Fasudil Hydrochloride is the hydrochloride form of Fasudil with higher solubility. Fasudil is a selective Rock inhibitor with Ki value of 0.33μM, as well as showed inhibitory activity against Protein kinase A, Protein kinase G, Protein kinase C, MLCK with Ki values of 1.6μM, 1.6μM, 3.3μM and 36μM. Addition of 0.3-100μM Fasudil could dose-dependently inhibited Ca2+ sensitization of force in guinea-pig ileum. Treatment with fasudil significantly suppressed LCc-EC migration, which may due to its impaction on polymerization of the cytoskeletal actin filament network. Incubation with Fasudil at concentration ranging in 1-100μM in MDA-MB-231 cell colonies for 21 days could concentration-dependently inhibit the the anchorage-independent cell growth in a soft agar assay. In an orthotopic MDA-MB-231 rat model, fasudil did not suppress growth of established tumors, but could greatly reduce the incidence of tumor formation through oral administration at dose of 200 mg/kg/day or continuously in the drink at dose of ~228 mg/kg/day.
Fasudil HCl/盐酸法舒地尔 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human embryonic stem cells
10 µM
Used for removal of the inserted provirus
Stem Cell Reports. 2020 Feb 11;14(2):300-311.
mouse embryonic fibroblasts (MEFs)
10μM
30 min
Fasudil reduced the relative traction stress of Acvr1R206H/+ cells on 10kPa to levels by Acvr1+/+ cells.
J Bone Miner Res. 2019 Oct;34(10):1894-1909.
primary cultured microglia isolated from the spinal cord
41 μM
6 h
To investigate the effect of Fasudil on microglial migration, the results showed that Fasudil significantly increased the number of migrating microglia.
Neural Regen Res. 2018 Apr;13(4):677-683.
MCF10A cells
10 μM
24 h
To assess the effect of Fasudil on cell viability, results showed that Fasudil treatment did not affect cell viability.
Nat Mater. 2020 Jul;19(7):797-806.
HEL cells
30 μM
5 days
To evaluate the effects of Fasudil on IFNα-induced anti-proliferative responses, the results showed that Fasudil in combination with IFNα significantly reduced the viability of HEL cells.
Nat Commun. 2022 Apr 1;13(1):1750.
primary PBMCs from PV patients
30 μM
To evaluate the effects of Fasudil on IFNα-induced anti-clonogenic responses, the results showed that Fasudil enhanced the suppressive effects of IFNα on primitive malignant erythroid precursors from PV patients who responded poorly to IFN treatment.
Nat Commun. 2022 Apr 1;13(1):1750.
cardiomyocytes
100 μM
To investigate the effect of Fasudil on mitochondrial function in cardiomyocytes by inhibiting Rock1 expression
Fasudil administration abolished any emergence of neoplasia and blunted YAP/TAZ nuclear accumulation, correlating with normalization of cellular tension as visualized by pMLC.
Nat Mater. 2020 Jul;19(7):797-806.
Mice
KPC pancreatic cancer model
Oral
2 mg/mouse
Daily for 2 weeks
Fasudil treatment significantly reduced the invasion of KPC tumor cells into healthy pancreatic tissue, but did not affect tumor cell proliferation.
Cancer Res. 2018 Jun 15;78(12):3321-3336
Mice
Jak2V617F KI bone marrow transplantation model
Intraperitoneal injection
25 mg/kg
Four times per week for 4 weeks
To evaluate the effects of Fasudil in combination with PEG-IFNα treatment in a MPN mouse model, the results showed that Fasudil blocked PEG-IFNα-induced ROCK1/2 activation and enhanced the anti-neoplastic effects of PEG-IFNα.
Nat Commun. 2022 Apr 1;13(1):1750.
Mice
Doxorubicin-induced cardiomyopathy model
Intraperitoneal injection
10 mg/kg
Once daily for 6 days
To investigate the protective effect of Fasudil against Doxorubicin-induced cardiomyopathy by inhibiting Rock1 expression
Cell Death Dis. 2025 Jan 4;16(1):2.
Mice
MPD model
Intraperitoneal
25 mg/kg
Every 24 hours for 21 days
ROCK inhibitors significantly prolonged the survival of mice bearing KITD814V or FLT3N51 and reduced spleen and liver weights.
Cancer Cell. 2011 Sep 13;20(3):357-69
Mice
Ang II infusion model
Drinking water
30 mg/kg
Once daily for 14 days
Fasudil treatment significantly inhibited Ang II-induced VSMC migration and dedifferentiation, and increased the expression of VSMC differentiation markers.
Inhibition of His-tagged human PRK2 expressed in HEK293 cells, IC50=4 μM.
10998351
insect cells
Function assay
10 mins
Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase coupled assay, Ki=0.53 μM.
26039570
Sf9 cells
Function assay
90 mins
Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay, IC50=0.3 μM.
17018693
Sf9 cells
Function assay
Inhibition of rat ROCK2 expressed in Sf9 cells, IC50=1.9 μM.
10998351
Sf9 cells
Function assay
Inhibition of His-tagged human MSK1 expressed in Sf9 cells, IC50=5 μM.
10998351
U937 cells
Function assay
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2, IC50=35 μM.
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