SB 415286
Based on 7 publication(s) in Google Scholar
SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
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- Pureté: 99.46%
- CAS No.: 264218-23-7
- Formule: C16H10ClN3O5
- Masse moléculaire:359.72
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SB 415286
More- Brain Behav Immun. 2021 May:94:327-337. [Abstract]
- Food Biosci. 7 May 2022, 101766.
- Food Biosci. April 2022, 101571.
- Front Pharmacol. 2022 Sep 26:13:925489. [Abstract]
- Prog Neuropsychopharmacol Biol Psychiatry. 2024 Feb 8:129:110874. [Abstract]
- Norges teknisk-naturvitenskapelige universitet. 2025.
- Oncotarget. 2017 Jul 7;8(47):82174-82184. [Abstract]
Customer Validation & Images
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WB
Activité biologique
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hGSK-3α 77.5 nM (IC50) |
hGSK-3β 77.5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
45.6 μM
Compound: SB-415286
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Stimulation of glycogen synthase in CHO cells expressing human insulin receptor
Stimulation of glycogen synthase in CHO cells expressing human insulin receptor
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[PMID: 12852764] |
SB 415286 (SB-415286) inhibits human GSK-3α with an IC50 of 77.5 nM, and a Ki of 30.75 nM. SB-415286 stimulates glycogen synthesis in the Chang human liver cell line with EC50 of 2.9 μM. SB-415286 stimulates glycogen synthase activity in Chang human liver cells. SB-415286 induces transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells[1]. SB 415286 (SB-415286, 5-44 μM) attenuates B65 cell loss mediated by 1 mM H2O2. SB-415286 (5-44 μM) causes a significant dose-dependent decrease in the fluorescence intensity of DCF, and attenuates B65 ROS production as mediated by 1 mM H2O2. SB-415286 (5-44 μM) also attenuates ROS production in CGN mediated by 1 mM H2O2[2]. SB-415286 (50 μM) induces a substantial suppression of immunoprecipitated GSK3 activity by 97%[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 264218-23-7
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Appearance Solid
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Masse moléculaire 359.72
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Formule C16H10ClN3O5
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Color Light yellow to yellow
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SMILES
O=C(C(NC1=CC=C(O)C(Cl)=C1)=C2C3=CC=CC=C3[N+]([O-])=O)NC2=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Brain Behav Immun
Ghrelin modulates dopaminergic neuron formation and attention deficit hyperactivity disorder-like behaviors: From animals to human models. [Abstract]2021 May:94:327-337. PMID: 33412253 -
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Front Pharmacol
GSK3β-dependent lysosome biogenesis: An effective pathway to mitigate renal fibrosis with LM49. [Abstract]2022 Sep 26:13:925489. PMID: 36225562 -
Prog Neuropsychopharmacol Biol Psychiatry
Transcriptome profile of reserpine-induced locomotor behavioral changes in zebrafish (Danio rerio). [Abstract]2024 Feb 8:129:110874. PMID: 37839537 -
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Oncotarget
Quaking-5 suppresses aggressiveness of lung cancer cells through inhibiting β-catenin signaling pathway. [Abstract]2017 Jul 7;8(47):82174-82184. PMID: 29137254
SB 415286 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 7;8(47):82174-82184. [Abstract]
Comparisons of β-catenin and QKI-5 levels between H1299-vector and H1299-QKI-5 cells in which β-catenin degradation is blocked with proteasome inhibitor MG132 or GSK3β inhibitor SB415286 (25 μM).
Solvant et solubilité
DMSO : 100 mg/mL (277.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
GSK-3 kinase activity is measured, in the presence or absence of SB-216763 or SB-415286, in a reaction mixture containing final concentrations of: 1 nM human GSK-3α or rabbit GSK3α; 50 mM MOPS pH 7.0; 0.2 mM EDTA; 10 mM Mg-acetate; 7.5 mM β-mercaptoethanol; 5% (w/v) glycerol; 0.01% (w/v) Tween-20; 10% (v/v) DMSO; 28 μM GS-2 peptide substrate. The GS-2 peptide sequence corresponds to a region of glycogen synthase that is phosphorylated by GSK-3. The assay is initiated by the addition of 0.34 μCi [33P]γ-ATP (IC50 determinations) or 2.7 μCi [33P]γ-ATP (Ki determinations). The total ATP concentration is 10 μM (IC50 determinations) or ranges from 0 to 45 μM (Ki determinations). Following 30 min incubation at room temperature the assay is stopped by the addition of one third assay volume of 2.5% (v/v) H3PO4 containing 21 mM ATP. Samples are spotted onto P30 phosphocellulose mats and these are washed six times in 0.5% (v/v) H3PO4. The filter mats are sealed into sample bags containing Wallac betaplate scintillation fluid. 33P incorporation into the substrate peptide is determined by counting the mats in a Wallac microbeta scintillation counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
B65 cells are used after 24 h of in vitro culture. CGN are used after 7-8 days in vitro. Lithium and SB-415286 are dissolved in culture media and DMSO, respectively, and added to the neuronal preparation at the precise concentrations, 1 h before addition H2O2 (50 μM to 1 mM). To assess the loss in cell viability, we use the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium] method. MTT is added to the cells at a final concentration of 250 μM and incubated for 1 h, allowing the reduction in MTT to produce a dark blue formazan product. Media are then removed, and cells are dissolved in dimethylsulfoxide. Formazan production is measured by the absorbency change at 595 nm using a microplate reader. Viability results are expressed as percentages. The absorbency measured from non-treated cells is taken to be 100%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (289 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803. [Content Brief]
[2]. Pizarro JG, et al. Neuroprotective effects of SB-415286 on hydrogen peroxide-induced cell death in B65 rat neuroblastoma cells and neurons. Int J Dev Neurosci. 2008 May-Jun;26(3-4):269-76. [Content Brief]
[3]. MacAulay K, et al. Use of lithium and SB-415286 to explore the role of glycogen synthase kinase-3 in the regulation of glucose transport and glycogen synthase. Eur J Biochem. 2003 Sep;270(18):3829-38. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7799 mL | 13.8997 mL | 27.7994 mL | 69.4985 mL |
| 5 mM | 0.5560 mL | 2.7799 mL | 5.5599 mL | 13.8997 mL | |
| 10 mM | 0.2780 mL | 1.3900 mL | 2.7799 mL | 6.9498 mL | |
| 15 mM | 0.1853 mL | 0.9266 mL | 1.8533 mL | 4.6332 mL | |
| 20 mM | 0.1390 mL | 0.6950 mL | 1.3900 mL | 3.4749 mL | |
| 25 mM | 0.1112 mL | 0.5560 mL | 1.1120 mL | 2.7799 mL | |
| 30 mM | 0.0927 mL | 0.4633 mL | 0.9266 mL | 2.3166 mL | |
| 40 mM | 0.0695 mL | 0.3475 mL | 0.6950 mL | 1.7375 mL | |
| 50 mM | 0.0556 mL | 0.2780 mL | 0.5560 mL | 1.3900 mL | |
| 60 mM | 0.0463 mL | 0.2317 mL | 0.4633 mL | 1.1583 mL | |
| 80 mM | 0.0347 mL | 0.1737 mL | 0.3475 mL | 0.8687 mL | |
| 100 mM | 0.0278 mL | 0.1390 mL | 0.2780 mL | 0.6950 mL |
SB 415286 Related Classifications
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