Home Cell Cycle ROCK inhibitor - Autophagy activator - PKA inhibitor - PKC inhibitor - MLCK inhibitor - Rho inhibitor - Calcium Channel inhibitor - PKG inhibitor Fasudil HCl For research use only.

Fasudil HCl

Synonyms: AT-877,HA-1077 HCl

Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.

Fasudil HCl Chemical Structure

Fasudil HCl Chemical Structure

CAS: 105628-07-7

Selleck's Fasudil HCl has been cited by 79 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Fasudil HCl

Celecoxib

Fasudil and Celecoxib significantly decreases COX-2 and Rho kinase II expression surrounding the lesion site in rats with spinal cord injury.

Hou XL, et al. Neural Regen Res. 2015 Nov; 10(11): 1836–1840.

Ozagrel sodium

Fasudil HCl and Ozagrel sodium have superior effectiveness over only ozagrel sodium in treating patients at risk of vasospasm after aneurysmal subarachnoid hemorrhage.

Nakashima S, et al. Neurol Med Chir (Tokyo). 1998 Dec;38(12):805-10; discussion 810-1.

Sildenafil

Fasudil and Sildenafil combination therapy inhibits monocrotaline (MCT)-induced Rho-kinase activation in rats and significantly increases the eNOS expression in the lung tissue.

Mamun MEA, et al. Circ J. 2014;78(4):967-76.

Methylcobalamin

Fasudil and Methylcobalamin combination therapy improves neuropathic symptoms and nerve conduction velocity in patients with diabetic peripheral neuropathy (DPN).

Jiang DQ, et al. Medicine (Baltimore). 2018 Jul; 97(27): e11390.

Rosuvastatin calcium

Fasudil and Rosuvastatin combination treatment significantly decreases infarct size and percentage of apoptosis and increases the content of NO and eNOS expression in an isolated rat heart model.

Wu N, et al. Pharmazie. 2014 Sep;69(9):704-8.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U937 cells Function assay Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2, IC50=35 μM. 17084087
Sf9 cells Function assay Inhibition of His-tagged human MSK1 expressed in Sf9 cells, IC50=5 μM. 10998351
HEK293 cells Function assay Inhibition of His-tagged human PRK2 expressed in HEK293 cells, IC50=4 μM. 10998351
Sf9 cells Function assay Inhibition of rat ROCK2 expressed in Sf9 cells, IC50=1.9 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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Targets
Rho [1] Calcium channel [2] ROCK2 [1]
(Cell-free assay)		 PKA [1]
(Cell-free assay)		 PKG [1]
(Cell-free assay)		 Click to View More Targets
330 nM(Ki) 1.6 μM(Ki) 1.6 μM(Ki)
In vitro
In vitro

Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. [2]

Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. [3]

Fasudil induces disorganization of actin stress fiber and cell migration inhibition. [4]

Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. [5]
Kinase Assay Cyclic AMP-dependent protein kinase activity assay
Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30 ℃ for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter.
Experimental Result Images Methods Biomarkers Images PMID
Western blot ROCK2 / p-ROCK2 / MLC2 / p-MLC2 ABCG2 Moesin / p-Moesin / β-catenin / p-β-catenin 29416017
Immunofluorescence p-ROCK2 / ABCG2 29416017
Growth inhibition assay Cell viability 29262624
In Vivo
In vivo

Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. [3]

Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. [6]

The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice. [7]
Animal Research Animal Models Mongrel dogs
Dosages 0.01, 0.03, 0.1 and 0.3 mg/kg
Administration i.v.

Chemical lnformation & Solubility

Molecular Weight 327.83 Formula

C14H17N3O2S.HCl
CAS No. 105628-07-7 SDF Download Fasudil HCl SDF
Smiles C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 65 mg/mL

DMSO : 57 mg/mL ( (173.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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