GSK 650394
Modify Date: 2024-01-02 16:21:47
GSK 650394 structure
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Common Name | GSK 650394 | ||
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| CAS Number | 890842-28-1 | Molecular Weight | 382.454 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C25H22N2O2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
Use of GSK 650394GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. |
| Name | 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid |
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| Synonym | More Synonyms |
| Description | GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. |
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| Related Catalog | |
| Target |
IC50: 62 nM (SGK1), 103 nM (SGK2) |
| 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[1]. 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[2]. |
| 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]. |
| Cell Assay | The toxicity of GSK650394 to M-1 and HeLa cells is assessed using the Cell Proliferation Kit (XTT) following manufacturer’s instructions. Briefly, 10,000 HeLa or M-1 cells/well are plated into 96-well plates in 100μL of the appropriate maintenance media. After 48 h, media is removed and replaced with 100 μL of EMEM with Earle’s salts containing 2 mM L-glutamine and 1% antibiotic-antimycotic overnight. M-1 cells are also supplemented with 1 μg/mL insulin, 6.25 μg/mL sodium selenite, and 6.25 μg/mL transferrin. After 24 h, the media is removed and replaced with 100 μL media alone or media containing increasing concentrations of GSK650394. For HeLa cells, 50 μL of activated XTT solution is added after 4 h. For M-1 cells, 50 μL of activated XTT solution is added after 24 h. Following a 2 h incubation, absorbance is measured at 490 nm using a SpectraMAX PLUS spectrophotometer and the data analyzed to obtain IC50 values using GraphPad Prism 3 software. |
| Animal Admin | Briefly, the rats are anesthetized under isoflurane anesthesia (induction 5%, maintenance 2% in oxygen). An incision is made, and the left L5 spinal nerves are carefully isolated and tightly ligated with 6-0 silk sutures 2-5 mm distal to the dorsal root ganglia. GSK650394 (10, 30, and 100 nM, 10 μL) is administered by bolus injection at 3 or 7 d or by daily injection for 7 d (day 0-6) postspinal nerve ligation. A vehicle solution of a volume identical to that of the tested agents is dispensed to serve as a control. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C25H22N2O2 |
| Molecular Weight | 382.454 |
| Exact Mass | 382.168121 |
| PSA | 65.98000 |
| LogP | 6.95 |
| Index of Refraction | 1.680 |
| Storage condition | -20℃ |
| RIDADR | NONH for all modes of transport |
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| Benzoic acid, 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)- |
| hms2043a20 |
| 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid |
| GSK 650394 |
- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: GSK 650394
- Price: ￥2736.0/100mg ￥1216.0/25mg ￥406.0/5mg ￥1826.0/50mg
- Purity: 98.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: SGK inhibitor GS650394
- Price: $500.0/100mg $900.0/250mg $1800.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: GSK 650394
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Ms Wang
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Price: $110/10mM*1mLinDMSO
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