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
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 361551-1MG