GSK650394

Category	Influenza Virus
CAS	890842-28-1
Description	GSK650394 is a competitive inhibitor that quantitatively blocks the effect of androgens on LNCaP cell growth.

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Product Information

Synonyms	GSK650394; GSK-650394; GSK 650394
Molecular Weight	382.45
Molecular Formula	C25H22N2O2
Canonical SMILES	C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=NC=C(C=C34)C5=CC=CC=C5)C(=O)O
InChI	InChI=1S/C25H22N2O2/c28-25(29)20-11-10-18(12-21(20)17-8-4-5-9-17)23-15-27-24-22(23)13-19(14-26-24)16-6-2-1-3-7-16/h1-3,6-7,10-15,17H,4-5,8-9H2,(H,26,27)(H,28,29)
InChIKey	WVSBGSNVCDAMCF-UHFFFAOYSA-N
Purity	0.98
Density	1.3±0.1 g/cm3
Solubility	In Vitro: DMSO : ≥ 40.7 mg/mL(106.42 mM) In Vivo: 1.Add each solvent one by one:10% DMSO >> 40%PEG300 >> 5%Tween-804 >> 5% 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
Appearance	Solid powder
Storage	Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month
Complexity	569
Exact Mass	382.168127949
Index Of Refraction	1.680
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. 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.
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. 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.
PSA	65.98000
Target	SGK; Influenza Virus
XLogP3-AA	6.1