Fasudil (HA-1077) HCl |
| Katalog-Nr.GC14289 |
Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μ ;M, 1.650 μM fÜr ROCK2 bzw. PKA, PKC, PKG. Fasudil (HA-1077) HCl ist auch ein potenter Ca2+-Kanal-Antagonist und Vasodilatator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 105628-07-7
Sample solution is provided at 25 µL, 10mM.
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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.
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