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GPCR/G Protein PKA Fasudil hydrochloride

Fasudil hydrochloride

Catalog No. T3060   CAS 105628-07-7
Synonyms: AT-877, Fasudil HCl, HA-1077, Fasudil (HA-1077) HCl, HA-1077 hydrochloride
Purity 100.00% Datasheet MSDS

Fasudil Hydrochloride 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.

Fasudil hydrochloride, CAS 105628-07-7
Pack Size Availability Price/USD Quantity
25 mg In stock 32.00
50 mg In stock 42.00
100 mg In stock 51.00
200 mg In stock 78.00
500 mg In stock 131.00
1 mL * 10 mM (in DMSO) In stock 50.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description Fasudil Hydrochloride 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.
Targets&IC50 MLCK :ic50 36μM(Ki),   PKA :ic50 1.6μM(Ki),   PKC :ic50 3.3μM(Ki),   PKG :ic50 1.6μM(Ki),   ROCK2 :ic50 330nM(Ki),  
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.
Synonyms AT-877, Fasudil HCl, HA-1077, Fasudil (HA-1077) HCl, HA-1077 hydrochloride
Purity 99.54%
Appearance solid
Molecular Weight 327.83
Formula C14H18ClN3O2S
CAS No. 105628-07-7

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 24.6 mg/mL (75 mM)

water: 32.8 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

Saline: 30 mg/mL

Citations

References and Literature
1. Ono-Saito N, et al. Pharmacol Ther, 1999, 82(2-3), 123-131. 2. Asano T, et al. J Pharmacol Exp Ther, 1987, 241(3), 1033-1040. 3. Asano T, et al. Br J Pharmacol, 1989, 98(4), 1091-1100. 4. Negoro N, et al. Biochem Biophys Res Commun, 1999, 262(1), 211-215. 5. Fukushima M, et al. Liver Int, 2005, 25(4), 829-838. 6. Zhang J, et al. Clin Chim Acta, 2009, 401(1-2), 76-80.

Related Compound Libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Stem cell Differentiation Compound Library Apoptosis Compound Library Autophagy Compound Library Epigenetics Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library GPCR Compound Library Anti-Cardiovascular Disease Compound Library TGF-beta/Smad Compound Library Cell cycle related Compound Library

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