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HA-100 (hydrochloride)

HA-100 (hydrochloride)

Catalog Number:
L002373128APE
Mfr. No.:
APE-C4953
Price:
$223
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      • Overview

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          Background

          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.

      • Properties
        • Alternative Name
          C-1; 5-(1-piperazinylsulfonyl)-isoquinoline, dihydrochloride
          CAS Number
          210297-47-5
          Molecular Formula
          C13H15N3O2S·2HCl
          Molecular Weight
          350.3
          Purity
          98.00%
          Solubility
          insoluble in EtOH; ≥131.8 mg/mL in H2O; ≥19.17 mg/mL in DMSO with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

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