Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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S129716-5mg | 5mg | In stock | $64.90 | |
S129716-10mg | 10mg | In stock | $90.90 | |
S129716-25mg | 25mg | In stock | $204.90 | |
S129716-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $273.90 | |
S129716-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $469.90 |
Potent selective GSK3 inhibitor
Synonyms | FT-0688716 | B5716 | CHEBI:91421 | GTPL8015 | Lopac-S-3442 | Q4918914 | Z2065671802 | 3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione;SB-216763 | C19H12Cl2N2O2 | CCG-101287 | SDCCGSBI-0050908.P002 | NCGC00015949-01 | NCGC00025232-02 | LP009 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | SB 216763 is potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (Ki = 9 nM for GSK-3α); competes with ATP. SB 216763 has minimal activity against 24 other protein kinases (IC50 > 10 μ M). Stimulates glycogen synthesis, gene tran |
Legal Information | Sold for only research purposes |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of glycogen synthase kinase 3 alpha;Inhibitor of glycogen synthase kinase 3 beta |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | SB 216763 SB-216763 was used to inhibit GSK-3β in human brain microvascular endothelial cell line and colorectal cancer cells. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione |
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INCHI | InChI=1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25) |
InChi Key | JCSGFHVFHSKIJH-UHFFFAOYSA-N |
Canonical SMILES | CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl |
Isomeric SMILES | CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl |
WGK Germany | 3 |
PubChem CID | 176158 |
Molecular Weight | 371.22 |
PubChem CID | 176158 |
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CAS Registry No. | 280744-09-4 |
ChEMBL Ligand | CHEMBL102714 |
Reactome Reaction | R-HSA-9687724 |
Reactome Drug | R-ALL-9687662 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
C2212051 | Certificate of Analysis | Dec 20, 2023 | S129716 |
C2212092 | Certificate of Analysis | Dec 20, 2023 | S129716 |
C2212107 | Certificate of Analysis | Dec 20, 2023 | S129716 |
C2214293 | Certificate of Analysis | Dec 20, 2023 | S129716 |
C2214083 | Certificate of Analysis | Feb 17, 2022 | S129716 |
Solubility | DMSO 23 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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Sensitivity | Heat Sensitive |
Melt Point(°C) | 104 °C |
Pictogram(s) | GHS07 |
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Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
WGK Germany | 3 |
1. Eldar-Finkelman H, Schreyer SA, Shinohara MM, LeBoeuf RC, Krebs EG. (1999) Increased glycogen synthase kinase-3 activity in diabetes- and obesity-prone C57BL/6J mice.. Diabetes, 48 (8): (1662-6). [PMID:10426388] [10.1021/op500134e] |
2. Nikoulina SE, Ciaraldi TP, Mudaliar S, Mohideen P, Carter L, Henry RR. (2000) Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes.. Diabetes, 49 (2): (263-71). [PMID:10868943] [10.1021/op500134e] |
3. Coghlan MP, Culbert AA, Cross DA, Corcoran SL, Yates JW, Pearce NJ, Rausch OL, Murphy GJ, Carter PS, Roxbee Cox L et al.. (2000) Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.. Chem Biol, 7 (10): (793-803). [PMID:11033082] [10.1021/op500134e] |
4. Cai Z, Zhao Y, Zhao B. (2012) Roles of glycogen synthase kinase 3 in Alzheimer's disease.. Curr Alzheimer Res, 9 (7): (864-79). [PMID:22272620] [10.1021/op500134e] |
5. Hurtado DE, Molina-Porcel L, Carroll JC, Macdonald C, Aboagye AK, Trojanowski JQ, Lee VM. (2012) Selectively silencing GSK-3 isoforms reduces plaques and tangles in mouse models of Alzheimer's disease.. J Neurosci, 32 (21): (7392-402). [PMID:22623685] [10.1021/op500134e] |
6. Takashima A, Noguchi K, Sato K, Hoshino T, Imahori K. (1993) Tau protein kinase I is essential for amyloid beta-protein-induced neurotoxicity.. Proc Natl Acad Sci USA, 90 (16): (7789-93). [PMID:8356085] [10.1021/op500134e] |
7. Dey D et al.. (2022) Diffusion of small molecule drugs is affected by surface interactions and crowder proteins.. iScience, 25 (10): (105088). [PMID:36157590] |
8. Collu GM et al.. (2012) Dishevelled limits Notch signalling through inhibition of CSL.. Development, 139 (23): (4405-15). [PMID:23132247] |
9. Cao S et al.. (2022) Effects of cGMP/Akt/GSK-3β signaling pathway on atrial natriuretic peptide secretion in rabbits with rapid atrial pacing.. Front Physiol, 13 (861981). [PMID:36060704] |
10. Ahmed T et al.. (2015) Rescue of impaired late-phase long-term depression in a tau transgenic mouse model.. Neurobiol Aging, 36 (2): (730-9). [PMID:25443285] |
11. Foertsch F et al.. (2013) S100A11 is involved in the regulation of the stability of cell cycle regulator p21(CIP1/WAF1) in human keratinocyte HaCaT cells.. FEBS J, 280 (16): (3840-53). [PMID:23745637] |
12. Zhang Y et al.. (2016) The anti-hyperglycemic efficacy of a lipid-lowering drug Daming capsule and the underlying signaling mechanisms in a rat model of diabetes mellitus.. Sci Rep, 6 (34284). [PMID:27721485] |
13. Macdougall CE et al.. (2018) Visceral Adipose Tissue Immune Homeostasis Is Regulated by the Crosstalk between Adipocytes and Dendritic Cell Subsets.. Cell Metab, 27 (3): (588-601.e4). [PMID:29514067] |