| HA-100 (hydrochloride)inhibitor of protein kinases (PKs) |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.33%
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| Cas No. | 210297-47-5 | SDF | Download SDF |
| Synonyms | C-1 | ||
| Chemical Name | 5-(1-piperazinylsulfonyl)-isoquinoline, dihydrochloride | ||
| Canonical SMILES | O=S(C1=C2C(C=NC=C2)=CC=C1)(N3CCNCC3)=O.Cl.Cl | ||
| Formula | C13H15N3O2S • 2HCl | M.Wt | 350.3 |
| Solubility | ≥131.8mg/mL in H2O | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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].
Reference:[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.
