1. PI3K/Akt/mTOR
    Stem Cell/Wnt
    Cell Cycle/DNA Damage
  2. GSK-3
    CDK

BIO (Synonyms: 6BIO; GSK 3 IX; GSK 3 Inhibitor IX; MLS 2052)

Cat. No.: HY-10580 Purity: 98.03%
Handling Instructions

BIO is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

For research use only. We do not sell to patients.

BIO Chemical Structure

BIO Chemical Structure

CAS No. : 667463-62-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 106 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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    BIO purchased from MCE. Usage Cited in: Mol Cell Endocrinol. 2016 May 15;427:33-44.

    Immunohistochemistry analyses of gene expression in the in vitro cultured tilapia ovaries obtained from 20 and 180 dah XX fish. The ovaries are cultured with or without Dkk1 and Bio.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BIO is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

    IC50 & Target[1]

    GSK-3α

    5 nM (IC50)

    GSK-3β

    5 nM (IC50)

    CDK5/p35

    80 nM (IC50)

    Cdk1/cyclin B

    320 nM (IC50)

    cdk2/cyclin A

    300 nM (IC50)

    Cdk4/cyclin D1

    10 μM (IC50)

    MAPKK

    10 μM (IC50)

    protein kinase Cα

    12 μM (IC50)

    In Vitro

    BIO 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, respectively. BIO selectively inhibits phosphorylation of STAT3 and induces apoptosis of human melanoma cells[4].

    In Vivo

    BIO (50 mg/kg, p.o.) suppresses melanoma tumor growth in a mouse xenograft model[4].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.8076 mL 14.0382 mL 28.0765 mL
    5 mM 0.5615 mL 2.8076 mL 5.6153 mL
    10 mM 0.2808 mL 1.4038 mL 2.8076 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    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, 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    COS1, Hepa (wild-type, CEM/LM AhR deficient and ELB1 ARNT deficient), or SH-SY5Y cells are grown in 6 cm culture dishes in Dulbecco's Modified Medium (DMEM) containing 10% fetal bovine serum. For treatment, IO (5 μM), BIO (5 or 10 μM), MeBIO (5 or 50 μM), LiCl (20 or 40 mM), or mock solution (DMSO, 0.5% final concentration) is added to medium when cell density reaches appr 70% confluence. After 12 (SH-SY5Y) or 24 hours, the cells, while still in plate, are lysed with lysis buffer (1% SDS, 1 mM sodium orthovanadate, 10 mM Tris [pH 7.4]). The lysate is passed several times through a 26G needle, centrifuged at 10,000× g for 5 min, and adjusted to equal protein concentration. About 8 μg of each sample is loaded for immunoblotting. Enhanced chemiluminescence is used for detection. The following primary antibodies are used: mouse anti-β-catenin CT, mouse anti-phospho-β-catenin, mouse anti-GSK-3 β, mouse anti-GSK-3 phosphoTyr216, rabbit anti-AhR (Aryl hydrocarbon receptor), and rabbit anti-actin. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    BIO is freshly prepared in 30% Solutol as 10 mg/mL.

    BALB/c mice (at 6-8 weeks old) and immunodeficient NOD/SCID/IL2Rgamma null (NSG) mice (female at 6-8 weeks old) are used in the assay. A2058 human melanoma cells at 5×106 cells in serum free medium are inoculated subcutaneously into the dorsal area of NSG mice to create xenograft model. When tumors become palpable, 6BIO or vehicle control is administered via oral gavage once daily at 50 mg/kg body weight. Tumor growth is monitored every other day. Tumor volumes are measured every 3 to 4 days. Tumor volumes are calculated using the formula: 0.5 × (larger diameter) × (small diameter)2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    356.17

    Formula

    C₁₆H₁₀BrN₃O₂

    CAS No.

    667463-62-9

    SMILES

    O/N=C(C1=CC=CC=C1N2)/C2=C3C(NC4=C/3C=CC(Br)=C4)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 23 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.03%

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    Inquiry Information

    Product Name:
    BIO
    Cat. No.:
    HY-10580
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