Rho Kinase Inhibitors
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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
Chemical Formula: |
|
C14H17N3O2·2HCl. |
CAS No.: |
|
938440-64-3 |
Molecular weight: |
|
364.3. |
Purity: |
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99% by HPLC |
Appearance: |
|
White solid |
Chemical name: |
|
5-Isoquinolinesulfonyl)homopiperazine Dihydrochloride |
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. |
Storage: |
|
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
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
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
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
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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