[CAS NO. 890842-28-1] GSK650394

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PRODUCTS SPECIFICATIONS [890842-28-1]

Catalog

HY-15192

Brand

MCE

CAS

890842-28-1

DESCRIPTION [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

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

11 Publications Citing Use of MCE

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

In Vitro:

DMSO : ≥ 40.7 mg/mL ( 106.42 mM )

* "≥" 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 available by MCE.