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GSK 3 Inhibitor IX

Catalog No. T1917 CAS 667463-62-9

Synonyms: BIO, GSK 3 IX, 6-BIO, 6-Bromoindirubin-3'-oxime, MLS 2052, 6-bromoindirubin-3-oxime

GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.

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GSK 3 Inhibitor IX, CAS 667463-62-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 75.00
10 mg	In stock	$ 103.00
25 mg	In stock	$ 240.00
50 mg	In stock	$ 433.00
100 mg	In stock	$ 642.00
500 mg	In stock	$ 1,370.00
1 mL * 10 mM (in DMSO)	In stock	$ 83.00

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Purity: 99.9%

Purity: 99.34%

Purity: 99.25%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.
Targets&IC50	CDK5-p35:0.08 μM, TYK2:30 nM, CDK2-CyclinA:0.30 μM, CDK1-CyclinB:0.32 μM, GSK-3:5 nM
In vitro	BIO inhibits the growth of melanoma in murine xenograft models.
In vivo	BIO is a pan-JAK inhibitor targeting TYK2, JAK1, JAK2, and JAK3 with IC50 values of 0.03, 1.5, 8.0, and 0.5 μM, respectively. It also acts as a specific inhibitor of glycogen synthase kinase-3 (GSK-3), with an IC50 of 5 nM for GSK-3α/β, demonstrating over 16-fold higher selectivity than for CDK5. BIO interacts with the ATP-binding pockets of these kinases, reducing phosphorylation at GSK-3 specific sites on β-catenin in cell models and promoting the proliferation of mammalian cardiomyocytes. Moreover, BIO selectively inhibits STAT3 phosphorylation, inducing apoptosis in human melanoma cells. In human and mouse embryonic stem cells, BIO preserves the undifferentiated phenotype and maintains the expression of pluripotency-specific transcription factors Oct-3/4, Rex-1, and Nanog.
Kinase Assay	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.
Cell Research	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 ～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 26 g 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 (Upstate Biotechnolgies, Clone 7D8, recognizes total β-catenin), mouse anti-phospho-β-catenin (Upstate Biotechnologies, Clone 8E7, recognizes dephosphorylated β-catenin), mouse anti-GSK-3 β, mouse anti-GSK-3 phosphoTyr216, rabbit anti-AhR (Aryl hydrocarbon receptor), and rabbit anti-actin.(Only for Reference)

Synonyms	BIO, GSK 3 IX, 6-BIO, 6-Bromoindirubin-3'-oxime, MLS 2052, 6-bromoindirubin-3-oxime
Molecular Weight	356.17
Formula	C16H10BrN3O2
CAS No.	667463-62-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 71 mg/mL (199.34 mM)

Ethanol: 21 mg/mL (58.96 mM)

References and Literature

1. Meijer L, et al. Chem Biol, 2003, 10(12), 1255-1266. 2. Sato N, et al. Nat Med, 2004, 10(1), 55-63. 3. Tseng AS, et al. Chem Biol, 2006, 13(9), 957-963. 4. Liu L, et al. Cancer Res. 2011 Jun 1;71(11):3972-3279.

Citations

1. Wen J, Li X, Zhao Q X, et al. Pharmacological suppression of glycogen synthase kinase-3 reactivates HIV-1 from latency via activating Wnt/β-catenin/TCF1 axis in CD4+ T cells. Emerging microbes & infections. 2022, 11(1): 391-405 2. Wen J, Li X, Zhao Q X, et al. Pharmacological suppression of glycogen synthase kinase-3 reactivates HIV-1 from latency via activating Wnt/β-catenin/TCF1 axis in CD4+ T cells: Suppression of GSK3 reactivates HIV-1 from latency. Emerging Microbes & Infections. 2022 (just-accepted): 1-36.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Inhibitor Library Anti-Liver Cancer Compound Library Anti-Breast Cancer Compound Library Antidepressant Compound Library Bioactive Lipid Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK 3 Inhibitor IX 667463-62-9 Apoptosis Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Stem Cells Tyrosine Kinase/Adaptors GSK-3 Tyrosine Kinases CDK BIO GSK 3 IX Cyclin dependent kinase Inhibitor Glycogen synthase kinase-3 Glycogen synthase kinase 3 MLS-2052 MLS2052 6-BIO 6-Bromoindirubin-3'-oxime inhibit MLS 2052 6-bromoindirubin-3-oxime inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.