| Name | Fasudil hydrochloride |
| Description | Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. |
| 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. |
| In vitro | Intravenous injections of Fasudil at doses of 0.01, 0.03, 0.1, and 0.3 mg/kg decreased mean blood pressure (MBP) and increased heart rate (HR), vertebral blood flow (VBF), cerebral blood flow (CBF), renal blood flow (RBF), and femoral blood flow (FBF) in a dose-dependent manner. A total Fasudil dose of 1.0 ng/mL enhanced cardiac output. Intracoronary injections of 30 μg Fasudil in experimental dogs resulted in approximately a 50% increase in CBF. Oral administration of Fasudil (dose of 100 mg/kg/day) significantly lowered the incidence and average maximum clinical score of experimental autoimmune encephalomyelitis (EAE) in SJL/J mice immunized with PLP p139-151. Fasudil inhibited the proliferation response of mouse spleen cells to antigens, demonstrating cardiovascular protective effects by reducing the activation of JNK and mitigating the mitochondrial translocation of apoptosis-inducing factor (AIF) in ischemic injury. |
| In vivo | Fasudil induces the disassembly of actomyosin fibers and inhibits cell migration, competitively suppressing Ca2+-induced depolarization and constriction of the rabbit aorta. It blocks contraction responses to KCl, serum phenylalanine, and prostaglandin F2α, and inhibits the proliferation of hepatic stellate cells, formation of stress fibers, and expression of α-SMA, while also repressing cell growth without inducing apoptosis. Fasudil curtails the phosphorylation of ERK1/2, JNK, and p38 MAPK induced by LPA. Additionally, it exerts vasodilatory effects by inhibiting the contraction induced by serotonin, noradrenaline, histamine, angiotensin, and dopamine. |
| Storage | keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 32.8 mg/mL (100.05 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (10.07 mM), Sonication is recommended.
DMSO : 82 mg/mL (250.13 mM), Sonication is recommended.
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| Keywords | TWNT-4 cells | TIMP-1 | threoninkinase | threonin kinase | Serinekinase | Serine kinase | ROCK2 | ROCK | rat HSCs | protein kinases | Protein kinase A | PKG | PKC | PKA | p38 | MLCK | lysophoaphatidic acid | LPA | human HSC | HIVProtease | HIV Protease | HIV | HA1077 Hydrochloride | HA1077 | HA 1077 Hydrochloride | HA 1077 | Fasudil | ERK1/2 | CalciumChannel | Calcium Channel | Ca2+ channel antagonist | Autophagy | AT-877 | AT877 | AT 877 | a-SMA |
| Inhibitors Related | Stavudine | Emtricitabine | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Lamivudine | Guanidine hydrochloride | Valproic Acid | Paeonol | Naringin | L-Ascorbic acid sodium salt | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Neuroprotective Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | TGF-beta/Smad Compound Library |
United States
