Rho Kinase Inhibitors
본문
Rho Kinase Inhibitors
Product Name: Fasudil (HA 1077) Dihydrochloride – ROCK Inhibitor
   
| 
                 A cell-permeable, reversible, and ATP-competitive Ca2+ antagonist with anti-vasospastic properties. Inhibits protein kinase A (Ki = 1.6 µM), protein kinase G (Ki = 1.6 µM), and myosin light chain kinase (Ki = 3.6 µM). Also reported to potently inhibit Rho-associated kinase (ROCK; IC50 = 10.7 µM). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency.  | 
        
Details
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             Chemical Formula:  | 
        
             
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             C14H17N3O2·2HCl.  | 
    
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             CAS No.:  | 
        
             
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             938440-64-3  | 
    
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             Molecular weight:  | 
        
             
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             364.3.  | 
    
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             Purity:  | 
        
             
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             99% by HPLC  | 
    
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             Appearance:  | 
        
             
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             White solid  | 
    
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             Chemical name:  | 
        
             
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             5-Isoquinolinesulfonyl)homopiperazine Dihydrochloride  | 
    
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             Solubility:  | 
        
             
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             Water (200 mg/mL), DMSO (10 mg/mL). Addition of an aqueous solution of fasudil dihydrochloride into a buffer solution may significantly alter its solubility.  | 
    
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             Storage:  | 
        
             
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             Protect from light. Packaged under inert gas  | 
    
References
1. Watanabe, K. et al. Nature Biotech. 2007, 25, 681;
2. Swärd, K. et al. J. Physiol. 2000, 522, 33;
3. Takizawa, S. et al. Eur. J. Pharmacol. 1993, 250, 431;
4. Seto, M. et al. Eur. J. Pharmacol. 1991, 195, 267;
5. Shirotani, M. et al. J. Pharmacol. Exp. Ther. 1991, 259, 738;
6. Asano, T. et al. Eur. J. Pharmacol. 1990, 190, 365;
7. Sasaki, Y., and Sasaki, Y. Biochem. Biophys. Res. Commun. 1990, 171, 1182;
8. Asano, T. et al. Br. J. Pharmacol. 1989, 98, 1091.
Product Name: Rho Kinase Inhibitor III (Rockout) – ROCK Inhibitor
   
| 
                 A cell-permeable, selective, reversible, and ATP-competitive inhibitor of Rho kinase activity (IC50 = 25 µM). Does not inhibit the activation of Rho kinase nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be 5-fold less potent than Y-27632 (Cat# CD0141; IC50 ~5 µM), and display a similar specificity profile as H-89 (Cat. No. 371963). Affects cell migration, inhibits blebbing (IC50 ~12 µM in M2 cells), and decreases stress fibers in Bulb 3T3 cells at 50 µM.  | 
        
Details
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             Chemical Formula:  | 
        
             
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             C13H10N2  | 
    
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             CAS No.:  | 
        
             
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             7272-84-6  | 
    
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             Molecular weight:  | 
        
             
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             194.2  | 
    
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             Purity:  | 
        
             
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             99% by HPLC  | 
    
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             Appearance:  | 
        
             
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             Yellow solid  | 
    
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             Chemical name:  | 
        
             
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 3-(4-Pyridyl)-1H-indole  | 
    
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             Solubility:  | 
        
             
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             DMSO (25mg/mL)  | 
    
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             Storage:  | 
        
             
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             Protect from light. Packaged under inert gas  | 
    
Reference
Product Name: Y-27632 – ROCK Inhibitor
   
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                 A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. Exhibits 10- to 50-fold lower affinity for PKCε than p160ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 µM). Also acts as a potent inhibitor of agonist- induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC50 = 700 nM for phenylephrine-induced contractions in aortic strips). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency.  | 
        
Details
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             Chemical Formula:  | 
        
             
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             C14H21N3O·2HCl·H2O  | 
    
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             CAS No.:  | 
        
             
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             146986-50-7  | 
    
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             Molecular weight:  | 
        
             
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             338.3.  | 
    
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             Purity:  | 
        
             
  | 
        
             99% by HPLC  | 
    
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             Appearance:  | 
        
             
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             white solid  | 
    
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             Chemical name:  | 
        
             
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             (1E,4S,4aR,5R,6aS,7S,9aR)-5-(Acetyloxy)-1-[[[3-(dimethylamino)propyl]methylamino]methylene]-4a,5,6,6a,7,8,9,9a-octahydro-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethylcyclopenta[5,6]na-phtho[1,2-c]pyran-2,10(1H,4H)-dione  | 
    
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             Solubility:  | 
        
             
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             water (100 mg/mL)  | 
    
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             Storage:  | 
        
             
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             Protect from light. Packaged under inert gas  | 
    
References
1. Watanabe, K. et al. Nature Biotech. 2007, 25, 681;
2. Chitaley, K. et al. Nat. Med. 2001, 7, 119;
3. Davies, S. P. et al. Biochem. J. 2000, 351, 95;
4. Narumiya, S. et al. Methods Enzymol. 2000, 325, 273;
5. Hirose, M. et al. J. Cell Biol. 1998, 141, 1625;
Ordering informations
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                 Catalog No.  | 
            
                 Product Name  | 
            
                 Size  | 
        
| 
                 CD0160  | 
            
                 Fasudil (HA 1077) Dihydrochloride – ROCK Inhibitor  | 
            
                 250mg, 500mg, 1g, 2g & 5g  | 
        
| 
                 CD0222  | 
            
                 Rho Kinase Inhibitor III (Rockout) – ROCK Inhibitor  | 
            
                 5mg, 10mg, 50mg, 100mg & 200mg  | 
        
| 
                 CD0141  | 
            
                 Y-27632 – ROCK Inhibitor  | 
            
                 1mg, 5mg, 10mg, 25mg, 50mg ,100mg, 250mg & 1g  | 
        
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