GSK 650394

SKU: orb1305255

Description

GSK 650394 is a potent small molecule inhibitor of serum- and glucocorticoid-regulated kinases SGK1 and SGK2. It has demonstrated antitumor properties in research models and has been shown to inhibit osteoclast differentiation, suggesting utility in studies of cancer and bone metabolism.

Research Area

Infectious Disease & Virology, Metabolism Research

Key Properties

• CAS Number: 890842-28-1
• MW: 382.45
• Purity: >99.99% (May vary between batches)
• Formula: C₂₅H₂₂N₂O₂
• SMILES: OC(=O)c1ccc(cc1C1CCCC1)-c1c[nH]c2ncc(cc12)-c1ccccc1
• Target: Influenza Virus,SGK
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (6.54 mM);DMSO:16.67 mg/mL (43.59 mM)

Bioactivity

• Target IC50:
  SGK2:103 nM|SGK1:62 nM
• In Vivo:
  METHODS: To validate in vivo efficacy against chronic HCV, Grazoprevir (1 mg/kg) was administered orally to HCV-infected chimpanzees harboring chronic gt1a or gt1b infections twice daily for seven days. RESULTS: Grazoprevir was able to suppress viral load by 4-5 logs in vivo. METHODS: To assess in vivo pharmacokinetics, Grazoprevir (5 mg/kg) was administered orally to rats. RESULTS: Plasma exposure to Grazoprevir was favorable, with an AUC of 0.7 µM h/mL.
• In Vitro:
  METHODS: HB1 cells were treated with Grazoprevir (6-30 nM) and G418 (0.5 mg/mL) for 3 weeks for in vitro resistance selection. RESULTS: Grazoprevir showed good mutational potency in all resistant variants and inhibited R155 and D168 mutations in particular. METHODS: 315 compounds with electrophilic moieties were experimentally screened to determine if they would covalently bind to the active site cysteine of SARS-CoV-2 3CLpro. RESULTS: Among the compounds, Grazoprevir was able to inhibit the activity of SARS-CoV-2 3CLpro.
• Cell Research:
  LNCaP cells are plated at a density of 5,000 cells per well in 96-well plates in 100 μL PRF-RPMI 1640, supplemented with 8% CS-FBS, 0.1 mM NEAA, and 1 mM NaPyr. At day three, cells are treated with hormone with or without GSK650394 by removing 50 μL of the media and replacing this with 50 μL of PRF-RPMI 1640 with 8% CS-FBS, NEAA, NaPyr containing a 2X concentration of the appropriate hormone/inhibitor treatment. At days 5 and 7, the treatment is repeated. On the tenth day, the media is removed and the relative cell number is measured using the FluoReporter Blue assay according to the manufacturer's instructions.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Influenza Virus, InfluenzaVirus, inhibit, GSK 650394, GSK650394, GSK-650394, Inhibitor, Serum and glucocorticoid-regulated kinase, Serum-glucocorticoid regulated kinase, SGK, SGK1, SGK2

Compound Identifiers

PubChem CID

25022668