210297-47-5

HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC₅₀s = 8, 12, and 4 μM, respectively). It less effectively blocks the activity of myosin light chain kinase (IC₅₀ = 240 μM).

HA-100 dihydrochloride is an inhibitor of MYLK, PKA, and PKC.

PKA: 8 μM (IC₅₀); PKC: 12 μM (IC₅₀); PKC: 6.5 μM (Ki); PKG: 4 μM (IC₅₀); MLCK: 240 μM (IC₅₀); MLCK: 61 μM (Ki)

[1] hagiwara m, inagaki m, watanabe m, et al. selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives[j]. molecular pharmacology, 1987, 32(1): 7-12.
[2] krebs e g. protein kinases[j]. current topics in cellular regulation, 1972, 5: 99-133.