SB 216763
Based on 47 publication(s) in Google Scholar
SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 280744-09-4
- Formula: C19H12Cl2N2O2
- Molecular Weight:371.22
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) SB 216763
More- Cell Res. 2022 Jun;32(6):513-529. [Abstract]
- Nat Commun. 2022 Apr 19;13(1):2105. [Abstract]
- Adv Sci (Weinh). 2026 Jun;13(36):e75157. [Abstract]
- Theranostics. 2019 Aug 12;9(20):5769-5783. [Abstract]
- Haematologica. 2020 Mar;105(3):661-673. [Abstract]
- Brain Behav Immun. 2026 Jun 22:137:106877.
- Biomed Pharmacother. 2025 Jun 27:189:118290. [Abstract]
- Biomed Pharmacother. 2019 Dec;120:109231. [Abstract]
- Br J Cancer. 2023 Mar;128(7):1344-1359. [Abstract]
- Cell Mol Life Sci. 2025 May 28;82(1):218. [Abstract]
- Biochem Pharmacol. 2018 Apr:150:280-292. [Abstract]
- Life Sci. 2025 Aug 30:380:123939. [Abstract]
- Life Sci. 2020 Sep 1;256:117983. [Abstract]
- Int J Mol Sci. 2024 May 17;25(10):5478. [Abstract]
- Biomolecules. 2024 Mar 15;14(3):354. [Abstract]
- Front Bioeng Biotechnol. 2023 Jul 28:11:1215233. [Abstract]
- Front Pharmacol. 2022 Mar 17;13:830554. [Abstract]
- Int Immunopharmacol. 2025 May 7:157:114796. [Abstract]
- Biosci Rep. 2023 Mar 31;43(3):BSR20222429. [Abstract]
- Eur J Pharmacol. 2022 Apr 5;920:174830. [Abstract]
- J Mol Cell Cardiol. 2020 Dec;149:82-94. [Abstract]
- Cancers (Basel). 2022 Nov 28;14(23):5854. [Abstract]
- Drug Dev Res. 2024 Jun;85(4):e22196. [Abstract]
- Mol Nutr Food Res. 2024 May 29:e2400123. [Abstract]
- iScience. 2025 Dec 1;29(1):114292. [Abstract]
- J Funct Foods. 2025 Apr.
- Sci Rep. 2024 Aug 16;14(1):19008. [Abstract]
- J Biol Chem. 2024 Apr;300(4):107208. [Abstract]
- Sci Rep. 2022 Nov 11;12(1):19323. [Abstract]
- Cell Signal. 2025 Dec 19:139:112333. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2023 Oct 31;1871(1):119623. [Abstract]
- Toxicol Appl Pharmacol. 2020 Jan 1;386:114813. [Abstract]
- Toxicol Appl Pharmacol. 2016 Dec 15:313:195-203. [Abstract]
- Mol Carcinog. 2026 Jun;65(6):754-769. [Abstract]
- Int J Med Sci. 2022 Mar 6;19(3):525-536. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2025 Oct 31. [Abstract]
- Mol Immunol. 2025 Oct:186:1-12. [Abstract]
- J Cell Biochem. 2018 Jul;119(7):5934-5943. [Abstract]
- SLAS Discov. 2024 Nov 5;29(8):100191. [Abstract]
- Theriogenology. 2026 Apr 1:254:117816. [Abstract]
- Biochem Biophys Res Commun. 2020 May 14;525(4):1074-1080. [Abstract]
- Radiat Med Prot. 2026 Jun 12.
- bioRxiv. 2023 Dec 13.
- SSRN. 2023 Jun 20.
- University of Rijeka. 2023.
- Evid Based Complement Alternat Med. 2022 Oct 11:2022:9969729. [Abstract]
- Evid Based Complement Alternat Med. 2019 May 30:2019:9692350. [Abstract]
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WB
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WB
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IF
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WB
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IF
Biological Activity
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GSK-3α 34.3 nM (IC50) |
GSK-3β 34.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Fibroblast | IC50 |
3 μM
Compound: 6, SB216763
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Inhibition of human SOD1 expressed in mouse fibroblasts after 48 hrs by ELISA relative to control
Inhibition of human SOD1 expressed in mouse fibroblasts after 48 hrs by ELISA relative to control
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[PMID: 24560539] |
| HEK293 | EC50 |
0.2 μM
Compound: SB-216763
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Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta
Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta
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[PMID: 12941331] |
| HEK293 | EC50 |
0.2 μM
Compound: SB-216763
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Effective concentration of compound against glycogen synthase kinase-3 in HEK293 cells
Effective concentration of compound against glycogen synthase kinase-3 in HEK293 cells
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[PMID: 15149684] |
| HEK293 | EC50 |
3.6 μM
Compound: 8
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Activation of GSK-3 in HEK293 cells assessed as induction in beta-catenin-LEF/TCF regulated reporter gene transcription
Activation of GSK-3 in HEK293 cells assessed as induction in beta-catenin-LEF/TCF regulated reporter gene transcription
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[PMID: 30616053] |
| MIA PaCa-2 | IC50 |
25 μM
Compound: 78, SB-216763
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Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay
Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay
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[PMID: 19338355] |
SB-216763 (10-20 μM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 μM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 μM) can maintain J1 mESCs in a pluripotent state for more than a month[2].
SB-216763 inhibits GSK-3 with IC50 of 34 nM[3].
SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 280744-09-4
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Appearance Solid
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Molecular Weight 371.22
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Formula C19H12Cl2N2O2
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Color Orange to red
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SMILES
O=C(NC1=O)C(C2=CC=C(C=C2Cl)Cl)=C1C3=CN(C4=C3C=CC=C4)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (47)
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Journal Impact Factor
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Most Recent
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Cell Res
Derivation of totipotent-like stem cells with blastocyst-like structure forming potential. [Abstract]2022 Jun;32(6):513-529. PMID: 35508506 -
Nat Commun
2022 Apr 19;13(1):2105. PMID: 35440636 -
Adv Sci (Weinh)
Hyperlipidemia Aggravates Alveolar Bone Loss via Periodontal Ligament Stem Cell Ferroptosis Through GSK3β Dependent Ubiquitin-Mediated NRF2 Degradation. [Abstract]2026 Jun;13(36):e75157. PMID: 41945797 -
Theranostics
Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]2019 Aug 12;9(20):5769-5783. PMID: 31534518 -
Haematologica
2020 Mar;105(3):661-673. PMID: 31289202 -
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Biomed Pharmacother
Pharmacological interventions on GSK3β phosphorylation-mediated tau aggregation by modulating phase separation of tau proline-rich domain. [Abstract]2025 Jun 27:189:118290. PMID: 40580878 -
Biomed Pharmacother
Dexmedetomidine prevents septic myocardial dysfunction in rats via activation of α7nAChR and PI3K/Akt- mediated autophagy. [Abstract]2019 Dec;120:109231. PMID: 31546082 -
Br J Cancer
Transcriptome analysis of newly established carboplatin-resistant ovarian cancer cell model reveals genes shared by drug resistance and drug-induced EMT. [Abstract]2023 Mar;128(7):1344-1359. PMID: 36717670 -
Cell Mol Life Sci
Dual phosphorylation of glycogen synthase kinase 3β differentially integrates metabolic programs to determine T cell immunity across vertebrates. [Abstract]2025 May 28;82(1):218. PMID: 40434714 -
Biochem Pharmacol
Lanatoside C inhibits cell proliferation and induces apoptosis through attenuating Wnt/β-catenin/c-Myc signaling pathway in human gastric cancer cell. [Abstract]2018 Apr:150:280-292. PMID: 29475060
SB 216763 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Apr:150:280-292. [Abstract]
Expression of c-Myc in MKN-45 cells treated with Lanatoside C and SB216763 at indicated concentrations for 24 h.
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Life Sci
SGK1 inhibits oxidative injury and extracellular matrix degradation by activating the GSK-3β (Ser9)/Fyn/NRF2 pathway in pelvic organ prolapse. [Abstract]2025 Aug 30:380:123939. PMID: 40889699 -
Life Sci
Arctigenin inhibits proliferation of ER-positive breast cancer cells through cell cycle arrest mediated by GSK3-dependent cyclin D1 degradation. [Abstract]2020 Sep 1;256:117983. PMID: 32565252 -
Int J Mol Sci
Inhibition of ERK1/2 or CRMP2 Disrupts Alcohol Memory Reconsolidation and Prevents Relapse in Rats. [Abstract]2024 May 17;25(10):5478. PMID: 38791516 -
Biomolecules
The Osteocyte with SB216763-Activated Canonical Wnt Signaling Constructs a Multifunctional 4D Intelligent Osteogenic Module. [Abstract]2024 Mar 15;14(3):354. PMID: 38540772 -
Front Bioeng Biotechnol
Sustained release of a highly specific GSK3β inhibitor SB216763 in the PCL scaffold creates an osteogenic niche for osteogenesis, anti-adipogenesis, and potential angiogenesis. [Abstract]2023 Jul 28:11:1215233. PMID: 37576993 -
Front Pharmacol
Number 2 Feibi Recipe Inhibits H2O2-Mediated Oxidative Stress Damage of Alveolar Epithelial Cells by Regulating the Balance of Mitophagy/Apoptosis. [Abstract]2022 Mar 17;13:830554. PMID: 35370684 -
Int Immunopharmacol
OPTN ameliorates chondrocyte apoptosis in temporomandibular joint osteoarthritis by modulating ER-mitochondria Ca2+ transfer. [Abstract]2025 May 7:157:114796. PMID: 40339496 -
Biosci Rep
The Wnt/β-catenin pathway regulates inflammation and apoptosis in ventilator-induced lung injury. [Abstract]2023 Mar 31;43(3):BSR20222429. PMID: 36825682 -
Eur J Pharmacol
GSK-3β-mediated activation of NLRP3 inflammasome leads to pyroptosis and apoptosis of rat cardiomyocytes and fibroblasts. [Abstract]2022 Apr 5;920:174830. PMID: 35182545 -
J Mol Cell Cardiol
Glycogen synthase kinase-3β inhibition alleviates activation of the NLRP3 inflammasome in myocardial infarction. [Abstract]2020 Dec;149:82-94. PMID: 32991876 -
Cancers (Basel)
Drug Repurposing Applications to Overcome Male Predominance via Targeting G2/M Checkpoint in Human Esophageal Squamous Cell Carcinoma. [Abstract]2022 Nov 28;14(23):5854. PMID: 36497337 -
Drug Dev Res
Apigenin alleviates doxorubicin-induced myocardial pyroptosis by inhibiting glycogen synthase kinase-3β in vitro and in vivo. [Abstract]2024 Jun;85(4):e22196. PMID: 38812449 -
Mol Nutr Food Res
Gallic Acid Attenuates Sepsis-Induced Liver Injury through C/EBPβ-Dependent MAPK Signaling Pathway. [Abstract]2024 May 29:e2400123. PMID: 38809052 -
iScience
2025 Dec 1;29(1):114292. PMID: 41509906 -
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Sci Rep
hUMSCs restore ovarian function in POI mice by regulating GSK3β-mediated mitochondrial dynamic imbalances in theca cells. [Abstract]2024 Aug 16;14(1):19008. PMID: 39152165 -
J Biol Chem
Upregulation of CYR61 by TGF-β and YAP signaling exerts a counter-suppression of hepatocellular carcinoma. [Abstract]2024 Apr;300(4):107208. PMID: 38521502 -
Sci Rep
2022 Nov 11;12(1):19323. PMID: 36369319 -
Cell Signal
PERK-eIF2alpha-mediated translational inhibition of MCL-1 contributes to potential 2-deoxy-D-glucose and BAD mimetic combinatorial cancer therapy. [Abstract]2025 Dec 19:139:112333. PMID: 41423011 -
Biochim Biophys Acta Mol Cell Res
Hepatocyte growth factor attenuates high glucose-disturbed mitochondrial dynamics in podocytes by decreasing ARF6-dependent DRP1 translocation. [Abstract]2023 Oct 31;1871(1):119623. PMID: 37913847 -
Toxicol Appl Pharmacol
Pristimerin suppresses colorectal cancer through inhibiting inflammatory responses and Wnt/β-catenin signaling. [Abstract]2020 Jan 1;386:114813. PMID: 31715269 -
Toxicol Appl Pharmacol
Inhibition of glycogen synthase kinase 3beta ameliorates triptolide-induced acute cardiac injury by desensitizing mitochondrial permeability transition. [Abstract]2016 Dec 15:313:195-203. PMID: 27751939
SB 216763 purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2016 Dec 15:313:195-203. [Abstract]
SB 216763 blocks augmentation of phosphor-glycogen synthase and depletion of inhibitory phosphorylated GSK-3β at serine 9 sites, but maintains total GSK-3β levels. Cardiac protection following SB 216763 is dependent on GSK-3β activity inhibition, not on decrease in basal GSK-3β levels. H9c2 cells are treated with 160 nM TP for 24 h after pretreatments with 2 μM SB 216763 or vehicle 2 h later. Levels of p-GS, p-GSK-3β, GSK-3β and GAPDH are measured by western blot.
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Mol Carcinog
BTG1 Acts as a Critical Tumor Suppressor Link Between HDAC Inhibition and β-Catenin Signaling Suppression in Diffuse Large B-Cell Lymphoma. [Abstract]2026 Jun;65(6):754-769. PMID: 41950351 -
Int J Med Sci
RIP1-dependent Apoptosis and Differentiation Regulated by Skp2 and Akt/GSK3β in Acute Myeloid Leukemia. [Abstract]2022 Mar 6;19(3):525-536. PMID: 35370472 -
Naunyn Schmiedebergs Arch Pharmacol
5-Methoxyflavone inhibits the proliferation of lung adenocarcinoma cells through PI3K/AKT/GSK3β/β-catenin/Cyclin D1 signaling and attenuates chemoresistance and PD-L1 expression. [Abstract]2025 Oct 31. PMID: 41168435 -
Mol Immunol
Luteolin attenuates type 2 inflammation in asthmatic mice induced by OVA by regulating IL-33/ST2- GSK3β-M2 macrophage polarization. [Abstract]2025 Oct:186:1-12. PMID: 40752323 -
J Cell Biochem
SB-216763, a GSK-3β inhibitor, protects against aldosterone-induced cardiac, and renal injury by activating autophagy. [Abstract]2018 Jul;119(7):5934-5943. PMID: 29600538
SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943. [Abstract]
SB-216763 activates cardiac autophagy. Cardiac protein expression of LC3-I, LC3-II, and p62 are assayed in cardiac tissues treated with Aldo-salt or with Aldo-salt plus SB-216763.
SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943. [Abstract]
SB-216763 activates cardiac autophagy. Images showing immunofluorescent staining for LC3-II for among different groups as indicated.
SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943. [Abstract]
SB-216763 activates renal autophagy. Renal protein expression of LC3-I, LC3-II and p62 are assayed in renal tissues treated with Aldo-salt or with Aldo-salt plus SB-216763. SB-216763 increased the Aldo-salt-induced autophagy.
SB 216763 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):5934-5943. [Abstract]
SB-216763 activates renal autophagy. Representative micrographs showing immunofluorescent staining for LC3-II for among different groups as indicated.
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SLAS Discov
Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ. [Abstract]2024 Nov 5;29(8):100191. PMID: 39510350 -
Theriogenology
SB216763 enhances proliferation and sustains the undifferentiated state of porcine spermatogonial cells in prolonged In vitro culture. [Abstract]2026 Apr 1:254:117816. PMID: 41518868 -
Biochem Biophys Res Commun
Involvement of MCL1, c-myc, and cyclin D2 protein degradation in ponatinib-induced cytotoxicity against T315I(+) Ph+leukemia cells. [Abstract]2020 May 14;525(4):1074-1080. PMID: 32184020 -
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Evid Based Complement Alternat Med
Calycosin Ameliorates Bleomycin-Induced Pulmonary Fibrosis via Suppressing Oxidative Stress, Apoptosis, and Enhancing Autophagy. [Abstract]2022 Oct 11:2022:9969729. PMID: 36267093 -
Evid Based Complement Alternat Med
Antimetastasis Effect of Astragalus membranaceus- Curcuma zedoaria via β-Catenin Mediated CXCR4 and EMT Signaling Pathway in HCT116. [Abstract]2019 May 30:2019:9692350. PMID: 31275425
Solvent & Solubility
DMSO : 100 mg/mL (269.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 (6.73 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 (6.73 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Protocol
MESCs maintained with LIF or 10 µM SB-216763 for more than a month are resuspended at 40,000 cells/mL in LIF-free mESC medium. EBs are prepared by a hanging drop procedure. Briefly, 20 µL drops containing mESCs are pipetted on the inside of a 10-cm Petri dish lid. The lids are placed onto Petri dishes containing 10 mL of HBSS and the EBs are allowed to form and grow for 4 days in the incubator. After 4 days, 15-20 EBs are transferred to a well containing LIF-free mESC medium in a 24-well plate. The medium is exchanged every two days and autonomously beating cell aggregates are observed and counted.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice are allocated to four groups (n=12/group) as follows: 1) intratracheal saline + vehicle (25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline), 2) intratracheal saline + SB216763 (20 mg/kg) dissolved in vehicle, 3) intratracheal BLM (3 U/kg) + vehicle, and 4) intratracheal BLM + SB216763 (20 mg/kg) in vehicle. Another set of experiments to assess cytokine expression by reverse transcription-PCR is conducted in the mice (n=12/group) to receive 1) intratracheal saline + vehicle, 2) intratracheal BLM, and 3) intratracheal BLM + SB216763. To induce pulmonary fibrosis, BLM is intratracheally administered in mice (n=15/group) on day 0. BLM and saline-treated mice are administered with SB216763 dissolved in vehicle or vehicle alone intravenously at day 0 and then intraperitoneally twice a week until day 28. Mice are sacrificed by CO2 inhalation on days 2, 7, and 28. In the terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) experiments, the cohorts of mice are as follows: saline-treated (n=6), BLM-treated (n=6), and BLM + SB216763-treated (n=6).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (288 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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Handling Instructions (2659 KB)
References
[1]. Gurrieri, et al. 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. J.Pharmacol.Exp.Ther.2010 [Content Brief]
[2]. Kirby LA, et al. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.PLoS One. 2012;7(6):e39329. Epub 2012 Jun 26. [Content Brief]
[3]. Wang M, et al. The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3).Bioorg Med Chem Lett. 2011 Jan 1;21(1):245-9. Epub 2010 Nov 11. [Content Brief]
[4]. The ceiling effect of pharmacological postconditioning with the phytoestrogen genistein is reversed by the GSK3beta inhibitor SB 216763 [3-(2,4-dichlorophenyl)-4(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione] through mitochondrial ATP-dependent potassium channel opening. [Content Brief]
[5]. 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]
[6]. Wang W, et al. Inhibition of glycogen synthase kinase 3beta ameliorates triptolide-induced acute cardiac injury by desensitizing mitochondrial permeability transition. Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6938 mL | 13.4691 mL | 26.9382 mL | 67.3455 mL |
| 5 mM | 0.5388 mL | 2.6938 mL | 5.3876 mL | 13.4691 mL | |
| 10 mM | 0.2694 mL | 1.3469 mL | 2.6938 mL | 6.7346 mL | |
| 15 mM | 0.1796 mL | 0.8979 mL | 1.7959 mL | 4.4897 mL | |
| 20 mM | 0.1347 mL | 0.6735 mL | 1.3469 mL | 3.3673 mL | |
| 25 mM | 0.1078 mL | 0.5388 mL | 1.0775 mL | 2.6938 mL | |
| 30 mM | 0.0898 mL | 0.4490 mL | 0.8979 mL | 2.2449 mL | |
| 40 mM | 0.0673 mL | 0.3367 mL | 0.6735 mL | 1.6836 mL | |
| 50 mM | 0.0539 mL | 0.2694 mL | 0.5388 mL | 1.3469 mL | |
| 60 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1224 mL | |
| 80 mM | 0.0337 mL | 0.1684 mL | 0.3367 mL | 0.8418 mL | |
| 100 mM | 0.0269 mL | 0.1347 mL | 0.2694 mL | 0.6735 mL |