一般描述
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.
生化/生理作用
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
警告
Toxicity: Standard Handling (A)
制备说明
Further dilute with aqueous buffers just prior to use.
重悬
Following reconstitution, store in the refrigerator (4°C). Aqueous stock solutions are stable for up to 6 months at 4°C.
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany