1. Metabolic Enzyme/Protease
    Anti-infection
  2. SGK
    Influenza Virus
  3. GSK 650394

GSK 650394 

Cat. No.: HY-15192 Purity: 99.76%
Handling Instructions

GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.

For research use only. We do not sell to patients.

GSK 650394 Chemical Structure

GSK 650394 Chemical Structure

CAS No. : 890842-28-1

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 479 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

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Description

GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.

IC50 & Target

IC50: 62 nM (SGK1), 103 nM (SGK2)

In Vitro

GSK650394 is relatively non-toxic, with LC50 values of 41 μM in M1 cells (68 times its activity IC50) and a LC50 greater than 100 μM in HeLa cells. GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. GSK650394 inhibits the growth of LNCaP cells with IC50 of approximately 1 μM[1]. GSK650394A inhibits the insulin-induced phosphorylation of PKB-Ser473 at 3 µM, and essentially abolishes this response at 10 µM. GSK650394A (1-10 µM) does not alter the phosphorylation of PRAS40-Ser246 in hormone-deprived cells or prevent the insulin-induced phosphorylation of this residue[2].

In Vivo

GSK650394 (1, 10, and 30 μM, 10 μL/rat, intrathecally) dose-dependently prevents CFA-induced pain behavior and the associates SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration[3]. GSK650394 at concentrations of 10, 30, and 100 nM (10 μL), but not vehicle solution (SNL 3D+Veh and SNL 7D+Veh, respectively), dose-dependently increases the withdrawal latency of the ipsilateral hindpaw at 1-3 and 1-5 h after injection at days 3 and 7 postsurgery (SNL 3D+GSK and SNL 7D+GSK, respectively). GSK650394 (from day 0 to 6 postsurgery; 100 nM, 10 μL, i.t.) administration alleviates SNL-induced allodynia at days 3, 5, and 7 postsurgery in SNL animals[4].

Molecular Weight

382.45

Formula

C₂₅H₂₂N₂O₂

CAS No.

890842-28-1

SMILES

O=C(O)C(C=C1)=C(C2CCCC2)C=C1C3=CNC(C3=C4)=NC=C4C5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40.7 mg/mL (106.42 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6147 mL 13.0736 mL 26.1472 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 mL
10 mM 0.2615 mL 1.3074 mL 2.6147 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.54 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.54 mM); Suspended solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

The toxicity of GSK650394 to M-1 and HeLa cells is assessed using the Cell Proliferation Kit (XTT) following manufacturer’s instructions. Briefly, 10,000 HeLa or M-1 cells/well are plated into 96-well plates in 100μL of the appropriate maintenance media. After 48 h, media is removed and replaced with 100 μL of EMEM with Earle’s salts containing 2 mM L-glutamine and 1% antibiotic-antimycotic overnight. M-1 cells are also supplemented with 1 μg/mL insulin, 6.25 μg/mL sodium selenite, and 6.25 μg/mL transferrin. After 24 h, the media is removed and replaced with 100 μL media alone or media containing increasing concentrations of GSK650394. For HeLa cells, 50 μL of activated XTT solution is added after 4 h. For M-1 cells, 50 μL of activated XTT solution is added after 24 h. Following a 2 h incubation, absorbance is measured at 490 nm using a SpectraMAX PLUS spectrophotometer and the data analyzed to obtain IC50 values using GraphPad Prism 3 software.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Briefly, the rats are anesthetized under isoflurane anesthesia (induction 5%, maintenance 2% in oxygen). An incision is made, and the left L5 spinal nerves are carefully isolated and tightly ligated with 6-0 silk sutures 2-5 mm distal to the dorsal root ganglia. GSK650394 (10, 30, and 100 nM, 10 μL) is administered by bolus injection at 3 or 7 d or by daily injection for 7 d (day 0-6) postspinal nerve ligation. A vehicle solution of a volume identical to that of the tested agents is dispensed to serve as a control.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.76%

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Keywords:

GSK 650394GSK650394GSK-650394SGKInfluenza VirusSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinaseInhibitorinhibitorinhibit

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GSK 650394
Cat. No.:
HY-15192
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