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

Name: GSK 3 Inhibitor IX
Brand: MedChemExpress
SKU: HY-10580
Rating: 5.0 (12 reviews)

Cat. No.: HY-10580 Purity: 99.74%: FAQs
Data Sheet SDS COA Handling Instructions

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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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 116	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 594	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 12 publication(s) in Google Scholar

11 Publications Citing Use of MCE GSK 3 Inhibitor IX

IHC

: 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.

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Description

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.

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.

667463-62-9

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
10 mM	0.2808 mL	1.4038 mL	2.8076 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (257 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

References

[1]. Meijer L, et al. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol. 2003 Dec;10(12):1255-66. [Content Brief]

[2]. Sato N, et al. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nat Med. 2004 Jan;10(1):55-63. Epub 2003 Dec 21. [Content Brief]

[3]. Tseng AS, et al. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem Biol. 2006 Sep;13(9):957-63. [Content Brief]

[4]. Liu L1, et al. 6-Bromoindirubin-3'-oxime inhibits JAK/STAT3 signaling and induces apoptosis of human melanoma cells. Cancer Res. 2011 Jun 1;71(11):3972-9 [Content Brief]

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	[1]. Meijer L, et al. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol. 2003 Dec;10(12):1255-66. [Content Brief] [2]. Sato N, et al. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nat Med. 2004 Jan;10(1):55-63. Epub 2003 Dec 21. [Content Brief] [3]. Tseng AS, et al. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem Biol. 2006 Sep;13(9):957-63. [Content Brief] [4]. Liu L1, et al. 6-Bromoindirubin-3'-oxime inhibits JAK/STAT3 signaling and induces apoptosis of human melanoma cells. Cancer Res. 2011 Jun 1;71(11):3972-9 [Content Brief]

Complete Stock Solution Preparation Table

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

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

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GSK 3 Inhibitor IX Related Antibodies

11 Publications Citing Use of MCE GSK 3 Inhibitor IX

Featured Recommendations

•Related Screening Libraries:

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View All GSK-3 Isoform Specific Products:

View All CDK Isoform Specific Products:

Biological Activity

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Purity & Documentation

References

Customer Review

GSK 3 Inhibitor IX Related Antibodies

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Complete Stock Solution Preparation Table

GSK 3 Inhibitor IX Related Classifications

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