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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Y-27632 is a potent and selective inhibitor of ROCK1 (p160ROCK) with IC50 of 140 nM in a cell-free assay, it exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. Y27632 prevents dimethylnitrosamine-induced hepatic fibrosis in rats, increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium, affects initial heart myofibrillogenesis in cultured chick blastoderm, promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord. Y-27632 suppresses the kinase activity of both ROCK-1 and ROCK-2 in vitro, and this compound inhibits the kinases by binding to the catalytic site of ROCK-1 and ROCK-2. Thus Y-27632 function on Rho-mediated stress fiber formation, the G1-S phase progression and cytokinesis.
| ln Vitro |
Y-27632 exhibits a 100-fold increase in concentration-inhibitory delay in the emergence of BrdU labeling, as well as an extension of the delay duration. In Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively, delays of about 1 and 4 hours were noted [1]. Adipose tissue-derived stem cells (ADSCs) are encouraged by Y-27632 in the oral cavity of neurons. The 5.0 μM Y-27632 induction group had the greatest number of neural-like cells when compared to the 1.0 and 2.5 μM Y-27632 induction groups [2]. In epithelial cells, actin masks remodel and upregulate cytokines [8].
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| ln Vivo |
In comparison to the saline group, Y-27632 (5 and 10 mg/kg) considerably extended the onset time of myoclonic seizures. When Y-27632 (5 and 10 mg/kg) was administered, the onset of clonic convulsions was significantly delayed in comparison to the saline group [3]. Rats treated with dimethylnitrosamine (DMN) showed a significant reduction in liver weight and body weight (DMN-S group) when compared to the control group (SS group). Rats (DMN-Y group) were essentially shielded from this DMN-induced loss of body and liver weight by oral administration of Y27632 (30 mg/kg) [4].
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| References |
[1]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
[2]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells.Chin Med J (Engl). 2012 Sep;125(18):3332-5. [3]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36. [4]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51. [5]. Maldonado M, et al. ROCK inhibitor primes human induced pluripotent stem cells to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymal transition-like modulation. Stem Cell Res. 2016 Sep;17(2):222-227. [6]. Kan L, et al. Rho-Associated Kinase Inhibitor (Y-27632) Attenuates Doxorubicin-Induced Apoptosis of Human Cardiac Stem Cells. PLoS One. 2015;10(12):e0144513. Published 2015 Dec 8. [7]. Zhang L, et al. ROCK inhibitor Y-27632 suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells and increases their cloning efficiency. PLoS One. 2011;6(3):e18271. Published 2011 Mar 28. [8]. Svoboda KK, et al. ROCK inhibitor (Y27632) increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium. Dev Dyn. 2004;229(3):579-590 |
| Molecular Formula |
C14H21N3O
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| Molecular Weight |
247.34
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| CAS # |
146986-50-7
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| Related CAS # |
Y-27632 dihydrochloride;129830-38-2;Y-27632 dihydrochloride;129830-38-2
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| SMILES |
O=C([C@@H]1CC[C@]([C@H](N)C)([H])CC1)NC2=CC=NC=C2
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (8.09 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0430 mL | 20.2151 mL | 40.4302 mL | |
| 5 mM | 0.8086 mL | 4.0430 mL | 8.0860 mL | |
| 10 mM | 0.4043 mL | 2.0215 mL | 4.0430 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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