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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
GSK650394 (GSK-650394) is a novel and potent competitive inhibitor of SGK1 (serum and glucocorticoid-regulated kinase 1) with anticancer effects. It inhibits SGK with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. SGK1 is an androgen-regulated target gene in cellular models of prostate cancer. GSK650394 quantitatively blocks the effect of androgens on LNCaP cell growth. SGK inhibitors could attenuate the stroke-mediated brain injury.
| ln Vitro |
In M1 cells, GSK650394 has an LC50 value of 41 μM (68 times its activity IC50) and larger than 100 μM in HeLa cells, suggesting that it is relatively innocuous. With an IC50 of 0.6 μM in the SCC assay, GSK650394 inhibits SGK1-mediated epithelial transport. With an IC50 of roughly 1 μM, GSK650394 suppresses the proliferation of LNCaP cells [1]. At 3 µM, GSK650394A blocks the phosphorylation of PKB-Ser473 induced by insulin, and at 10 µM, it completely eliminates this reaction. Hormone-deprived cells' phosphorylation of PRAS40-Ser246 is unaffected by GSK650394A (1–10 µM), and insulin-induced phosphorylation of this residue is also unaffected [2].
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| ln Vivo |
One day after CFA treatment, GSK650394 (1, 10, and 30 μM, 10 μL/rat, intrathecal) dose-dependently inhibits CFA-induced nociceptive behavior and related SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions [3]. Dose-dependently, GSK650394 at 10, 30, and 100 nM (10 μL) enhanced the ipsilateral hind paw at 1-3 and 1-3 retraction latency, but not the vehicle solution (SNL 3D+Veh and SNL 7D+Veh, respectively). On postoperative days 3 and 7 (SNL 3D+GSK and SNL 7D+GSK, respectively), one to five hours following injection. On postoperative days 3, 5, and 7, GSK650394 (100 nM, 10 μL, it) treatment decreased SNL-induced allodynia in SNL mice [4].
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| References |
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| Additional Infomation |
2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid is a phenylpyridine.
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| Molecular Formula |
C25H22N2O2
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|---|---|
| Molecular Weight |
382.4544
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| Exact Mass |
382.168
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| CAS # |
890842-28-1
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| PubChem CID |
25022668
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.680
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| LogP |
6.95
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
569
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WVSBGSNVCDAMCF-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid.
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| Synonyms |
GSK-650394; GSK650394; GSK 650394.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 40.7 mg/mL (~106.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.54 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 GSK650394 inhibits SGK1 activity and androgen-mediated LNCaP cell growth.Cancer Res.2008 Sep 15;68(18):7475-83. |
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 GSK650394 inhibits the activity of SGK1. |
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