GSK-650394


Catalog No. size PriceQuantity
M6577-2 2mg solid $95
M6577-10 10mg solid $391

Description

Cas:890842-28-1

Product Information:

GSK-650394 is a competitive inhibitor that quantitatively blocks the effect of androgens on LNCaP cell growth.

 

Chemical Formula: C25H22N2O2

 

Exact Mass: 382.16813

 

Molecular Weight: 382.45

 

Elemental Analysis: C, 78.51; H, 5.80; N, 7.32; O, 8.37

 

Synonym:

 

GSK650394

GSK-650394

GSK 650394

 

Chemical Name:

2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid.

 

InChi Key: 

WVSBGSNVCDAMCF-UHFFFAOYSA-N

 

InChi Code: 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)

 

Smiles Code:

O=C(O)C1=CC=C(C2=CNC3=NC=C(C4=CC=CC=C4)C=C32)C=C1C5CCCC5

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

 

References

 

  1. Su Y, Qadri SM, Cayabyab FS, Wu L, Liu L. Regulation of methylglyoxal-elicited leukocyte recruitment by endothelial SGK1/GSK3 signaling. Biochim Biophys Acta. 2014 Jul 5;1843(11):2481-2491. doi: 10.1016/j.bbamcr.2014.06.018. [Epub ahead of print] PubMed PMID: 25003317.

 

  1. Zhang L, Liu J, Liu Y, Xu Y, Zhao X, Qian J, Sun B, Xing C. Fluvastatin inhibits the expression of fibronectin in human peritoneal mesothelial cells induced by high-glucose peritoneal dialysis solution via SGK1 pathway. Clin Exp Nephrol. 2014 Jun 20. [Epub ahead of print] PubMed PMID: 24942605.

 

  1. Mattes C, Laube M, Thome UH. Rapid elevation of sodium transport through insulin is mediated by AKT in alveolar cells. Physiol Rep. 2014 Mar 20;2(3):e00269. doi: 10.1002/phy2.269. Print 2014. PubMed PMID: 24760523; PubMed Central PMCID: PMC4002249.

 

  1. Isikbay M, Otto K, Kregel S, Kach J, Cai Y, Vander Griend DJ, Conzen SD, Szmulewitz RZ. Glucocorticoid receptor activity contributes to resistance to androgen-targeted therapy in prostate cancer. Horm Cancer. 2014 Apr;5(2):72-89. doi: 10.1007/s12672-014-0173-2. Epub 2014 Mar 11. PubMed PMID: 24615402.

 

  1. Chatterjee S, Schmidt S, Pouli S, Honisch S, Alkahtani S, Stournaras C, Lang F. Membrane androgen receptor sensitive Na+/H+ exchanger activity in prostate cancer cells. FEBS Lett. 2014 May 2;588(9):1571-9. doi: 10.1016/j.febslet.2014.02.040. Epub 2014 Mar 4. PubMed PMID: 24607544.

 

Products are for research use only. Not for human use.

 

 

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