduces the number of tumors in a mouse model of chemical carcinogenesis. It prevents fructose and saline consumption-induced increases in systolic blood pressure in mice.{59340} EMD 638683 decreases body weight, fasting blood glucose and hemoglobin A1c (HbA1C) levels, and food intake in db/db diabetic mice.{59342} It also reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice.{59343}  

 

Available on backorder

SKU: 31117 - 1 mg Category:

Description

An inhibitor of SGK1; inhibits SGK1 by 85% at 1 µM; >27-fold selective for SGK1 over a panel of 11 kinases, but does inhibit SGK2, SGK3, PRK2, and MSK1 by >50% at 1 µM; inhibits phosphorylation of the SGK1 target NDRG1 in HeLa cells (IC50 = 3.35 µM); increases radiation-induced apoptosis of Caco-2 colon carcinoma cells at 50 µM; dietary administration reduces the number of tumors in a mouse model of chemical carcinogenesis; prevents fructose and saline consumption-induced increases in systolic blood pressure in mice; decreases body weight, fasting blood glucose and HbA1c levels, and food intake in db/db diabetic mice; reduces angiotensin II-induced collagen deposition and cardiac fibrosis in mice


Formal name: 3,5-difluoro-α-hydroxy-benzeneacetic acid, 2-(2-ethyl-4-hydroxy-3-methylbenzoyl)hydrazide

Synonyms: 

Molecular weight: 364.3

CAS: 1181770-72-8

Purity: ≥98%

Formulation: A crystalline solid