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Cell Cycle/Checkpoint ROCK Y-27632 dihydrochloride

Y-27632 dihydrochloride

Catalog No. T1725   CAS 129830-38-2
Synonyms: Y-27632 2HCl
Purity 99.98% Datasheet MSDS

Y-27632 is a selective inhibitor of ROCKs including p160ROCK (Ki: 140 nM) and ROCK2 (IC50: 800 nM).

Y-27632 dihydrochloride, CAS 129830-38-2
Pack Size Availability Price/USD Quantity
2 mg In stock 29.00
5 mg In stock 50.00
10 mg In stock 65.00
25 mg In stock 124.00
50 mg In stock 199.00
100 mg In stock 338.00
200 mg In stock 530.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Preparing Solutions
Description Y-27632 is a selective inhibitor of ROCKs including p160ROCK (Ki: 140 nM) and ROCK2 (IC50: 800 nM).
Targets&IC50 ROCK1 (p160ROCK) :ic50 140 nM (Ki, cell free),   ROCK2 :ic50 300 nM (Ki, cell free),  
In vivo Y-27632 significantly decreased the blood pressure in a dose-dependent manner in spontaneously hypertensive rats: a fall of 50 mm Hg was still observed 7 h after administration of 30 mg/kg of Y-27632. The same dose of this compound also caused a significant and persistent fall in blood pressure in renal hypertensive rats, as well as in deoxycorticosterone acetate (DOCA)-salt hypertensive rats. On the other hand, administration of the same dose of Y-27632 caused only a slight and transient fall in blood pressure in control Wistar rats [4]. Y-27632 (5-10 mg/kg) and fasudil 5-25 (mg/kg) diminished onset of myoclonic jerks, clonic convulsions and tonic hindlimb extensions in mice given pentylenetetrazole [5].
Kinase Assay Recombinant ROCK1/2, PKN, or citron kinase is expressed in HeLa cells as Myc-tagged proteins by transfection using Lipofectamine and is precipitated from the cell lysates by the use of 9E10 monoclonal anti-Myc antibody coupled to G protein-Sepharose. Recovered immunocomplexes are incubated with various concentrations of [32P]ATP and 10 mg of histone type 2 as substrates in the absence or presence of various concentrations of either Y-27632 or Y-30141 at 30°C for 30 min in a total volume of 30 μL of the kinase buffer containing 50 mM HEPES-NaOH, pH 7.4, 10 mM MgCl2, 5 mM MnCl2, 0.02% Briji 35, and 2 mM dithiothreitol. PKCa is incubated with 5 μM [32P]ATP and 200 μg/mL histone type 2 as substrates in the absence or presence of various concentrations of either Y-27632 or Y-30141 at 30°C for 10 min in a kinase buffer containing 50 mM Tris-HCl, pH 7.5, 0.5 mM CaCl2, 5 mM magnesium acetate, 25 μg/mL phosphatidylserine, 50 ng/mL 12-O-tetradecanoyl phorbol-13-acetate and 0.001% leupeptin in a total volume of 30 μL. Incubation is terminated by the addition of 10 μL of 43 Laemmli sample buffer. After boiling for 5 min, the mixture is subjected to SDS-polyacrylamide gel electrophoresis on a 16% gel. The gel is stained with Coomassie Brilliant Blue and then dried. The bands corresponding to histone type 2 are excised, and the radioactivity is measured [1].
Cell Research
HeLa cells are plated at a density of 3×10^4 cells per 3.5-cm dish. The cells are cultured in DMEM containing 10% FBS in the presence of 10 mM Thymidine for 16 h. After the cells are washed with DMEM containing 10% FBS, they are cultured for an additional 8 h, and then 40 ng/mL of Nocodazole is added. After 11.5 h of the Nocodazole treatment, various concentrations of Y-27632 (0-300 μM) or vehicle is added and the cells are incubated for another 30 min [1].
Animal Research
A group of animals was injected with a single dose of pentylenetetrazole (PTZ, 65?mg/kg) to investigate if the two Rho-kinase inhibitors, fasudil, and Y-27632, changed the onset of PTZ seizures. Fasudil, Y-27632 or saline was given intraperitoneally 30?min before the PTZ injection. Each mouse was then observed for a 15-min period to measure the onset of the first myoclonic jerk, the onset of the first clonic convulsion and the occurrence of tonic hindlimb extension. Some of the animals died after tonic hindlimb extension, which is an expected outcome of acute PTZ injection. After the observation period, all animals were killed by halothane anesthesia [5]. Seven-week-old male Wistar rats were anesthetized with sodium pentobarbital. A silver clip (0.2 mm in diameter) was placed on the left renal artery in the preparation of the renal hypertensive rats. In the preparation of the DOCA-salt hypertensive rats, the left kidney was removed and a DOCA pellet (50 mg) was implanted subcutaneously. The DOCA rats were then fed an 8% salt diet. Rats from both groups were used after 8 weeks in the experiments, together with a male, 17–22-week old spontaneously hypertensive rats. The average systolic pressure in these groups of hypertensive rats ranged from 209 to 237 mm Hg, and no significant difference was found between groups. Eight-week-old male Wistar rats were used as controls. Their average systolic pressure was 139 mm Hg. Y-27632was administered orally. The systolic blood pressure was measured by the tail cuff method at 1, 3, 5, 7 and 24 h. The rats were prewarmed to 40 8C for 10 min before each measurement. No toxicity was found in rats treated with 30 mg kg?1 of Y-27632 administered per os once per day for 10 days [4].
Animal Model: Wistar rats with spontaneous or induced hypertension; Swiss albino mice with Ehrlich ascites carcinoma
Synonyms Y-27632 2HCl
Purity 99.98%
Appearance solid
Molecular Weight 320.26
Formula C14H21N3O·2HCl
CAS No. 129830-38-2

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 199.8 mM

Water: 43.7 mM

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

Solution 1

Saline: 30 mg/mL

Citations

References and Literature
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. Watanabe K, et al. A ROCK inhibitor permits survival of dissociated human embryonic stem cells. Nat Biotechnol. 2007 Jun;25(6):681-6. 3. 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. 4. Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389(6654):990-4. 5. 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.

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