Biological Activity
Cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM). Suppress MMP-2 expression and induce apoptosis in glioblastoma cells in vivo. Ca2+ antagonist and vasodilator. Also inhibits proliferation of vascular smooth muscle cells.
Compound Libraries
Fasudil hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 327.83 |
| Formula | C14H17N3O2S.HCl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 105628-07-7 |
| PubChem ID | 163751 |
| InChI Key | LFVPBERIVUNMGV-UHFFFAOYSA-N |
| Smiles | Cl.O=S(=O)(N1CCCNCC1)C1=C2C=CN=CC2=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 32.78 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 327.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.05 mL | 15.25 mL | 30.5 mL |
| 5 mM | 0.61 mL | 3.05 mL | 6.1 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.05 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Arai et al (1993) Inhibition by the protein kinase inhibitor HA-1077 of the activation of NADPH oxidase in human neutrophils. Biochem.Pharmacol. 46 1487 PMID: 8240400
Shirotani et al (1991) A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture. J.Pharmacol.Exp.Ther. 259 738 PMID: 1941621
Satoh et al (1996) Neuroprotective properties of a protein kinase inhibitor against ischaemia-induced neuronal damage in rats and gerbils. Br.J.Pharmacol. 118 1592 PMID: 8842419
Sward et al (2000) Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum. J.Physiol. 522 33 PMID: 10618150
Deng et al (2010) Rho-kinase inhibitor, fasudil, suppresses glioblastoma cell line progression in vitro and in vivo. Cancer Biol Ther. 875 875 PMID: 20364104
Keywords: Fasudil hydrochloride, supplier, inhibitors, inhibits, cyclic, nucleotide, dependent-, Rho-kinases, HA1077, HA, 1077, Rho-kinases, Protein, Kinase, A, Rho-kinases, Tocris Bioscience
