- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 890842-28-1] GSK650394
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15192 |
| Brand: | MCE |
| CAS: | 890842-28-1 |
Overview
| MDL | MFCD12828779 |
|---|---|
| Molecular Weight | 382.45 |
| Molecular Formula | C25H22N2O2 |
| SMILES | O=C(O)C(C=C1)=C(C2CCCC2)C=C1C3=CNC(C3=C4)=NC=C4C5=CC=CC=C5 |
11 Publications Citing Use of MCE
- [1]Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
- [2]Oncogene. 2021 Sep;40(35):5367-5378.
- [3]Br J Pharmacol. 2020 Apr;177(7):1666-1676.
- [4]Immunology. 2021 Apr 9.
- [5]Int J Biol Sci. 2023; 19(1): 204-224.
- [6]Arch Biochem Biophys. 2020 Jul 15;687:108375.
- [7]Cancer Control. 2022 Jan-Dec;29:10732748221143881.
- [8]Acta Otolaryngol. 2021 Dec 28;1-7.
- [9]Research Square Print. December 27th, 2022.
- [10]Programa de Doctorado en Biomedicina. 2020 Sep.
- [11]Harvard Medical School LINCS LIBRARY
Summary
GSK 650394 is a novel SGK inhibitor with IC 50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.
IC50 & Target
|
SGK1
|
In Vitro
GSK650394 is relatively non-toxic, with LC 50 values of 41 μM in M1 cells (68 times its activity IC 50 ) and a LC 50 greater than 100 μM in HeLa cells. GSK650394 inhibits SGK1-mediated epithelial transport with an IC 50 of 0.6 μM in the SCC assay. GSK650394 inhibits the growth of LNCaP cells with IC 50 of approximately 1 μM [1] . GSK650394A inhibits the insulin-induced phosphorylation of PKB-Ser 473 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : ≥ 40.7 mg/mL ( 106.42 mM )
* "≥" means soluble, but saturation unknown.
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 |
References
- [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.
- [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.
- [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.
- [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.
- [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.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.