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Merck
CN

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

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About This Item

Empirical Formula (Hill Notation):
C14H17N3O2S · 2HCl
CAS Number:
108930-17-2
Molecular Weight:
364.29
UNSPSC Code:
12352200
MDL number:
MFCD00036961

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SMILES string

[S](=O)(=O)(N3C(CNCC3)C)c1c2c(cncc2)ccc1.[Cl-].[Cl-].[H+].[H+]

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

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

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.

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

Preparation Note

Following reconstitution, store in the refrigerator (4°C). Aqueous stock solutions are stable for up to 6 months at 4°C.
Further dilute with aqueous buffers just prior to use.

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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