- chroman 1
- Y-27632
- GSK429286A
- RKI-1447
- Y-27632 dihydrochloride
- GSK269962A
| Fasudil (HA-1077) HClProtein kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.76%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
Related Biological Data
| Cell experiment [1]: | |
Cell lines | 5637, UM-UC-3 and SCC-4 cell lines |
Preparation method | The solubility of this compound in DMSO is >16.4 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0-30 μM |
Applications | Lysophosphatidic acid and geranylgeraniol induced an increase of cell proliferation and migration in association with promotion of RhoA activity and upregulation of ROCK expression. Fasudil (HA-1077) could suppress cell proliferation and migration, and also induce apoptosis in a dose-dependent manner. Fasudil (HA-1077) also dramatically suppressed the expression of ROCK-I and ROCK-II, but did not affect RhoA activity. |
| Animal experiment [2]: | |
Animal models | Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders |
Dosage form | 100 mg/kg daily by oral gavage |
Application | In the Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders, by 2 weeks of treatment, total white cell and monocyte counts were significantly lower in mice treated with fasudil. A trend towards improved survival in fasudil-treated mice that did not reach statistical significance was also observed. Notably, prolonged survival beyond 27 weeks was seen in two fasudil-treated mice, nearly twice the 16-week average life-span in the Cbl/Cbl-b DKO MPD model. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Abe, H., et al., The Rho-kinase inhibitor HA-1077 suppresses proliferation/migration and induces apoptosis of urothelial cancer cells. BMC Cancer, 2014. 14: p. 412. [2] William, B.M., et al., Fasudil, a clinically safe ROCK inhibitor, decreases disease burden in a Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders. Hematology, 2015. | |
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| Cas No. | 105628-07-7 | SDF | Download SDF |
| Chemical Name | 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrochloride | ||
| Canonical SMILES | C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl | ||
| Formula | C14H17N3O2S.HCl | M.Wt | 327.83 |
| Solubility | ≥16.4mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Fasudil (HA-1077) HCl is a selective inhibitor of ROCK with IC50 value of 0.74 μM [1].
Rho-associated protein kinase (ROCK) belongs to the AGC family of serine-threonine kinases and plays a pivotal role in regulating a variety of cellular processes. It has been reported that abnormal expression of ROCK is correlated with numerous diseases and infections [2].
Fasudil (HA-1077) HCl is a potent ROCK inhibitor and has a different structure with the reported ROCK inhibitor Y-27632. When tested with 2 human bladder cancer cell lines (5637 and UM-UC-3), Fasudil (HA-1077) HCl treatment inhibits cell proliferation, decreases cell migration and induced cell apoptosis in a dose dependent manner via blocking Rho/ROCK pathway [3]. In oral squmous cell carcinoma SCC-4 cells, administration of Fasudil (HA-1077) HCl markedly decreases cell motility and inhibits cell migration or invasion in a dose dependent manner (1, 50 and 100 μmol/L [4].
In the Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders, oral administration of Fasudil (HA-1077) HCl (100 mg/kg, daily) markedly increases the total white cell and monocyte numbers while prolonged survival time has trend but no statistical difference compared with the control group [2].
References: [1].Wickman, G., C. Lan, and B. Vollrath, Functional roles of the rho/rho kinase pathway and protein kinase C in the regulation of cerebrovascular constriction mediated by hemoglobin: relevance to subarachnoid hemorrhage and vasospasm. Circ Res, 2003. 92(7): p. 809-16.[2].William, B.M., et al., Fasudil, a clinically safe ROCK inhibitor, decreases disease burden in a Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders. Hematology, 2015.[3].Abe, H., et al., The Rho-kinase inhibitor HA-1077 suppresses proliferation/migration and induces apoptosis of urothelial cancer cells. BMC Cancer, 2014. 14: p. 412. [4].Moreira Carboni, S.S., et al., HA-1077 inhibits cell migration/invasion of oral squamous cell carcinoma. Anticancer Drugs, 2015.
