Fasudil hydrochloride

Pricing Availability   Qty
Description: Inhibitor of cyclic nucleotide dependent- and Rho-kinases
Alternative Names: HA 1077
Purity: ≥98% (HPLC)
Citations (16)
Literature (3)

Biological Activity for Fasudil hydrochloride

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.

Compound Libraries for Fasudil hydrochloride

Fasudil hydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for Fasudil hydrochloride

M. Wt 327.83
Formula C14H17N3O2S.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 105628-07-7
PubChem ID 163751
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Fasudil hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 32.78 100
DMSO 24.59 75

Preparing Stock Solutions for Fasudil hydrochloride

The following data is based on the product molecular weight 327.83. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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 for Fasudil hydrochloride

Certificate of Analysis / Product Datasheet
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References for Fasudil hydrochloride

References are publications that support the biological activity of the product.

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

Pujols et al (2020) Chemical chaperones as novel drugs for Parkinson's Disease. Trends Mol.Med. 26 408 PMID: 32277934

If you know of a relevant reference for Fasudil hydrochloride, please let us know.

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Keywords: Fasudil hydrochloride, Fasudil hydrochloride supplier, inhibitors, inhibits, cyclic, nucleotide, dependent-, Rho-kinases, HA1077, apoptosis, apoptotic, alpha-synuclein, alfa-synuclein, parkinsons, neuroprotective, dopaminergic, HA, 1077, Protein, Kinase, A, 0541, Tocris Bioscience

16 Citations for Fasudil hydrochloride

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

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

Fazakas et al (2018) Rho-Kinase Inhibition Ameliorates Dasatinib-Induced Endothelial Dysfunction and Pulmonary Hypertension. Front Physiol 9 537 PMID: 29867576

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

Díez et al (2010) STAT inhibit angiotensin II/Smad pathway and related vascular fibrosis, by a TGF-β-independent process. PLoS One 5 e14145 PMID: 21152444

Panciera et al (2020) Reprogramming normal cells into tumour precursors requires ECM stiffness and oncogenemediated changes of cell mechanical properties. Nat Mater 19 797 PMID: 32066931

Pitha et al (2018) Rho-Kinase Inhibition Reduces Myofibroblast Differentiation and Proliferation of Scleral Fibroblasts Induced by Transforming Growth Factor β and Experimental Glaucoma. Transl Vis Sci Technol 7 6 PMID: 30479877

Wibberley et al (2003) Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle. Br J Pharmacol 138 757 PMID: 12642376

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

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

Lim et al (2012) The role of sphingosine kinase 1/sphingosine-1-phosphate pathway in the myogenic tone of posterior cerebral arteries. PLoS One 7 e35177 PMID: 22532844

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

Bailey et al (2014) A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells. J Biol Chem 289 30443 PMID: 25225290

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Literature in this Area

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