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Fasudil

Catalog No. T1606   CAS 103745-39-7
Synonyms: HA-1077, AT877

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

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Fasudil Chemical Structure
Fasudil, CAS 103745-39-7
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50 mg In stock $ 33.00
100 mg In stock $ 45.00
200 mg In stock $ 62.00
500 mg In stock $ 107.00
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Biological Description
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Description Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
Targets&IC50 ROCK1:0.33 μM(Ki), PKC:9.3 μM(Ki), PKA:1.0 μM(Ki), MLCK:55 μM(Ki)
In vitro Fasudil (Hydrochloride) has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme[1]. 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].
In vivo Fasudil (30 μg) produces an approximate 50% increase in CBF via intra-coronary injection to dogs. 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].
Kinase 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°C 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[1].
Synonyms HA-1077, AT877
Molecular Weight 291.37
Formula C14H17N3O2S
CAS No. 103745-39-7

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

TargetMolReferences and Literature

1. Ono-Saito N, et al. H-series protein kinase inhibitors and potential clinical applications. Pharmacol Ther. 1999 May-Jun;82(2-3):123-31. 2. Asano T, et al. Mechanism of action of a novel antivasospasm drug, HA1077. J Pharmacol Exp Ther. 1987 Jun;241(3):1033-40. 3. Asano T, et al. Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase. Br J Pharmacol. 1989 Dec;98(4):1091-100. 4. Negoro N, et al. The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells. Biochem Biophys Res Commun. 1999 Aug 19;262(1):211-5. 5. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38.

Related compound libraries

This product is contained In the following compound libraries:
Autophagy Compound Library Ion Channel Inhibitor Library Inhibitor Library Approved Drug Library

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Keywords

Fasudil 103745-39-7 Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Membrane transporter/Ion channel Metabolism Stem Cells Tyrosine Kinase/Adaptors ROCK Serine/threonin kinase Calcium Channel PKA PKC LPA ROK Protein kinase C human HSC Inhibitor ERK1/2 AT-877 vasodilator Rho-associated kinase HA-1077 AT877 HA 1077 inhibit TIMP-1 AT 877 HA1077 protein kinases lysophoaphatidic acid JNK rat HSCs collagen Ca2+ channel antagonist TWNT-4 cells Rho-associated protein kinase orally active Rho-kinase Protein kinase A Ca channels a-SMA p38 Ca2+ channels inhibitor

 

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