An inhibitor of SGK1 and SGK2
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SGK1 Inhibitor

Item No. 25652

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
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
Synonyms
  • GS-9007
  • SGK1i
  • SGK1-inh
Molecular Formula
C17H12Cl2N6O2S
Formula Weight
435.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
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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    1 mg

    $41

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    5 mg

    $186

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    10 mg

    $351

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    25 mg

    $775

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    Product Description

    SGK1 inhibitor is an ATP-competitive inhibitor of serum/glucocorticoid-regulated kinase 1 (SGK1) and SGK2 (IC50s = 0.442 and 0.924 µM, respectively).1 It is selective for SGK1 and SGK2 over SGK3 (IC50 = 23.3 μM) and a panel of 60 additional kinases at 1 μM but does inhibit AMP-activated protein kinase (AMPK) by greater than 50% at 1 µM.2 SGK1 inhibitor (5 µM) reduces ERK phosphorylation and inhibits colony formation in AML12 hepatocytes expressing DNAJ-PKAc, a fusion protein found in fibrolamellar carcinoma tumors.3 It also reduces phosphorylation of glycogen synthase kinase 3β (GSK3β) in U2OS cells (IC50 = 1.4 μM) and sensitizes HCC1954 hepatocellular carcinoma cells to the PI3Kα inhibitor BYL719 (Item No. 16986).2,1 SGK1 inhibitor (50 mg/kg) enhances the reduction in tumor growth induced by BYL719 in an HCC1954 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Castel, O., Ellis, H., Bago, R., et al. PDK1-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 al. Discovery 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).

    3. Lee, G., and Muir, T.W. Distinct phases of cellular signaling revealed by time-resolved protein synthesis. bioRxiv [Preprint] (2024).