General description
A broad-based, cell-permeable, reversible, ATP-competitive serine-threonine kinase inhibitor. Potent inhibitor of myosin light chain kinase (Ki = 97 µM), protein kinase A (Ki = 3.0 µM), protein kinase C (Ki = 6 µM), and protein kinase G (Ki = 5.8 µM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Also inhibits telomerase activity in quercetin-, H-89-, or herbimycin A-treated NPC-076 cells.
A broad-based, cell-permeable, reversible, ATP-competitive serine/threonine kinase inhibitor. Inhibits protein kinase A (Ki = 3.0 µM), myosin light chain kinase (Ki = 97 µM), protein kinase C (Ki = 6.0 µM), and protein kinase G (Ki = 5.8 µM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Also inhibits telomerase activity in quercetin-, H-89-, or herbimycin A-treated NPC-076 cells.
Biochem/physiol Actions
Primary Target
MLCK
Target Ki: 3.0 µM, 97 µM, 6.0 µM, 5.8 µM against protein kinase A , myosin light chain kinase, protein kinase C , and protein kinase G, respectively
Warning
Toxicity: Standard Handling (A)
Preparation Note
Further dilute with aqueous buffers just prior to use.
Reconstitution
Following reconstitution, store in the refrigerator (4°C). Aqueous stock solutions are stable for up to 6 months at 4°C.
Other Notes
Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730.
Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Bergstrand, H., et al. 1992. J. Pharmacol. Exp. Therap.263, 1334.
Gimond, C., et al. 1992. Exp. Cell Res.203, 365.
Quick, J., et al. 1992. Biochem. Biophys. Res. Commun.187, 657.
Bouli, N.M., and Davis, M. 1990. Brain Res.525, 198.
Takahashi, I., et al. 1990. J. Pharmacol. Exp. Ther.255, 1218.
Schachtele, C., et al. 1988. Biochem. Biophys.Res. Commun.151, 542.
Kawamoto, S., and Hidaka, H. 1984. Biochem. Biophys. Res. Commun.125, 258.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51112704
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 371955-1MG
- CAS:
- 108930-17-2
