NSC45586 sodium
Based on 1 publication(s) in Google Scholar
NSC45586 sodium is an inhibitor of PHLPP. NSC45586 sodium targets the PP2C phosphatase domains of PHLPP1 and PHLPP2, blocks the phosphatase activity of PHLPP, increases the expression level of FOXO1 in the nucleus, and reduces the protein expression of PHLPP1. NSC45586 sodium activates the AKT survival signaling pathway, enhances IGF-1-induced AKT activation, and inhibits the phosphorylation of AKT/ERK under basal conditions. NSC45586 sodium reduces staurosporine-induced neuronal death, preserves notochord cell morphology and KRT19 expression, inhibits cell apoptosis (apoptosis), improves the viability and proliferation of nucleus pulposus cells, upregulates the expression of ACAN/SOX9, and downregulates the expression of MMP13. NSC45586 sodium binds tightly to bovine serum albumin (bovine serum albumin), and exerts a more significant effect on nucleus pulposus in male individuals. NSC45586 sodium can be used in studies related to global cerebral ischemia and intervertebral disc degeneration.
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- 純度: 98.0%
- CAS 番号: 6300-44-3
- 分子式: C20H17N6NaO3
- 分子量:412.38
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 NSC45586 sodium
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生物活性
PHLPP1/2, Akt[1]
NSC45586 (0-100 μM; 35 min) sodium activates basal AKT in primary rat cortical neurons and enhances IGF-1-induced AKT activation[1].
NSC45586 (0-250 μM; 24 h) sodium significantly reduces STS (HY-15141)-induced death of primary rat cortical neurons[1].
NSC45586 (200 μM; 24 h) sodium increases the number of viable cells in rat primary neuron/astrocyte co-cultures following exposure to STS[1].
NSC45586 (50 μM; 35 min) sodium significantly inhibits basal AKT and ERK phosphorylation in primary rat astrocytes[1].
NSC45586 (100 μM; 24 h) sodium reduces the expression of PHLPP1 protein in degenerative human nucleus pulposus (NP) cells, with a more significant effect in male cells[2].
NSC45586 (0-100 μM; 24 h) sodium exhibits cytocompatibility and significantly promotes the proliferation of degenerated male human nucleus pulposus cells[2].
NSC45586 (25-100 μM; 24 h) sodium promotes the formation of healthy nucleus pulposus cell phenotypes by upregulating the expression of KRT19, ACAN and SOX9 and downregulating the expression of MMP13 in degenerative human nucleus pulposus cells, and this effect is more pronounced in male cells[2].
NSC45586 (25-100 μM; 30 min) sodium upregulates the phosphorylation level of AKT and the expression of FOXO1 protein in degenerative human nucleus pulposus cells from male donors in a dose-dependent manner[2].
NSC45586 (100 μM; 24 h) sodium promotes a healthy nucleus pulposus cell phenotype in degenerative human nucleus pulposus cells from male donors by activating the FOXO1 signaling pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:100 μM
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Incubation Time:24 h
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Result:Significantly reduced PHLPP1 protein expression (but not PHLPP2) in human NP cells, with a more pronounced reduction observed in male cells.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:25, 50, and 100 μM
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Incubation Time:24 h
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Result:Demonstrated good cytocompatibility at concentrations up to 100 μM.
Significantly increased cell proliferation in male human NP cells at all tested concentrations.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:25, 50, and 100 μM
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Incubation Time:24 h
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Result:Significantly increased KRT19 gene expression in both female and male cells.
Significantly increased SOX9 gene expression in both female and male cells.
Significantly increased ACAN gene expression in male cells.
Significantly reduced MMP13 gene expression in male cells, with effects more pronounced in males overall.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:25, 50, and 100 μM
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Incubation Time:30 min
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Result:Increased AKT phosphorylation in male human NP cells in a dose-dependent manner.
Increased FOXO1 protein expression in male human NP cells in a dose-dependent manner.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:100 μM
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Incubation Time:24 h (following 1 h pre-incubation with 200 nM AS1842856 or 100 nM Wortmannin)
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Result:Reversed the beneficial effects on KRT19 and ACAN gene expression in male human NP cells when pre-treated with the FOXO1 inhibitor AS1842856.
Showed no significant effect on gene expression changes induced by NSC45586 when pre-treated with the PI3K/AKT inhibitor Wortmannin.
化学情報
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CAS 番号 6300-44-3
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性状 Solid
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分子量 412.38
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分子式 C20H17N6NaO3
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Color Brown to black
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SMILES
O=C(O[Na])C1=CC(/N=N/C2=CC=C(/N=N/C3=CC(C)=C(N)C=C3N)C=C2)=CC=C1O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Int Dent J
Calpain-1 Potentiates Periodontal Regeneration via PHLPP1-ERK-Driven Osteogenesis in Periodontal Ligament Stem Cells. [Abstract]2025 Dec 6;76(1):109309. PMID: 41353895
溶剤 & 溶解度
H2O : 5 mg/mL (12.12 mM; ultrasonic and warming and heat to 80°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Jackson TC, et al. Pharmacological inhibition of pleckstrin homology domain leucine-rich repeat protein phosphatase is neuroprotective: differential effects on astrocytes. J Pharmacol Exp Ther. 2013;347(2):516-528. [Content Brief]
[2]. Zhang C, et al. Differential efficacy of two small molecule PHLPP inhibitors to promote nucleus Pulposus cell health. JOR Spine. 2023;7(1):e1306. Published 2023 Dec 4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.4249 mL | 12.1247 mL | 24.2495 mL | 60.6237 mL |
| 5 mM | 0.4850 mL | 2.4249 mL | 4.8499 mL | 12.1247 mL | |
| 10 mM | 0.2425 mL | 1.2125 mL | 2.4249 mL | 6.0624 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
NSC45586 sodium 関連分類
HY-19820A 関連分類
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