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Fasudil (HA-1077) HClProtein kinase inhibitor

Fasudil (HA-1077) HCl

Catalog No. A5734
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
200mg $70.00 In stock
500mg $120.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Hu, Haiyan, et al. "Fasudil prevents calcium oxalate crystal deposit and renal fibrogenesis in glycoxylate-induced nephrolithic mice." Experimental and Molecular Pathology (2015). PMID:25697583

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Chemical structure

Fasudil (HA-1077) HCl

Related Biological Data

Fasudil (HA-1077) HCl

Related Biological Data

Fasudil (HA-1077) HCl

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Chemical Properties

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 Soluble in DMSO > 10 mM Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.