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Submit ReviewFasudil hydrochloride
说明： Inhibitor of cyclic nucleotide dependent- and Rho-kinases
别名： HA 1077
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for Fasudil hydrochloride
Fasudil hydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Fasudil hydrochloride
| 分子量 | 327.83 |
| 公式 | C14H17N3O2S.HCl |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Fasudil hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 32.78 | 100 | |
| DMSO | 24.59 | 75 |
制备储备液 for Fasudil hydrochloride
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Fasudil hydrochloride
参考文献 for Fasudil hydrochloride
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 Fasudil hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Fasudil hydrochloride 的部分引用包括：
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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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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