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Formula | C19H12N2O2Cl2 |
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Molecular Weight | 371.22 | CAS No. | 280744-09-4 | |
Solubility (25°C)* | In vitro | DMSO | 23 mg/mL (61.95 mM) | |
Ethanol | 1 mg/mL (2.69 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy. | ||||
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In vitro | SB 216763 displays similar potency for GSK-3β with 96% inhibition at 10 μM while exhibiting minimal activity against 24 other protein kinases including PKBα and PDK1 with IC50 of >10 μM. SB 216763 stimulates glycogen synthesis in human liver cells with EC50 of 3.6 μM, and induces dose-dependent transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells with a maximum 2.5-fold induction at 5 μM. [1] SB 216763 protects the cerebellar granule neurones from apoptotic cell death induced by LY-294002 or potassium-deprivation in a concentration-dependent manner, with a maximal neuroprotection at 3 μM in contrast with the effect of lithium chloride at which 10 mM is required. SB 216763 at 3 μM also completely prevents death of chicken dorsal root ganglion sensory neurones induced by LY-294002 regardless of NGF. SB 216763 treatment at 5 μM markedly inhibits the GSK-3-dependent phosphorylation of neuronal-specific microtubule-associated protein tau in cerebellar granule neurones or recombinant tau in HEK293 cells, and induces increased levels of cytoplasmic β-catenin in both cells mimicking the effect of Wnt-mediated inhibition of GSK-3. [2] In pancreatic cancer cell lines including BXPC-3, MIA-PaCa2, PANC1, ASPC1, and CFPAC, SB 216763 treatment at 25-50 μM reduces cell viability in a dose-dependent manner, and leads to significant increase in apoptosis by 50% at 72 hours due to the specific down regulation of GSK-3β, while has no effect in HMEC or WI38 cell lines. [3] | ||||
In vivo | Administration of SB 216763 at 20 mg/kg significantly prevents lung inflammation and the subsequent fibrosis in bleomycin (BLM)-induced pulmonary inflammation and fibrosis model in mice by significantly blocking the production of inflammatory cytokines MCP-1 and TNF-α by macrophages, and significantly improves the survival of BLM-treated mice. SB 216763 treatment causes a significant reduction in BLM-induced alveolitis by inhibiting alveolar epithelial cell damage. [4] |
Kinase Assay:[1] |
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Cell Assay:[3] |
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Animal Study:[4] |
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Data from [Mol Cancer Ther, 2014, 13(1), 37-48]
Data from [Data independently produced by , , Cancer Res, 2018, doi:10.1158/0008-5472]
Data from [Data independently produced by , , Mol Cancer Ther, 2013, 13(2): 454-67 ]
Data from [Data independently produced by , , Am J Transl Res, 2016, 8(5):1985-97.]
Dexmedetomidine facilitates autophagic flux to promote liver regeneration by suppressing GSK3β activity in mouse partial hepatectomy [ Biomed Pharmacother, 2024, 177:117038] | PubMed: 39002441 |
Jnk1 and downstream signalling hubs regulate anxiety-like behaviours in a zebrafish larvae phenotypic screen [ Sci Rep, 2024, 14(1):11174] | PubMed: 38750129 |
Development of a live cell assay for real-time monitoring the interactions between the Hippo pathway components 14-3-3 and TAZ [ SLAS Discov, 2024, 29(8):100191] | PubMed: 39510350 |
The ribosomal protein S6 kinase alpha-1 (RPS6KA1) induces resistance to venetoclax/azacitidine in acute myeloid leukemia [ Leukemia, 2023, 37(8):1611-1625] | PubMed: 37414921 |
The ribosomal protein S6 kinase alpha-1 (RPS6KA1) induces resistance to venetoclax/azacitidine in acute myeloid leukemia [ Leukemia, 2023, 37(8):1611-1625] | PubMed: 37414921 |
Kidins220 sets the threshold for survival of neural stem cells and progenitors to sustain adult neurogenesis [ Cell Death Dis, 2023, 14(8):500] | PubMed: 37542079 |
Kidins220 sets the threshold for survival of neural stem cells and progenitors to sustain adult neurogenesis [ Cell Death Dis, 2023, 14(8):500] | PubMed: 37542079 |
The GSK3β/Mcl-1 axis is regulated by both FLT3-ITD and Axl and determines the apoptosis induction abilities of FLT3-ITD inhibitors [ Cell Death Discov, 2023, 9(1):44] | PubMed: 36739272 |
Progranulin Protects against Hyperglycemia-Induced Neuronal Dysfunction through GSK3β Signaling [ Cells, 2023, 12(13)1803] | PubMed: 37443837 |
Minichromosome maintenance 6 protects against renal fibrogenesis by regulating DUSP6-mediated ERK/GSK-3β/Snail1 signaling [ iScience, 2023, 26(10):107940] | PubMed: 37810227 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.