An inhibitor of SGK1 and SGK2 (IC50s = 4.8 and 2.8 nM

SGK1 Inhibitor – 5 mg

Brand:
Cayman
CAS:
1426214-51-8
Storage:
-20
UN-No:
Non-Hazardous - /

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2 (IC50s = 4.8 and 2.8 nM, respectively).{43799} It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP (IC50s = 0.442, 0.924, and 23.3 μM, respectively) and only inhibits AMPK by more than 50% in a panel of 60 additional kinases when used at a concentration of 1 μM.{43800} SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells with an IC50 value of 1.4 μM. It decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719 (Item No. 16986).{43799} SGK1 inhibitor (50 mg/kg) reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.  

 

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Description

An inhibitor of SGK1 and SGK2 (IC50s = 4.8 and 2.8 nM, respectively); selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP (IC50s = 0.442, 0.924, and 23.3 μM, respectively); only inhibits AMPK by more than 50% in a panel of 60 additional kinases at 1 μM; prevents phosphorylation of GSK3β in U2OS cells (IC50 = 1.4 μM); decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with BYL719; reduces tumor growth in an HCC1954 mouse xenograft model when administered at 50 mg/kg in combination with BYL719

Formal name: N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2,3-dichloro-benzenesulfonamide

Synonyms: 

Molecular weight: 435.3

CAS: 1426214-51-8

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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