MedKoo Cat#: 574246 | Name: SGK1 inhibitor
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719.

Chemical Structure

SGK1 inhibitor
SGK1 inhibitor
CAS#1426214-51-8

Theoretical Analysis

MedKoo Cat#: 574246

Name: SGK1 inhibitor

CAS#: 1426214-51-8

Chemical Formula: C17H12Cl2N6O2S

Exact Mass: 434.0119

Molecular Weight: 435.28

Elemental Analysis: C, 46.91; H, 2.78; Cl, 16.29; N, 19.31; O, 7.35; S, 7.37

Price and Availability

Size Price Availability Quantity
1mg USD 250.00 2 Weeks
5mg USD 375.00 2 Weeks
10mg USD 760.00 2 Weeks
25mg USD 1,250.00 2 Weeks
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Related CAS #
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Synonym
SGK1 inhibitor
IUPAC/Chemical Name
N-[4-(3-amino-1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-2,3-dichloro-benzenesulfonamide
InChi Key
MBNNXCKHRKSGSU-UHFFFAOYSA-N
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)
SMILES Code
ClC1=CC=CC(S(NC2=CC=C(C3=CN=C(C(N)=NN4)C4=N3)C=C2)(=O)=O)=C1Cl
Appearance
Solid powder
Purity
>95% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
SGK1 inhibitor inhibits SGK1 and SGK2 (IC50s = 4.8 and 2.8 nM, respectively). 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. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells with an IC50 value of 1.4 μM.
In vitro activity:
To be determined
In vivo activity:
To be determined

Preparing Stock Solutions

The following data is based on the product molecular weight 435.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
To be determined
In vitro protocol:
To be determined
In vivo protocol:
To be determined
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).