GSK650394
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406547

CAS#: 890842-28-1

Description: GSK650394 is a competitive inhibitor that quantitatively blocks the effect of androgens on LNCaP cell growth.


Chemical Structure

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GSK650394
CAS# 890842-28-1

Theoretical Analysis

MedKoo Cat#: 406547
Name: GSK650394
CAS#: 890842-28-1
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

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Same day
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 750.0 Same day
500.0mg USD 1550.0 Same day
1.0g USD 2650.0 Same day
2.0g USD 3750.0 Same day
5.0g USD 5650.0 2 weeks
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Synonym: GSK650394; GSK-650394; GSK 650394.

IUPAC/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

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

Preparing Stock Solutions

The following data is based on the product molecular weight 382.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

2: 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.

3: 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.

4: 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.

5: 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.

6: Bradford D, Raghuram V, Wilson JL, Chou CL, Hoffert JD, Knepper MA, Pisitkun T. Use of LC-MS/MS and Bayes' theorem to identify protein kinases that phosphorylate aquaporin-2 at Ser256. Am J Physiol Cell Physiol. 2014 Jul 15;307(2):C123-39. doi: 10.1152/ajpcell.00377.2012. Epub 2014 Mar 5. PubMed PMID: 24598363; PubMed Central PMCID: PMC4101623.

7: Bomberger JM, Coutermarsh BA, Barnaby RL, Sato JD, Chapline MC, Stanton BA. Serum and glucocorticoid-inducible kinase1 increases plasma membrane wt-CFTR in human airway epithelial cells by inhibiting its endocytic retrieval. PLoS One. 2014 Feb 21;9(2):e89599. doi: 10.1371/journal.pone.0089599. eCollection 2014. PubMed PMID: 24586903; PubMed Central PMCID: PMC3931797.

8: Burgon J, Robertson AL, Sadiku P, Wang X, Hooper-Greenhill E, Prince LR, Walker P, Hoggett EE, Ward JR, Farrow SN, Zuercher WJ, Jeffrey P, Savage CO, Ingham PW, Hurlstone AF, Whyte MK, Renshaw SA. Serum and glucocorticoid-regulated kinase 1 regulates neutrophil clearance during inflammation resolution. J Immunol. 2014 Feb 15;192(4):1796-805. doi: 10.4049/jimmunol.1300087. Epub 2014 Jan 15. PubMed PMID: 24431232; PubMed Central PMCID: PMC3921102.

9: Liu J, Wu X, Liu Y, Xu Y, Huang Y, Xing C, Wang X. High-glucose-based peritoneal dialysis solution induces the upregulation of VEGF expression in human peritoneal mesothelial cells: The role of pleiotrophin. Int J Mol Med. 2013 Nov;32(5):1150-8. doi: 10.3892/ijmm.2013.1491. Epub 2013 Sep 12. PubMed PMID: 24042838.

10: Anacker C, Cattaneo A, Musaelyan K, Zunszain PA, Horowitz M, Molteni R, Luoni A, Calabrese F, Tansey K, Gennarelli M, Thuret S, Price J, Uher R, Riva MA, Pariante CM. Role for the kinase SGK1 in stress, depression, and glucocorticoid effects on hippocampal neurogenesis. Proc Natl Acad Sci U S A. 2013 May 21;110(21):8708-13. doi: 10.1073/pnas.1300886110. Epub 2013 May 6. PubMed PMID: 23650397; PubMed Central PMCID: PMC3666742.

11: Peng HY, Chen GD, Lai CY, Hsieh MC, Lin TB. 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. doi: 10.1523/JNEUROSCI.4452-12.2013. PubMed PMID: 23516288.

12: Alamares-Sapuay JG, Martinez-Gil L, Stertz S, Miller MS, Shaw ML, Palese P. 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. doi: 10.1128/JVI.01258-12. Epub 2013 Mar 13. PubMed PMID: 23487453; PubMed Central PMCID: PMC3648197.

13: Peng HY, Chen GD, Hsieh MC, Lai CY, Huang YP, Lin TB. 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. doi: 10.1016/j.pain.2012.08.004. Epub 2012 Sep 11. PubMed PMID: 22980744.

14: Borst O, Schmidt EM, Münzer P, Schönberger T, Towhid ST, Elvers M, Leibrock C, Schmid E, Eylenstein A, Kuhl D, May AE, Gawaz M, Lang F. The serum- and glucocorticoid-inducible kinase 1 (SGK1) influences platelet calcium signaling and function by regulation of Orai1 expression in megakaryocytes. Blood. 2012 Jan 5;119(1):251-61. doi: 10.1182/blood-2011-06-359976. Epub 2011 Oct 26. PubMed PMID: 22031864.

15: Thomas SV, Kathpalia PP, Rajagopal M, Charlton C, Zhang J, Eaton DC, Helms MN, Pao AC. Epithelial sodium channel regulation by cell surface-associated serum- and glucocorticoid-regulated kinase 1. J Biol Chem. 2011 Sep 16;286(37):32074-85. doi: 10.1074/jbc.M111.278283. Epub 2011 Jul 22. PubMed PMID: 21784856; PubMed Central PMCID: PMC3173222.

16: Mansley MK, Wilson SM. 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. doi: 10.1111/j.1476-5381.2010.00898.x. PubMed PMID: 20880397; PubMed Central PMCID: PMC2990156.

17: Sherk AB, Frigo DE, Schnackenberg CG, Bray JD, Laping NJ, Trizna W, Hammond M, Patterson JR, Thompson SK, Kazmin D, Norris JD, McDonnell DP. 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. doi: 10.1158/0008-5472.CAN-08-1047. PubMed PMID: 18794135; PubMed Central PMCID: PMC2562281.



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