C-1 - CAS 84468-24-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
C-1 is a protein kinase inhibitor selecitive for PKG, PKA and PKC (IC50 = 4, 8 and 12 µM, respectively) and is widely used as a ROCK inhibitor.
Brife Description:
protein kinase inhibitor, ROCK inhibitor
≥99% by HPLC
HA 100; HA100; HA-100; 5-Piperazin-1-ylsulfonylisoquinoline; 1-(5-Isoquinolinesulfonyl)piperazine
Canonical SMILES:
1.Down-regulation of endothelin-1 receptors by protein kinase C in streptozotocin diabetic rats.
Awazu M;Parker RE;Harvie BR;Ichikawa I;Kon V J Cardiovasc Pharmacol. 1991;17 Suppl 7:S500-2.
The vasoconstrictor response is defective in diabetes mellitus (DM). Activation of protein kinase C (PKC) is also known to prevail in diabetes mellitus, and it is thought to be secondary to abnormal diacylglycerol metabolism. To ascertain whether this PKC activation in diabetes underlies the vasomotor defect by regulating biological receptors, we studied the characteristics of the receptor for endothelin (ET), "the vasoconstrictor of injury." For this purpose, diabetes was induced in rats by intravenous streptozotocin. One to 2 weeks after streptozotocin treatment (average glucose at time of experiments: 518 mg/dl), glomeruli were isolated and assessed for ET receptor and PKC activity. ET receptor characteristics were also assessed following infusion of a specific PKC inhibitor, 1-(5-isoquinolinesulfonyl)piperazine (CI). For comparison, nondiabetic controls with and without PKC inhibitor were studied. No differences in high-affinity ET-1 receptor (ER-1) characteristics were found among the diabetic and normal rats. In contrast, receptor density for the lower-affinity receptor (ER-2) was significantly depressed in DM without changes in the equilibrium dissociation constant. Infusion of CI 20 min before glomerular harvesting did not affect the glomerular PKC activity in controls (particulate: 28.
2.Cyclosporine A-induced prostacyclin release is maintained by extracellular calcium in rat aortic endothelial cells: role of protein kinase C.
Oriji GK Prostaglandins Leukot Essent Fatty Acids. 1999 Aug;61(2):119-23.
Chronic treatment with the immunosuppressive drug Cyclosporine A (CsA) is associated with increased intracellular calcium in vascular smooth muscle cells, which may activate phospholipase A2. We used rat aortic endothelial cells to investigate the role of protein kinase C (PKC) in CsA-induced prostacyclin (PGI2) release. CsA (10(-9) M) produced a significant increase in PGI2 release. CsA-induced PGI2 release were inhibited 80-85% by 10(-9) M, and 99-100% by 10(-6) M pretreatment doses of any of three different PKC inhibitors, i.e. 1-(5-isoquinolinesulfonylmethyl)piperazine(H7), staurosporine or 1-(5-isoquinolinesulfonyl)piperazine. Pretreatment with (10(-9) M) of diltiazem (a voltage-sensitive L-type calcium channel blocker) completely inhibited both CsA-induced PGI2 release. Conversely, pretreatment with (10(-9) M) of thapsigargin (an intracellular calcium channel blocker) did not alter the action of CsA. These results strongly suggest that PKC, in association with an influx of extracellular calcium, mediates CsA-induced PGI2 release in rat aortic endothelial cells.
3.Protein adsorption and osteoblast precursor cell attachment to hydroxyapatite of different crystallinities.
Yang Y;Dennison D;Ong JL Int J Oral Maxillofac Implants. 2005 Mar-Apr;20(2):187-92.
PURPOSE: ;The effect of hydroxyapatite (HA) crystallinity on protein adsorption and osteoblast precursor cell attachment to HA was investigated.;MATERIALS AND METHODS: ;Different weight ratios of 100% crystalline HA and 100% amorphous calcium phosphate powders were mixed and pressed into disks (0.5 g) of different crystallinities--either 0% (HAO), 30% (HA30), 50% (HA50), 70% (HA70), or 100% (HA100).;RESULTS: ;X-ray diffraction indicated differences in HA crystallinities. In addition, dissolution of the HA was dependent on its crystallinity, with an increase in phosphorus dissolution as the degree of crystallinity was decreased. No significant difference in albumin adsorption and initial osteoblast precursor cell attachment was observed in the range of HA0 to HA70 surfaces. However, a significantly lower albumin adsorption and initial osteoblast precursor cell attachment were observed on HA100.;DISCUSSION: ;It was suggested that changes in ionic interactions as a result of a change in crystallinity affect the amount of calcium ion ligands readily available to electrostatically bind to proteins.;CONCLUSION: ;It was thus concluded from this study that HA crystallinity affects the amount of albumin adsorbed and initial osteoblast attachment.
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CAS 84468-24-6 C-1

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