371955-M

H-7, Dihydrochloride - CAS 108930-17-2 - Calbiochem

A broad-based, cell-permeable, reversible, ATP-competitive serine/threonine kinase inhibitor.

• Synonym(s): H-7, Dihydrochloride - CAS 108930-17-2 - Calbiochem, 1-(5-Isoquinolinesulfonyl)-2-methylpiperazine, 2HCl
• Empirical Formula (Hill Notation): C₁₄H₁₇N₃O₂S · 2HCl
• CAS Number: 108930-17-2
• Molecular Weight: 364.29
• MDL number: MFCD00036961
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (TLC)
• form: lyophilized solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light yellow
• solubility: water: 20 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C14H17N3O2S.2ClH/c1-11-9-16-7-8-17(11)20(18,19)14-4-2-3-12-10-15-6-5-13(12)14;;/h2-6,10-11,16H,7-9H2,1H3;2*1H
• InChI key: OARGPFMFRLLKPF-UHFFFAOYSA-N

Description

General description

A broad-based, cell-permeable, reversible, ATP-competitive serine-threonine kinase inhibitor. Potent inhibitor of myosin light chain kinase (K_i = 97 µM), protein kinase A (K_i = 3.0 µM), protein kinase C (K_i = 6 µM), and protein kinase G (K_i = 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 (K_i = 3.0 µM), myosin light chain kinase (K_i = 97 µM), protein kinase C (K_i = 6.0 µM), and protein kinase G (K_i = 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 K_i: 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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable