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Submit ReviewFasudil hydrochloride
Description: Inhibitor of cyclic nucleotide dependent- and Rho-kinases
Alternative Names: HA 1077
Purity: ≥98% (HPLC)
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 |
| 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 Data for Fasudil hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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
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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:
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
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
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
Inan and Büyükafşar (2008) Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. J Neurosci 155 44 PMID: 18536751
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
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
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
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
Choi et al (2009) Comparison of contractile mechanisms of sphingosylphosphorylcholine and sphingosine-1-phosphate in rabbit coronary artery. Diabetes 82 324 PMID: 19218288
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
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
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
Fazakas et al (2018) Rho-Kinase Inhibition Ameliorates Dasatinib-Induced Endothelial Dysfunction and Pulmonary Hypertension. Front Physiol 9 537 PMID: 29867576
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
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Stem cells have potential as a source of cells and tissues for research and treatment of disease. This poster summarizes some key protocols demonstrating the use of small molecules across the stem cell workflow, from reprogramming, through self-renewal, storage and differentiation to verification. Advantages of using small molecules are also highlighted.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.