371958

H-8, Dihydrochloride

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of cyclic-nucleotide-dependent protein kinases.

• Synonym(s): H-8, Dihydrochloride, N-[2-(Methylamino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor I
• Empirical Formula (Hill Notation): C₁₂H₁₅N₃O₂S · 2HCl
• CAS Number: 113276-94-1
• Molecular Weight: 338.25
• UNSPSC Code: 12352200
• MDL number: MFCD00036962

Properties

• Product Name: H-8, Dihydrochloride, A potent, cell-permeable, reversible, and ATP-competitive inhibitor of cyclic-nucleotide-dependent protein kinases.
• InChI: 1S/C12H15N3O2S.2ClH/c1-13-7-8-15-18(16,17)12-4-2-3-10-9-14-6-5-11(10)12;;/h2-6,9,13,15H,7-8H2,1H3;2*1H
• InChI key: RJJLZYZEVNCZIW-UHFFFAOYSA-N
• assay: >95% (TLC)
• form: lyophilized
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• solubility: water: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• Quality Level: 100

Description

Biochem/physiol Actions

Cell permeable: yes

Product competes with ATP.

Reversible: yes

Target K_i: 68 µM against MLCK

Disclaimer

Toxicity: Standard Handling (A)

General description

A potent, cell-permeable, reversible, and ATP-competitive, and highly active inhibitor of cyclic-nucleotide-dependent protein kinases. Inhibits myosin light chain kinase (K_i = 68 µM), protein kinase A (K_i = 1.2 µM), protein kinase C (K_i = 15 µM), and protein kinase G (K_i = 480 nM).

Other Notes

Ido, M., et al. 1991. Br. J. Cancer 64, 1103.
Hagiwara, M., et al. 1987. Mol. Pharmacol. 31, 523.
Inagaki, M., et al. 1986. Mol. Pharmacol.29, 577.
Hidaka, H., et al. 1984. Biochemistry23, 5036.

Preparation Note

Further dilute with aqueous buffer just prior to use.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

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