An inhibitor of SGK1 and SGK2
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SGK1 Inhibitor

Item No. 25652

Technical Information
Formal Name
N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2,3-dichloro-benzenesulfonamide
CAS Number
1426214-51-8
Molecular Formula
C17H12Cl2N6O2S
Formula Weight
Purity
≥95%
A solid
SMILES
ClC1=CC=CC(S(NC2=CC=C(C3=CN=C(C(N)=NN4)C4=N3)C=C2)(=O)=O)=C1Cl
InChi Code
InChI=1S/C17H12Cl2N6O2S/c18-11-2-1-3-13(14(11)19)28(26,27)25-10-6-4-9(5-7-10)12-8-21-15-16(20)23-24-17(15)22-12/h1-8,25H,(H3,20,22,23,24)
InChi Key
MBNNXCKHRKSGSU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2 (IC50s = 4.8 and 2.8 nM, respectively).1 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.2 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).1 SGK1 inhibitor (50 mg/kg) reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Castel, O., Ellis, H., Bago, R., et alPDK1-SGK1 signaling sustains AKT-independent mTORC1 activation and confers resistance to PI3Kα inhibition. Cancer Cell 30(2), 229-242 (2016).

    2. Halland, N., Schmidt, F., Weiss, T., et alDiscovery of N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as highly active and selective SGK1 inhibitors. ACS Med. Chem. Lett. 6(1), 73-78 (2014).