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.
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
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Limited solubility in aqueous buffers; serial dilutions in DMSO may be required prior to dilution in buffer.
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
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
| Quality Segment | 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 |
