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

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

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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

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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