Fasudil hydrochloride
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Description: Inhibitor of cyclic nucleotide dependent- and Rho-kinases
Alternative Names: HA 1077
Purity: ≥98%
Biological Activity
Fasudil hydrochloride is a cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM). Fasudil suppresses MMP-2 expression and induces apoptosis in glioblastoma cells in vivo. Fasudil is a Ca2+ antagonist, vasodilator and inhibits proliferation of vascular smooth muscle cells. Fasudil binds to α-synuclein to reduce aggregate formation in cellular models of Parkinson's disease, also displays neuroprotective properties and increases survival of dopaminergic neurons in vivo.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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
The role of sphingosine kinase 1/sphingosine-1-phosphate pathway in the myogenic tone of posterior cerebral arteries.
Lim M, Choi SK, Cho YE
PLoS ONE, 2012;7(4):e35177. -
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 -
Rho-kinase inhibitor, fasudil, suppresses glioblastoma cell line progression in vitro and in vivo.
Deng et al.
Cancer Biol Ther., 2010;875:875 -
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 -
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 -
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
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Citations for Fasudil hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Fasudil hydrochloride include:
16 Citations: Showing 1 - 10
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Reprogramming normal cells into tumour precursors requires ECM stiffness and oncogenemediated changes of cell mechanical properties.
Authors: Panciera Et al.
Nat Mater 2020;19:797
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Rho-Kinase Inhibition Ameliorates Dasatinib-Induced Endothelial Dysfunction and Pulmonary Hypertension.
Authors: Fazakas Et al.
Front Physiol 2018;9:537
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Rho-Kinase Inhibition Reduces Myofibroblast Differentiation and Proliferation of Scleral Fibroblasts Induced by Transforming Growth Factor β and Experimental Glaucoma.
Authors: Pitha Et al.
Transl Vis Sci Technol 2018;7:6
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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
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A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells.
Authors: Bailey Et al.
J Biol Chem 2014;289:30443
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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
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The role of sphingosine kinase 1/sphingosine-1-phosphate pathway in the myogenic tone of posterior cerebral arteries.
Authors: Lim Et al.
PLoS One 2012;7:e35177
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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
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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
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STAT inhibit angiotensin II/Smad pathway and related vascular fibrosis, by a TGF-β-independent process.
Authors: Díez Et al.
PLoS One 2010;5:e14145
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Comparison of contractile mechanisms of sphingosylphosphorylcholine and sphingosine-1-phosphate in rabbit coronary artery.
Authors: Choi Et al.
Diabetes 2009;82:324
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Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice.
Authors: Inan and Büyükafşar
J Neurosci 2008;155:44
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Rho-associated kinase inhibitor Y-27632 promotes survival of cynomolgus monkey embryonic stem cells.
Authors: Takehara Et al.
Mol Hum Reprod 2008;14:627
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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
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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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Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle.
Authors: Wibberley Et al.
Br J Pharmacol 2003;138:757
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