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

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

Cat. No.: HY-10580 Purity: 99.47%
Handling Instructions Technical Support

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.

CAS No. : 667463-62-9

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of GSK 3 Inhibitor IX:

Top Publications Citing Use of Products

    GSK 3 Inhibitor IX purchased from MedChemExpress. Usage Cited in: JCI Insight. 2025 Nov 13:e191606.  [Abstract]

    GSK 3 Inhibitor IX (BIO) (10 mL/kg; i.p.) treatment substantially ameliorated skeletal abnormalities and augmented bone formation in Aebp1OsxCre mice at P0 and P21.

    GSK 3 Inhibitor IX purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 11;15(1):4969.  [Abstract]

    GSK 3 Inhibitor IX (10 μM; 10 h), a GSK3β inhibitor, inhibited the MYG1-induced phosphorylation of PKM2 in HCT116 cells.

    GSK 3 Inhibitor IX purchased from MedChemExpress. Usage Cited in: Chem Eng J. 19 November 2021, 133671.

    GSK 3 Inhibitor IX (BIO) (0.1-40 μg/mL; 24 h) at concentrations ranging from 0.1 to 20 μg/mL enhanced cell viability, and 10 μg/mL BIO had the maximal cytoprotective effect.

    GSK 3 Inhibitor IX purchased from MedChemExpress. Usage Cited in: NPJ Regen Med. 2021 Sep 6;6(1):51.  [Abstract]

    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) (2.0 μM) recovered the expression of Osterix and VEGF-A inhibited by YAP-1 knockdown in MSCs.

    GSK 3 Inhibitor IX purchased from MedChemExpress. Usage Cited in: NPJ Regen Med. 2021 Sep 6;6(1):51.  [Abstract]

    Treatment with GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) (2.0 μM) reduced the degradation and promoted the nuclear translocation of β-Catenin in the CSFP + YAP1-knockdown MSC.

    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. Gonads were collected from 180 dah XX fish and cultured in L15 medium with 30 μg/ml Dkk1. Cyp19a1a remained unchanged in the presence of Dkk1. Dkk1 upregulated Cyp11b2 and Dmrt1 expression, which was abolished by simultaneous treatment with GSK 3 Inhibitor IX (Bio) (15-30 μg/mL). The positive signal corresponds to the brownish color. Dkk1, antagonist of canonical Wnt/β-cat signal pathway; Bio, agonist of canonical Wnt/β-cat signal pathway.

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

    Real-time PCR analysis of cyp11b2 and dmrt1 expression in the in vitro cultured 180 dah tilapia gonad with Dkk1 (0-50 μg/mL) and with or without GSK 3 Inhibitor IX (Bio) (15-30 μg/mL). Gonads were collected from 180 dah XX fish and cultured in L15 medium with 30 μg/mL Dkk1. Dkk1 upregulated cyp11b2 and dmrt1 expression in a dose dependent manner, which was abolished by simultaneous treatment with Bio.
    • Biological Activity

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    • 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)

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    5.2 μM
    Compound: 17
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    [PMID: 19783149]
    HL-60 IC50
    5.4 μM
    Compound: 17
    Antiproliferative activity against human HL60 cells after 5 days by MTT assay
    Antiproliferative activity against human HL60 cells after 5 days by MTT assay
    [PMID: 19783149]
    HepG2 IC50
    5.3 μM
    Compound: 3b
    Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 24 hrs by alamar blue assay
    Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 24 hrs by alamar blue assay
    [PMID: 28743492]
    Huh-7 IC50
    6.2 μM
    Compound: 17
    Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay
    [PMID: 19783149]
    IMR-90 IC50
    1.9 μM
    Compound: 17
    Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
    Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
    [PMID: 19783149]
    K562 IC50
    1.3 μM
    Compound: 17
    Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
    [PMID: 19783149]
    Monocyte IC50
    0.2 μM
    Compound: 15, 6BIO
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced IL-1beta expression
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced IL-1beta expression
    [PMID: 24697244]
    Monocyte IC50
    0.5 μM
    Compound: 15, 6BIO
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced TNFalpha expression
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced TNFalpha expression
    [PMID: 24697244]
    Monocyte IC50
    1.6 μM
    Compound: 15, 6BIO
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced IL-6 expression
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced IL-6 expression
    [PMID: 24697244]
    Monocyte IC50
    > 3 μM
    Compound: 15, 6BIO
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced IL-8 expression
    Antiinflammatory activity against human monocytes assessed as reduction of LPS-induced IL-8 expression
    [PMID: 24697244]
    Oocyte IC50
    0.32 μM
    Compound: 53
    Inhibition of starfish oocyte CDK1/Cyclin B using histone H1 as substrate incubated for 10 mins in presence of [gamma-32P]ATP by scintillation counter analysis
    Inhibition of starfish oocyte CDK1/Cyclin B using histone H1 as substrate incubated for 10 mins in presence of [gamma-32P]ATP by scintillation counter analysis
    [PMID: 34161865]
    Oocyte IC50
    0.32 μM
    Compound: 6-bromoindirubin-3'-oxime
    Inhibitory activity against cyclin dependent kinase 1-cyclinB from starfish (Marthasterias glacialis) oocytes
    Inhibitory activity against cyclin dependent kinase 1-cyclinB from starfish (Marthasterias glacialis) oocytes
    [PMID: 14761195]
    SH-SY5Y EC50
    > 30 μM
    Compound: 15, 6BIO
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability
    [PMID: 24697244]
    SH-SY5Y IC50
    0.29 μM
    Compound: 6BIO
    Inhibition of GSK3-mediated beta-casein phosphorylation in human SH-SY5Y cells in presence of MG132 by Western blot analysis
    Inhibition of GSK3-mediated beta-casein phosphorylation in human SH-SY5Y cells in presence of MG132 by Western blot analysis
    [PMID: 18816110]
    SH-SY5Y IC50
    10 μM
    Compound: 6BIO
    Death of human SH-SY5Y cells in absence of 20 uM Q-VD-OPh by MTS reduction assay
    Death of human SH-SY5Y cells in absence of 20 uM Q-VD-OPh by MTS reduction assay
    [PMID: 16854069]
    SH-SY5Y IC50
    13 μM
    Compound: 6BIO
    Death of human SH-SY5Y cells in presence of 20 uM Q-VD-OPh by MTS reduction assay
    Death of human SH-SY5Y cells in presence of 20 uM Q-VD-OPh by MTS reduction assay
    [PMID: 16854069]
    SH-SY5Y IC50
    18 μM
    Compound: 6BIO
    Survival of human SH-SY5Y cells after 24 hrs by MTS reduction assay
    Survival of human SH-SY5Y cells after 24 hrs by MTS reduction assay
    [PMID: 16854069]
    SH-SY5Y IC50
    9 μM
    Compound: 6BIO
    Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS reduction assay
    Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS reduction assay
    [PMID: 18816110]
    SH-SY5Y IC50
    9.5 μM
    Compound: 6BIO
    Survival of human SH-SY5Y cells after 48 hrs by MTS reduction assay
    Survival of human SH-SY5Y cells after 48 hrs by MTS reduction assay
    [PMID: 16854069]
    Sf9 IC50
    0.014 μM
    Compound: BIO
    Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    0.041 μM
    Compound: BIO
    Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    0.27 μM
    Compound: BIO
    Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    0.45 μM
    Compound: BIO
    Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    0.527 μM
    Compound: BIO
    Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    Sf9 IC50
    3.5 μM
    Compound: BIO
    Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
    [PMID: 30234987]
    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.

    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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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.73%

    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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    • 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.

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    Product Name:
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