General description
A cell-permeable, reversible, substrate competitive and potent p56lck tyrosine kinase inhibitor (IC50 = 18.5 µM). Selectively blocks the growth of v-ras transformed human bronchial epithelial cells (IC50 = 14.8 µM) without affecting normal human bronchial epithelial cells, even at a concentration of 370 mM. Reported to act as an inhibitor of Tau aggregation and aid in the disassembly of PHF in vitro and in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
p56lck tyrosine kinase
Product does not compete with ATP.
Reversible: yes
Target IC50: 18.5 µM against p56lck tyrosine kinase
Preparation Note
Following reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 3 months at -20°C. Unstable in aqueous alkali; reconstitute just prior to use.
Other Notes
Pickhardt, M., et al. 2004. J. Biol. Chem.280, 3628.
Zhang, L., and Hung. M.C. 1996. Oncogene 12, 571.
Chan, T.C., et al. 1993. Biochem. Biophys. Res. Commun. 193, 1152.
Jayasuriya, H., et al. 1992. J. Nat. Prod.55, 696.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| description | Merck USA index - 14, 3561 |
| assay | ≥90% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze |
| color | orange |
| solubility | DMSO: 1 mg/mL,aqueous base: soluble,ethanol: soluble |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | Oc1c2c(cc(c1)O)C(=O)c3c(c(cc(c3)C)O)C2=O |
| InChI | 1S/C15H10O5/c1-6-2-8-12(10(17)3-6)15(20)13-9(14(8)19)4-7(16)5-11(13)18/h2-5,16-18H,1H3 |
| InChI key | RHMXXJGYXNZAPX-UHFFFAOYSA-N |
