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371958 Sigma-Aldrich

H-8, Dihydrochloride

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

Synonym: H-8, Dihydrochloride, N-[2-(Methylamino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor I

  • CAS Number 113276-94-1

  • Empirical Formula (Hill Notation) C12H15N3O2S · 2HCl

  • Molecular Weight 338.25

  •  MDL number MFCD00036962

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology, Protein Kinase A (PKA), Serine/Threonine Kinase Biology,
Quality Level   100
assay   >95% (TLC)
form   lyophilized
mfr. no.   Calbiochem®
storage condition   OK to freeze
storage conditions   +2C to +8C
solubility   water: 10 mg/mL
shipped in   ambient
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

Description

General description

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

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

Packaging

1 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Product competes with ATP.

Reversible: yes

Target Ki: 68 µM against MLCK

Warning

Toxicity: Standard Handling (A)

Preparation Note

Further dilute with aqueous buffer just prior to use.

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.

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