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

GSK 3 Inhibitor IX (Synonyms: 6-Bromoindirubin-3'-oxime; BIO; MLS 2052)

Cat. No.: HY-10580 Purity: 99.66%
Handling Instructions

GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; 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.

GSK 3 Inhibitor IX Chemical Structure

GSK 3 Inhibitor IX Chemical Structure

CAS No. : 667463-62-9

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

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK 3 Inhibitor IX 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.
    • Biological Activity

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    • References

    • Customer Review

    Description

    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; 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

    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

    GSK 3 Inhibitor IX (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. GSK 3 Inhibitor IX 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, GSK 3 Inhibitor IX (BIO) maintains the undifferentiated phenotype and sustains expression of the pluripotent state-specific transcription factors Oct-3/4, Rex-1 and Nanog. GSK 3 Inhibitor IX (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]. GSK 3 Inhibitor IX (BIO) promotes proliferation in mammalian cardiomyocytes[3]. GSK 3 Inhibitor IX (BIO) 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. GSK 3 Inhibitor IX (BIO) selectively inhibits phosphorylation of STAT3 and induces apoptosis of human melanoma cells[4].

    In Vivo

    GSK 3 Inhibitor IX (BIO) (50 mg/kg, p.o.) suppresses melanoma tumor growth in a mouse xenograft model[4].

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 23 mg/mL (64.58 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    References
    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), GSK 3 Inhibitor IX (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]

    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, 6 GSK 3 Inhibitor IX (BIO) 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

    Purity: 99.66%

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    Keywords:

    GSK 3 Inhibitor IX6-Bromoindirubin-3'-oxime BIO MLS 2052MLS2052MLS 2052MLS-2052GSK-3ApoptosisCDKGlycogen synthase kinase-3Glycogen synthase kinase 3Cyclin dependent kinaseInhibitorinhibitorinhibit

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    Product name:
    GSK 3 Inhibitor IX
    Cat. No.:
    HY-10580
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