hh Fasudil hydrochloride (CAS 105628-07-7): R&D Systems
Catalog Number: 0541
Alternate Names: HA 1077
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.
Technical Data
  • M.Wt:
    327.83
  • Formula:
    C14H17N3O2S.HCl
  • Solubility:
    Soluble to 100 mM in water and to 75 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    105628-07-7
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.
Background References
  1. A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture.
    Shirotani et al.
    J.Pharmacol.Exp.Ther., 1991;259:738
  2. Neuroprotective properties of a protein kinase inhibitor against ischaemia-induced neuronal damage in rats and gerbils.
    Satoh et al.
    Br.J.Pharmacol., 1996;118:1592
  3. Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum.
    Sward et al.
    J.Physiol., 2000;522:33
  4. Inhibition by the protein kinase inhibitor HA-1077 of the activation of NADPH oxidase in human neutrophils.
    Arai et al.
    Biochem.Pharmacol., 1993;46:1487
  5. Rho-kinase inhibitor, fasudil, suppresses glioblastoma cell line progression in vitro and in vivo.
    Deng et al.
    Cancer Biol Ther., 2010;875:875
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Fasudil hydrochloride include:

10 Citations: Showing 1 - 10
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  1. The atypical structure and function of newborn arterial endothelium is mediated by Rho/Rho kinase signaling.
    Authors: Flavahan and Flavahan
    Am J Physiol Heart Circ Physiol 2014;307:H628
  2. Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction.
    Authors: Akhtar Et al.
    PLoS One 2013;8:e67813
  3. Inhibition of TNF-α improves the bladder dysfunction that is associated with type 2 diabetes.
    Authors: Wang Et al.
    BMC Ear Nose Throat Disord 2012;61:2134
  4. Cyclic AMP-Rap1A signaling activates RhoA to induce α(2c)-adrenoceptor translocation to the cell surface of microvascular smooth muscle cells.
    Authors: Jeyaraj Et al.
    Br J Pharmacol 2012;303:C499
  5. Statins inhibit angiotensin II/Smad pathway and related vascular fibrosis, by a TGF-β-independent process.
    Authors: Díez Et al.
    PLoS One 2010;5:e14145
  6. Comparison of contractile mechanisms of sphingosylphosphorylcholine and sphingosine-1-phosphate in rabbit coronary artery.
    Authors: Choi Et al.
    Diabetes 2009;82:324
  7. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice.
    Authors: Inan and Büyükafşar
    J Neurosci 2008;155:44
  8. Rho-associated kinase inhibitor Y-27632 promotes survival of cynomolgus monkey embryonic stem cells.
    Authors: Takehara Et al.
    Mol Hum Reprod 2008;14:627
  9. Endothelin-1, via ETA receptor and independently of transforming growth factor-β, increases the connective tissue growth factor in vascular smooth muscle cells.
    Authors: Rodríguez-Vita Et al.
    Cardiovasc Res 2005;97:125
  10. Pharmacological reversal of endothelin-1 mediated constriction of the spiral modiolar artery: a potential new treatment for sudden sensorineural hearing loss.
    Authors: Scherer Et al.
    Am J Physiol Cell Physiol 2005;5:10

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