Catalog No.S7198 Synonyms: GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime
Molecular Weight(MW): 356.17
BIO 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.
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Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
PLoS One 2014 9(7), e100947. BIO purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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|Description||BIO 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.|
|Features||The first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells.|
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.  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.  BIO promotes proliferation in mammalian cardiomyocytes. 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. 
|In vivo||BIO suppresses melanoma tumor growth in a mouse xenograft model. |
Kinase assay:Kinase activities are assayed in Buffer A or C at 30°C, at a final ATP concentration of 15 μM. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated during a 10 min incubation. Controls are performed with appropriate dilutions of dimethylsulfoxide. In a few cases phosphorylation of the substrate is assessed by autoradiography after SDS-PAGE. GSK-3α/β is purified from porcine brain by affinity chromatography on immobilized axin. It is assayed, following a 1/100 dilution in 1 mg BSA/ml 10 mM DTT, with 5 μl 40 μM GS-1 peptide, a specific GSK-3 substrate, (YRRAAVPPSPSLSRHSSPHQSpEDEEE), in buffer A, in the presence of 15 μM [γ-32P] ATP (3,000 Ci/mmol; 1 mCi/ml) in a final volume of 30 μl. After 30 min incubation at 30°C, 25 μl aliquots of supernatant are spotted onto 2.5 × 3 cm pieces of Whatman P81 phosphocellulose paper, and 20 seconds later, the filters are washed five times (for at least 5 min each time) in a solution of 10 ml phosphoric acid/liter of water. The wet filters are counted in the presence of 1 ml ACS scintillation fluid.
|In vitro||DMSO||71 mg/mL (199.34 mM)|
|Ethanol||21 mg/mL (58.96 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 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.
|Synonyms||GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02753439||Not yet recruiting||Impacted Third Molar Tooth||The Baruch Padeh Medical Center, Poriya|Geistlich Pharma AG||February 2017||--|
|NCT02155764||Not yet recruiting||Tooth Extraction|Atrophy of Edentulous Alveolar Ridge||I.M. Sechenov First Moscow State Medical University|Central Scientific Research Institute of Dentistry and Maxillo-facial Surgery, Moscow, Russia|Bionova, Skolkovo Community, Russia||November 2016||Phase 2|
|NCT02736565||Not yet recruiting||Ewings Sarcoma||Strike Bio, Inc.|Gradalis, Inc.||September 2016||Phase 1|
|NCT02844270||Not yet recruiting||Heart Diseases||Shanghai Bio-heart Biological Technology Co., Ltd.||July 2016||Phase 1|
|NCT02802319||Recruiting||Alveolar Bone Loss||The University of Texas Health Science Center at San Antonio||July 2016||--|
|NCT02555072||Recruiting||Yellow Fever Vaccine|Immunity||The Immunobiological Technology Institute (Bio-Manguinhos) / Oswaldo Cruz Foundation (Fiocruz)|Ministry of Health, Brazil||July 2016||Phase 4|
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