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Formula | C16H10BrN3O2 |
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Molecular Weight | 356.17 | CAS No. | 667463-62-9 | |
Solubility (25°C)* | In vitro | DMSO | 71 mg/mL (199.34 mM) | |
Ethanol | 21 mg/mL (58.96 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 | BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells. | |||||||||||
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Targets |
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In vitro | BIO (6-bromoindirubin-3'-oxime) is a specific inhibitor of glycogen synthase kinase-3 (GSK-3), with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5. BIO interacts within the ATP binding pocket of these kinases, reduces β-catenin phosphorylation on a GSK-3-specific site in cellular models, closely mimicks Wnt signaling in Xenopus embryos. [1] In human and mouse embryonic stem cells, BIO maintains the undifferentiated phenotype and sustains expression of the pluripotent state-specific transcription factors Oct-3/4, Rex-1 and Nanog. BIO-mediated Wnt activation is functionally reversible, as withdrawal of the compound leads to normal multidifferentiation programs in both human and mouse embryonic stem cells. [2] BIO promotes proliferation in mammalian cardiomyocytes. [3]6BIO is also a pan-JAK inhibitor, with IC50 values of 0.03, 1.5, 8.0, 0.5 μM for TYK2, JAK1, JAK2 and JAK3. BIO selectively inhibits phosphorylation of STAT3 and induces apoptosis of human melanoma cells. [4] | |||||||||||
In vivo | BIO suppresses melanoma tumor growth in a mouse xenograft model. [4] | |||||||||||
Features | The first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells. |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Animal Study:[4] |
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Data from [Data independently produced by PLoS One, 2014, 9(7), e100947]
Data from [Data independently produced by , , Int J Oncol, 2017, 50(1):101-110]
Extraembryonic mesoderm cells derived from human embryonic stem cells rely on Wnt pathway activation [ Cell Prolif, 2024, 10.1111/cpr.13761] | PubMed: 39385268 |
CDKAL1 Drives the Maintenance of Cancer Stem-Like Cells by Assembling the eIF4F Translation Initiation Complex [ Adv Sci (Weinh), 2023, 10(12):e2206542] | PubMed: 36786012 |
Upregulation of β-catenin signaling represents a single common pathway leading to the various phenotypes of spinal degeneration and pain [ Bone Res, 2023, 11(1):18] | PubMed: 37059724 |
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530] | PubMed: 37543570 |
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530] | PubMed: 37543570 |
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] | PubMed: 35051357 |
Neddylation is essential for β-catenin degradation in Wnt signaling pathway [ Cell Rep, 2022, 38(12):110538] | PubMed: 35320710 |
Yes-associated protein activation potentiates glycogen synthase kinase-3 inhibitor-induced proliferation of neonatal cardiomyocytes and iPS cell-derived cardiomyocytes [ J Cell Physiol, 2022, 10.1002/jcp.30724] | PubMed: 35312066 |
BAP31 Regulates Wnt Signaling to Modulate Cell Migration in Lung Cancer [ Front Oncol, 2022, 12:859195] | PubMed: 35359416 |
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
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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.
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