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Fasudil(HA-1077)HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fasudil(HA-1077)HCl图片
CAS NO:105628-07-7
规格:98%
分子量:327.83
包装与价格:
包装价格(元)
200mg电议
500mg电议

产品介绍
Protein kinase inhibitor
CAS:105628-07-7
分子式:C14H17N3O2S.HCl
分子量:327.83
纯度:98%
存储:Store at -20°C

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].


参考文献:
[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.