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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
If you know of a relevant reference for Fasudil hydrochloride, please let us know.
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Keywords: Fasudil hydrochloride, supplier, inhibitors, inhibits, cyclic, nucleotide, dependent-, Rho-kinases, HA1077, HA, 1077, Rho-kinases, Protein, Kinase, A, Rho-kinases, Tocris Bioscience
10 Citations for Fasudil hydrochloride
Citations are publications that use Tocris products. Selected citations for Fasudil hydrochloride include:
Akhtar et al (2013) Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction. PLoS One 8 e67813 PMID: 23826343
Wang et al (2012) Inhibition of TNF-α improves the bladder dysfunction that is associated with type 2 diabetes. BMC Ear Nose Throat Disord 61 2134 PMID: 22688336
Jeyaraj et al (2012) Cyclic AMP-Rap1A signaling activates RhoA to induce α(2c)-adrenoceptor translocation to the cell surface of microvascular smooth muscle cells. Br J Pharmacol 303 C499 PMID: 22621783
Díez et al (2010) Statins inhibit angiotensin II/Smad pathway and related vascular fibrosis, by a TGF-β-independent process. PLoS One 5 e14145 PMID: 21152444
Choi et al (2009) Comparison of contractile mechanisms of sphingosylphosphorylcholine and sphingosine-1-phosphate in rabbit coronary artery. Diabetes 82 324 PMID: 19218288
Takehara et al (2008) Rho-associated kinase inhibitor Y-27632 promotes survival of cynomolgus monkey embryonic stem cells. Mol Hum Reprod 14 627 PMID: 18940855
Inan and Büyükafşar (2008) Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. J Neurosci 155 44 PMID: 18536751
Rodríguez-Vita et al (2005) Endothelin-1, via ETA receptor and independently of transforming growth factor-β, increases the connective tissue growth factor in vascular smooth muscle cells. Cardiovasc Res 97 125 PMID: 15976312
Scherer et al (2005) Pharmacological reversal of endothelin-1 mediated constriction of the spiral modiolar artery: a potential new treatment for sudden sensorineural hearing loss. Am J Physiol Cell Physiol 5 10 PMID: 16316469
Flavahan and Flavahan (2014) The atypical structure and function of newborn arterial endothelium is mediated by Rho/Rho kinase signaling. Am J Physiol Heart Circ Physiol 307 H628 PMID: 24951756
Do you know of a great paper that uses Fasudil hydrochloride from Tocris? If so please let us know.
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