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HA-100 (hydrochloride)

Catalog No.
inhibitor of protein kinases (PKs)
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HA-100 is a dechlorinated analogue of 1-(8-chloro-5-isoquinolinesulfonyl)piperazine (HA-156). HA-100 is an inhibitor of protein kinases (PKs) including PKA, PKC, and PKG [1].

Protein kinases are enzymes that can phosphorylate other proteins. Phosphorylation of proteins usually results in a functional change of the target protein (substrate) by changing enzyme activity, cellular location, or association with other proteins. Protein kinases operate in a large number of distinct signaling pathways, especially those involved in signal transduction. Protein kinases have also existed in bacteria and plant [2].

HA-100 inhibited the activity of PKA, PKC, and PKG with the IC50 values of 8, 12, and 4 μM, respectively. It showed less activity in blocking the activity of myosin light chain kinase with the IC50 of 240 μM [1]. HA-100 markedly decreased the affinity for MLC-kinase. HA-100 did not inhibit myosin light chain phosphorylation in platelets exposed to collagen significantly [1].

[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.

Chemical Properties

StorageStore at -20°C
Cas No.210297-47-5
Solubility≥131.8mg/mL in H2O
Chemical Name5-(1-piperazinylsulfonyl)-isoquinoline, dihydrochloride
SDFDownload SDF
Canonical SMILESO=S(C1=C2C(C=NC=C2)=CC=C1)(N3CCNCC3)=O.Cl.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Chemical structure

HA-100 (hydrochloride)