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

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

Cat. No.: HY-10580 Purity: 99.74%
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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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 116 In-stock
Solution
10 mM * 1 mL in DMSO USD 116 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 106 In-stock
10 mg USD 158 In-stock
50 mg USD 594 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

GSK 3 Inhibitor IX Related Antibodies

Top Publications Citing Use of Products

    GSK 3 Inhibitor IX purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2016 May 15;427:33-44.  [Abstract]

    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.

    View All GSK-3 Isoform Specific Products:

    View All Isoforms
    GSK-3 GSK-3α GSK-3β

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • 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[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

    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].

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

    GSK 3 Inhibitor IX Related Antibodies
    In Vivo

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

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    356.17

    Formula

    C16H10BrN3O2
    CAS No.
    Appearance

    Solid

    Color

    Brown to red

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 23 mg/mL (64.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    (per animal)

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    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.74%

    COA (257 KB) LCMS (270 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8076 mL 14.0382 mL 28.0765 mL 70.1912 mL
    5 mM 0.5615 mL 2.8076 mL 5.6153 mL 14.0382 mL
    10 mM 0.2808 mL 1.4038 mL 2.8076 mL 7.0191 mL
    15 mM 0.1872 mL 0.9359 mL 1.8718 mL 4.6794 mL
    20 mM 0.1404 mL 0.7019 mL 1.4038 mL 3.5096 mL
    25 mM 0.1123 mL 0.5615 mL 1.1231 mL 2.8076 mL
    30 mM 0.0936 mL 0.4679 mL 0.9359 mL 2.3397 mL
    40 mM 0.0702 mL 0.3510 mL 0.7019 mL 1.7548 mL
    50 mM 0.0562 mL 0.2808 mL 0.5615 mL 1.4038 mL
    60 mM 0.0468 mL 0.2340 mL 0.4679 mL 1.1699 mL
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    GSK 3 Inhibitor IX Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GSK 3 Inhibitor IX667463-62-96-Bromoindirubin-3'-oxime BIO MLS 2052MLS2052MLS 2052MLS-2052GSK-3CDKApoptosisGlycogen synthase kinase-3Glycogen synthase kinase 3Cyclin dependent kinaseInhibitorinhibitorinhibit

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