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.

• Sinonimo/i: GSK-3 Inhibitor X, (2ʹZ,3ʹE)-6-Bromoindirubin-3ʹ-acetoxime, BIO-Acetoxime
• Formula empirica (notazione di Hill): C₁₈H₁₂BrN₃O₃
• Numero CAS: 740841-15-0
• Peso molecolare: 398.21
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: dark purple
• Solubilità: DMSO: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: no

Primary Target
GSK-3α/β

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 10 nM against GSK-3α/β

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Carcinogenic / Teratogenic (D)

Nota sulla preparazione

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

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable