Chemdea
 
작성일 : 14-04-05
[Chemdea] Rho Kinase Inhibitors
Fasudil (HA 1077) Dihydrochloride / Rho Kinase Inhibitor III (Rockout) / Y-27632 - ROCK Inhibitor


Rho Kinase Inhibitors



Product Name: Fasudil (HA 1077) Dihydrochloride – ROCK Inhibitor


   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요


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

Chemical Formula:

 

C14H17N3O2·2HCl.

CAS No.:

 

938440-64-3

Molecular weight:

 

364.3.

Purity:

99% by HPLC

Appearance:

 

White solid

Chemical name:

 

5-Isoquinolinesulfonyl)homopiperazine Dihydrochloride

Solubility:

 

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.

Storage:

Protect from light. Packaged under inert gas


References

1. Watanabe, K. et al. Nature Biotech. 2007, 25, 681;


Product Name: Rho Kinase Inhibitor III (Rockout) – ROCK Inhibitor


   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요


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

Chemical Formula:

 

C13H10N2

CAS No.:

 

7272-84-6

Molecular weight:

 

194.2

Purity:

99% by HPLC

Appearance:

 

Yellow solid

Chemical name:

 

3-(4-Pyridyl)-1H-indole

Solubility:

 

DMSO (25mg/mL)

Storage:

Protect from light. Packaged under inert gas


Reference


 

Product Name: Y-27632 – ROCK Inhibitor


   클릭하시면 닫힙니다.이미지 저장을 원하시면 마우스 오른쪽클릭후 '다른이름으로 저장'을 하세요


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

Chemical Formula:

 

C14H21N3O·2HCl·H2O

CAS No.:

 

146986-50-7

Molecular weight:

 

338.3.

Purity:

99% by HPLC

Appearance:

 

white solid

Chemical name:

 

(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

Solubility:

 

water (100 mg/mL)

Storage:

Protect from light. Packaged under inert gas


References


 

Ordering informations


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


 

▣ 관련 페이지 ; Chemdea