GSK 650394
Based on 27 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.76%
- CAS. Nr.: 890842-28-1
- Formel: C25H22N2O2
- Molecular Weight:382.45
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) GSK 650394
More- Mol Cell. 2025 Mar 19:S1097-2765(25)00186-8. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Genes Dis. 2025 Oct 3.
- MedComm. 2024 Apr 10;5(4):e540. [Abstract]
- Int J Biol Sci. 2023 Jan 1;19(1):204-224. [Abstract]
- Mol Psychiatry. 2025 Oct 1. [Abstract]
- J Transl Med. 2023 Aug 14;21(1):544. [Abstract]
- Chin Med J (Engl). 2025 Jul 22. [Abstract]
- Oncogene. 2021 Sep;40(35):5367-5378. [Abstract]
- Br J Pharmacol. 2026 Jun;183(11):2739-2760. [Abstract]
- Br J Pharmacol. 2020 Apr;177(7):1666-1676. [Abstract]
- CNS Neurosci Ther. 2026 Apr;32(4):e70860. [Abstract]
- Matrix Biol. 2025 Oct 17:S0945-053X(25)00104-0. [Abstract]
- Acta Physiol. 2026 Feb;242(2):e70163. [Abstract]
- Int Immunopharmacol. 2026 Mar 1:172:116207. [Abstract]
- Immunology. 2021 Aug;163(4):493-511. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2024 Jul;397(7):5207-5217. [Abstract]
- Viruses. 2024 Aug 16;16(8):1308. [Abstract]
- Arch Biochem Biophys. 2020 Jul 15;687:108375. [Abstract]
- Cancer Control. 2022 Jan-Dec:29:10732748221143881. [Abstract]
- JID Innov. 2026 Jan 19;6(2):100451. [Abstract]
- Biocell. 2025 Apr 18;49(5), 857-872.
- Rep Biochem Mol Biol. 2023 Apr;12(1):159-172. [Abstract]
- Acta Otolaryngol. 2022 Jan;142(1):6-12. [Abstract]
- Biomed Pharmacother. 2024 May:174:116447. [Abstract]
- Research Square Print. December 27th, 2022.
- Universidad de Granada. 2020 Sep.
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Biologische Aktivität
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SGK1 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 890842-28-1
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Appearance Solid
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Molecular Weight 382.45
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Formel C25H22N2O2
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Color Off-white to yellow
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SMILES
O=C(O)C(C=C1)=C(C2CCCC2)C=C1C3=CNC(C3=C4)=NC=C4C5=CC=CC=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (27)
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Journal Impact Factor
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Most Recent
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Mol Cell
PI3Kβ functions as a protein kinase to promote cellular protein O-GlcNAcylation and acetyl-CoA production for tumor growth. [Abstract]2025 Mar 19:S1097-2765(25)00186-8. PMID: 40132583
GSK 650394 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Mar 19:S1097-2765(25)00186-8. [Abstract]
U251 cells expressing OGT shRNA with reconstituted expression of WT FLAG-rOGT or FLAG-rOGT T985A mutant were pretreated with or without TGX-221 (10 μM), MK2206 (10 μM), GSK 650394 (10 μM), and rapamycin (0.4 μM) for 1 h before treatment with the indicated concentrations of glucose for 2 h. Immunoprecipitation analyses were performed with an anti-FLAG antibody.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
GSK 650394 purchased from MedChemExpress. Usage Cited in: Genes Dis. 2025 Oct 3.
Western blotting showed increased SGK1 levels following TSZ treatment, while the expression of SGK1, p-MLKL/MLKL, and p-RIP3/RIP3 decreased in HT22 cells after pretreatment with SGK1 siRNA and inhibitor GSK 650394 (15 μM; 30 min) before TSZ application.
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MedComm
2024 Apr 10;5(4):e540. PMID: 38606360
GSK 650394 purchased from MedChemExpress. Usage Cited in: MedComm. 2024 Apr 10;5(4):e540. [Abstract]
GSK 650394 (5 μM, 48 h) treated AD model N2a-APP cells, and the ratio of p‐FOXO3a to total FOXO3a decreased significantly relative to the DMSO vehicle control group, suggesting that APP metabolism was likely altered.
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Int J Biol Sci
TGFβ Governs the Pleiotropic Activity of NDRG1 in Triple-Negative Breast Cancer Progression. [Abstract]2023 Jan 1;19(1):204-224. PMID: 36594086 -
Mol Psychiatry
Hippocampal SGK1 promotes vulnerability to depression: the role of early life adversity, stress, and genetic risk. [Abstract]2025 Oct 1. PMID: 41034507
GSK 650394 purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2025 Oct 1. [Abstract]
GSK 650394 (5 mg/kg; i.p.; once daily for 10 days; mice) prevented a Chronic Social Defeat Stress (CSDS)-induced reduction in mobility during the last 4 min of the Forced Swim Test (FST).
GSK 650394 purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2025 Oct 1. [Abstract]
Systemic injections of GSK 650394 (5 mg/kg; i.p.; once daily for 10 days; mice) result in detectable drug concentrations in the hippocampus, confirming that the compound indeed crosses the blood-brain barrier.
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J Transl Med
TNFSF14/LIGHT promotes cardiac fibrosis and atrial fibrillation vulnerability via PI3Kγ/SGK1 pathway-dependent M2 macrophage polarisation. [Abstract]2023 Aug 14;21(1):544. PMID: 37580750 -
Chin Med J (Engl)
2025 Jul 22. PMID: 40693638 -
Oncogene
Dexamethasone enhances the lung metastasis of breast cancer via a PI3K-SGK1-CTGF pathway. [Abstract]2021 Sep;40(35):5367-5378. PMID: 34272474 -
Br J Pharmacol
Down-regulation of M6A demethylase ALKBH5 facilitates morphine tolerance via SGK1 in mice. [Abstract]2026 Jun;183(11):2739-2760. PMID: 41666459 -
Br J Pharmacol
PO-322 exerts potent immunosuppressive effects in vitro and in vivo by selectively inhibiting SGK1 activity. [Abstract]2020 Apr;177(7):1666-1676. PMID: 31724152 -
CNS Neurosci Ther
RFWD2 Mitigates AD-Like Cognitive Impairments via the JNK-SGK1 Signaling Pathway in Mice. [Abstract]2026 Apr;32(4):e70860. PMID: 41954517 -
Matrix Biol
Phosphorylation of UDP-glucose dehydrogenase increases glycosaminoglycan biosynthesis and promotes tumor cell motility, spheroid growth, and therapeutic resistance. [Abstract]2025 Oct 17:S0945-053X(25)00104-0. PMID: 41110727 -
Acta Physiol
Activation of TGR5 Alleviates Renal Fibrosis by Promoting NEDD4L-Mediated p-Smad2/3 Ubiquitination. [Abstract]2026 Feb;242(2):e70163. PMID: 41536162 -
Int Immunopharmacol
Glucocorticoid signaling mitigates colitis-associated visceral hypersensitivity by suppressing 5-HT release in enterochromaffin cells via a GR-PI3K-SGK1 axis. [Abstract]2026 Mar 1:172:116207. PMID: 41554225 -
Immunology
NLR family pyrin domain containing 3 (NLRP3) and caspase 1 (CASP1) modulation by intracellular Cl- concentration. [Abstract]2021 Aug;163(4):493-511. PMID: 33835494 -
Naunyn Schmiedebergs Arch Pharmacol
The protective effects of gallic acid and SGK1 inhibitor on cardiac damage and genes involved in Ca2+ homeostasis in an isolated heart model of ischemia/reperfusion injury in rat. [Abstract]2024 Jul;397(7):5207-5217. PMID: 38252301 -
Viruses
2024 Aug 16;16(8):1308. PMID: 39205282 -
Arch Biochem Biophys
Identification and characterization of human PEIG-1/GPRC5A as a 12-O-tetradecanoyl phorbol-13-acetate (TPA) and PKC-induced gene. [Abstract]2020 Jul 15;687:108375. PMID: 32339486 -
Cancer Control
The Serum- and Glucocorticoid-Inducible Kinase 1 (SGK1) as a Novel Therapeutic Target in Mantle Cell Lymphoma. [Abstract]2022 Jan-Dec:29:10732748221143881. PMID: 36519740 -
JID Innov
High-salt diet aggravates skin inflammation of psoriasis-like mouse model with CCL20‒CCR6 axis further activation. [Abstract]2026 Jan 19;6(2):100451. PMID: 41716629 -
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Rep Biochem Mol Biol
Effect of Gallic Acid Pretreatment and SGK1 Enzyme Inhibition on Cardiac Function and Inflammation in a Rat Model of Ischemia-Reperfusion Injury. [Abstract]2023 Apr;12(1):159-172. PMID: 37724153 -
Acta Otolaryngol
Insulin regulates Nedd4-2 via a PKB-dependent mechanism in HEI-OC1 auditory cells-crosstalks with sphingolipid and cAMP signaling. [Abstract]2022 Jan;142(1):6-12. PMID: 34962430 -
Biomed Pharmacother
Inhibition the ubiquitination of ENaC and Na,K-ATPase with erythropoietin promotes alveolar fluid clearance in sepsis-induced acute respiratory distress syndrome. [Abstract]2024 May:174:116447. PMID: 38518606 -
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Lösungsmittel & Löslichkeit
DMSO : 40 mg/mL (104.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Sherk AB, et al. Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res. 2008 Sep 15;68(18):7475-83. [Content Brief]
[2]. Mansley MK, et al. Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption. Br J Pharmacol. 2010 Oct;161(3):571-88. [Content Brief]
[3]. Peng HY, et al. Spinal SGK1/GRASP-1/Rab4 is involved in complete Freund's adjuvant-induced inflammatory pain via regulating dorsal horn GluR1-containing AMPA receptor trafficking in rats. Pain. 2012 Dec;153(12):2380-92. [Content Brief]
[4]. Peng HY, et al. Spinal serum-inducible and glucocorticoid-inducible kinase 1 mediates neuropathic pain via kalirin and downstream PSD-95-dependent NR2B phosphorylation in rats. J Neurosci. 2013 Mar 20;33(12):5227-40. [Content Brief]
[5]. Alamares-Sapuay JG, et al. Serum- and glucocorticoid-regulated kinase 1 is required for nuclear export of the ribonucleoprotein of influenza A virus. J Virol. 2013 May;87(10):6020-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6147 mL | 13.0736 mL | 26.1472 mL | 65.3680 mL |
| 5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL | 13.0736 mL | |
| 10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL | 6.5368 mL | |
| 15 mM | 0.1743 mL | 0.8716 mL | 1.7431 mL | 4.3579 mL | |
| 20 mM | 0.1307 mL | 0.6537 mL | 1.3074 mL | 3.2684 mL | |
| 25 mM | 0.1046 mL | 0.5229 mL | 1.0459 mL | 2.6147 mL | |
| 30 mM | 0.0872 mL | 0.4358 mL | 0.8716 mL | 2.1789 mL | |
| 40 mM | 0.0654 mL | 0.3268 mL | 0.6537 mL | 1.6342 mL | |
| 50 mM | 0.0523 mL | 0.2615 mL | 0.5229 mL | 1.3074 mL | |
| 60 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0895 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3268 mL | 0.8171 mL | |
| 100 mM | 0.0261 mL | 0.1307 mL | 0.2615 mL | 0.6537 mL |
GSK 650394 Related Classifications
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