361551

GSK-3 Inhibitor X

The GSK-3 Inhibitor X, also referenced under CAS 740841-15-0, controls the biological activity of GSK-3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): GSK-3 Inhibitor X, (2ʹZ,3ʹE)-6-Bromoindirubin-3ʹ-acetoxime, BIO-Acetoxime
• Empirical Formula (Hill Notation): C₁₈H₁₂BrN₃O₃
• CAS Number: 740841-15-0
• Molecular Weight: 398.21
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: dark purple
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

An acetoxime analog of BIO, GSK-3 Inhibitor IX (Cat. No. 361550) that exhibits greater selectivity for GSK-3α/β (IC₅₀ = 10 nM) over Cdk5/p25, Cdk2/A and Cdk1/B (IC₅₀ = 2.4 µM, 4.3 µM and 63 µM, respectively). Weakly affects the activities of Cdk4/D1 and many other kinases (IC₅₀ ≥ 10 µM). Also acts as an aryl hydrocarbon receptor agonist in both yeast (EC₅₀ ≥ 0.1 µM) and mammalian (EC₅₀ = 0.16 µM) reporter systems.

An acetoxime analog of BIO, GSK-3 Inhibitor IX (Cat. No. 361550) that exhibits greater selectivity for GSK-3α/β (IC₅₀ = 10 nM) over Cdk5/p25, Cdk2/cyclin A, and Cdk1/cyclin B (IC₅₀ = 2.4 µM, 4.3 µM, and 63 µM, respectively). A weak inhibitor of Cdk4/cyclin D1 and many other non-related kinases (IC₅₀ ≥ 10 µM). Yields BIO (Cat. No. 361550) upon hydrolysis.

Biochem/physiol Actions

Cell permeable: no

Primary Target
GSK-3α/β

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 10 nM against GSK-3α/β

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Preparation Note

Limited solubility in aqueous buffers; serial dilutions in DMSO may be required prior to dilution in buffer.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Knockaert, M., et al. 2004. Oncogene23, 4400.
Polychronopoulos, P., et al. 2004. J. Med. Chem.47, 935.
Meijer, L., et al. 2003. Chem. Biol.10, 1255.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable