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MedKoo Cat#: 406547 | Name: GSK650394
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Description:

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

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

Chemical Structure

GSK650394
GSK650394
CAS#890842-28-1

Theoretical Analysis

MedKoo Cat#: 406547

Name: GSK650394

CAS#: 890842-28-1

Chemical Formula: C25H22N2O2

Exact Mass: 382.1681

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
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 4,250.00 Ready to ship
2g USD 6,450.00 Ready to ship
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Related CAS #
No Data
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
More Info
         
Biological target:
GSK 650394 is a SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively.
In vitro activity:
To investigate the role of SGK1 in vitro, HK-2 cells were exposed to 30 mM glucose to induce DN cell modelling. The results revealed that protein and mRNA levels were augmented (Figure 3A and and3B).3B). GSK (GSK650394), as an inhibitor of SGK1, was then utilized in the present study. As presented in Figure 3C, the expression of E-cadherin was decreased, and the expression of N-cadherin and Vimentin were increased in the Glucose+GSK group. In TGF-β1 and high glucose treatment groups, the protein expression of E-cadherin was downregulated, which was accompanied with an upregulated expression of N-cadherin and Vimentin compared with the Glucose+GSK group. After treatment with TGF-β1 in combination with GSK, the expression of E-cadherin was augmented. Furthermore, N-cadherin and Vimentin levels were augmented. These results indicated that the inhibition of SGK1 suppressed EMT progression. Reference: Am J Transl Res. 2019; 11(8): 4946–4956. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6731399/
In vivo activity:
Contrary to expectation, the infarct volume in mice injected with SGK inhibitors was significantly smaller (gsk650394; 30.3±4.5%, n=10, p<0.01, EMD638683; 39.3±2.9%, n=10, p<0.01, Figure 1A). This study also investigated the effect of SGK inhibition on the infarct volume under diabetic condition, which is one of the common comorbidities of stroke. Similar results were observed in type I diabetic mice that underwent 45 min MCAO; administration of gsk650394 significantly decreased the infarct volume (DMSO; 52.3±3.3%, n=4, gsk650394; 39.0±4.2%, n=4, p<0.05, Figure 1B). Collectively, these data suggest that SGK inhibitors attenuate the stroke-mediated brain injury. Reference: J Neurochem. 2016 Jul; 138(2): 354–361. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4936920/
Solvent mg/mL mM
Solubility
DMSO 46.2 120.90
DMSO:PBS (pH 7.2) (1:1) 0.5 1.31
DMF 30.0 78.44
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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
Formulation protocol:
1. Zhuang L, Jin G, Hu X, Yang Q, Shi Z. The inhibition of SGK1 suppresses epithelial-mesenchymal transition and promotes renal tubular epithelial cell autophagy in diabetic nephropathy. Am J Transl Res. 2019 Aug 15;11(8):4946-4956. PMID: 31497211; PMCID: PMC6731399. 2. Wang M, Xue Y, Shen L, Qin P, Sang X, Tao Z, Yi J, Wang J, Liu P, Cheng H. Inhibition of SGK1 confers vulnerability to redox dysregulation in cervical cancer. Redox Biol. 2019 Jun;24:101225. doi: 10.1016/j.redox.2019.101225. Epub 2019 May 20. PMID: 31136958; PMCID: PMC6536746. 3. Lee RH, Grames MS, Wu CY, Lien CF, Couto E Silva A, Possoit HE, Clemons GA, Citadin CT, Neumann JT, Pastore D, Lauro D, Della-Morte D, Lin HW. Upregulation of serum and glucocorticoid-regulated kinase 1 exacerbates brain injury and neurological deficits after cardiac arrest. Am J Physiol Heart Circ Physiol. 2020 Nov 1;319(5):H1044-H1050. doi: 10.1152/ajpheart.00399.2020. Epub 2020 Sep 18. PMID: 32946263; PMCID: PMC8083081. 4. Inoue K, Leng T, Yang T, Zeng Z, Ueki T, Xiong ZG. Role of serum- and glucocorticoid-inducible kinases in stroke. J Neurochem. 2016 Jul;138(2):354-61. doi: 10.1111/jnc.13650. Epub 2016 May 25. PMID: 27123541; PMCID: PMC4936920.
In vitro protocol:
1. Zhuang L, Jin G, Hu X, Yang Q, Shi Z. The inhibition of SGK1 suppresses epithelial-mesenchymal transition and promotes renal tubular epithelial cell autophagy in diabetic nephropathy. Am J Transl Res. 2019 Aug 15;11(8):4946-4956. PMID: 31497211; PMCID: PMC6731399. 2. Wang M, Xue Y, Shen L, Qin P, Sang X, Tao Z, Yi J, Wang J, Liu P, Cheng H. Inhibition of SGK1 confers vulnerability to redox dysregulation in cervical cancer. Redox Biol. 2019 Jun;24:101225. doi: 10.1016/j.redox.2019.101225. Epub 2019 May 20. PMID: 31136958; PMCID: PMC6536746.
In vivo protocol:
1. Lee RH, Grames MS, Wu CY, Lien CF, Couto E Silva A, Possoit HE, Clemons GA, Citadin CT, Neumann JT, Pastore D, Lauro D, Della-Morte D, Lin HW. Upregulation of serum and glucocorticoid-regulated kinase 1 exacerbates brain injury and neurological deficits after cardiac arrest. Am J Physiol Heart Circ Physiol. 2020 Nov 1;319(5):H1044-H1050. doi: 10.1152/ajpheart.00399.2020. Epub 2020 Sep 18. PMID: 32946263; PMCID: PMC8083081. 2. Inoue K, Leng T, Yang T, Zeng Z, Ueki T, Xiong ZG. Role of serum- and glucocorticoid-inducible kinases in stroke. J Neurochem. 2016 Jul;138(2):354-61. doi: 10.1111/jnc.13650. Epub 2016 May 25. PMID: 27123541; PMCID: PMC4936920.
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.