Fasudil hydrochloride

Cat. No. 0541

Fasudil hydrochloride C14H17N3O2S.HCl [105628-07-7]

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Alternative Name: 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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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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.

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.

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Fasudil hydrochloride include:

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.

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.

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.

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.

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.

Inan and Büyükafşar (2008) Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. J Neurosci 155 44. PMID: 18536751.

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.

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.

Do you know of a great paper that uses Fasudil hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: Fasudil hydrochloride, supplier, inhibitors, inhibits, cyclic, nucleotide, dependent-, Rho-kinases, HA1077, Tocris Bioscience, Rho-Kinases Inhibitor products

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