Fasudil hydrochloride

Name: Fasudil hydrochloride
Brand: Tocris Bioscience
SKU: 0541

Catalog # 0541

Citations (16)

COA / SDS

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Key Product Details

Description:	Inhibitor of cyclic nucleotide dependent- and Rho-kinases
Alternative Names:	HA 1077
Purity:	≥98% (HPLC)
Molecular Weight:	327.83

View Full Technical Details for Fasudil hydrochloride

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.

Compound Libraries

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

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

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

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 the degree 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	30.50 mL
5 mM	0.61 mL	3.05 mL	6.10 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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References

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

Pujols Chemical chaperones as novel drugs for Parkinson's Disease. Trends Mol.Med. 2020 PMID: 32277934
Deng Rho-kinase inhibitor, fasudil, suppresses glioblastoma cell line progression in vitro and in vivo. Cancer Biol Ther. 2010 PMID: 20364104
Sward Inhibition of Rho-associated kinase blocks agonist-induced Ca²⁺ sensitization of myosin phosphorylation and force in guinea-pig ileum. J.Physiol. 2000 PMID: 10618150
Satoh Neuroprotective properties of a protein kinase inhibitor against ischaemia-induced neuronal damage in rats and gerbils. Br.J.Pharmacol. 1996 PMID: 8842419
Arai Inhibition by the protein kinase inhibitor HA-1077 of the activation of NADPH oxidase in human neutrophils. Biochem.Pharmacol. 1993 PMID: 8240400
Shirotani A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture. J.Pharmacol.Exp.Ther. 1991 PMID: 1941621

Citations for Fasudil hydrochloride (16)

Showing 1 - 10 of 16 citations Showing All

View all citations for the Small Molecules and Peptides platform.

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Citations are publications that use Bio-Techne products. Selected citations for Fasudil hydrochloride include:

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
Fazakas et al. (2018) Rho-Kinase Inhibition Ameliorates Dasatinib-Induced Endothelial Dysfunction and Pulmonary Hypertension. Front Physiol. 9:537
PMID: 29867576
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
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
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
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
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
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
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
Wibberley et al. (2003) Expression and functional role of Rho-kinase in rat urinary bladder smooth muscle. Br J Pharmacol. 138:757
PMID: 12642376

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