H-8 DIHYDROCHLORIDE

Description

The H series isoquinolinesulfonamide protein kinase (PK) inhibitors are widely used to block signaling pathways to elucidate mechanisms of cellular regulation and signal transduction. H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for PKC and MLCK with K_i values of 1.2, 0.48, 15, and 68 μM, respectively. H-8 can disrupt transcriptional elongation by inhibiting cyclin C/Cdk8 and cyclin H/Cdk7/p36 CTD kinase activity with IC₅₀ values of 47 and 6.2 μM, respectively.

Chemical Properties

white to off-white crystalline solid

Uses

Active inhibitor of cyclic-nucleotide-dependent protein kinases.

Biochem/physiol Actions

cAMP and cGMP-dependent protein kinase inhibitor.