Free shipping on all orders over $ 500

Y-27632 dihydrochloride

Cat. No. M1817
Y-27632 dihydrochloride Structure
Synonym:

Y-27632

Size Price Availability Quantity
10mg USD 150 In stock
50mg USD 400 In stock
100mg USD 650 In stock
Bulk Inquiry?

Quality Control
Biological Activity

Y-27632 is a potent, selective inhibitor of Rho-associated protein kinases (ROCK) with IC50 values of 140-220 nM for ROCK1 and ROCK2. Y-27632 inhibited the kinase activity of both ROCK-I and ROCK-II in vitro, and this inhibition was reversed by ATP in a competitive manner. The ROCK family of Rho-associated serine-threonine protein kinases is known to play an important role in Rho-mediated cell adhesion and smooth muscle contraction. It also inhibits PRK2 with an IC50 value of 600 nM. One-hour treatment with 10 µM Y-27632 blocks apoptosis of dissociated cultured human embryonic stem cells, increasing cloning efficiency by 25% and sustaining survival up to 30 passages. Y-27632 was found to increases human embryonic stem cell (hESC) survival.

Protocol
Cell Experiment
Cell lines cyES cells
Preparation method For 5-bromo-2′-deoxyuridine (BrdU) incorporation assays, dissociated cyES cells were seeded at a concentration of 500 cells/cm2 onto fresh feeder layers in the presence of the ROCK inhibitors Y-27632 (Wako Pure Chemical Industries, Tokyo, Japan) or Fasudil (Tocris Bioscience, MO, USA) during the first 24 h of culture. The BrdU incorporation assay was performed using colorimetric BrdU Cell proliferation Kit (Roche Diagnostics) according to the manufacturer's instructions. BrdU incorporations were also observed by immunocytochemical (ICC) staining with BrdU Labeling and Detection Kit I (Roche Diagnostics).
Concentrations 0, 0.1, 0.5, 5, 10, 20µM
Incubation time 24 h
Animal Experiment
Animal models EAC modeling
Formulation dissolved in 0.9% NaCl
Dosages 0.1, 1, 10 mg/kg/day for 14 days
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 320.26
Formula C14H21N3O.2HCl
CAS Number 129830-38-2
Purity 99.61%
Solubility Water ≥100 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Nature Protocols (2016) . Figure 3. Y-27632 (Abmole Bioscience)
Method MTT assay
Cell Lines mouse and human luminal cell
Concentrations 10 μM
Incubation Time 2–3 d
Results Absence of the ROCK inhibitor (Y-27632) will greatly decrease the efficiency of organoid outgrowth.
Rating
Source Nature (2016). Figure 1. Y-27632 (Abmole Bioscience Inc)
Method Cell culture.
Cell Lines single cells
Concentrations 10 μM
Incubation Time
Results
Rating
Source Materials Science and Engineering (2017). Figure 8. Y-27632 (Abmole Bioscience Inc, USA)
Method Cytoskeleton and nucleus staining in the absence or presence of ROCK inhibitor (Y-27632)
Cell Lines SaOS-2 cells
Concentrations 10 μM
Incubation Time 4 h and 24 h
Results After inhibition of ROCK by Y-27632, an expected formation of finger-like filopodia was seen for the cells of all groups after 4 h, as shown by white arrows in Fig. 8b, f and j.
Rating
Source Materials Science and Engineering (2017). Figure 7. Y-27632 (Abmole Bioscience Inc, USA)
Method Cytoskeleton and nucleus staining in the absence or presence of ROCK inhibitor (Y-27632)
Cell Lines SaOS-2 cells
Concentrations 10 μM
Incubation Time 4 h and 24 h
Results The attached cells on the three investigated surfaces in the presence or absence (control) of Y-27632 after 4 h and 24 h were summarized in Fig. 7
Rating
Product Citations
References

The ROCK inhibitor Y-27632 enhances the survival rate of human embryonic stem cells following cryopreservation.
Li X, et al. Stem Cells Dev. 2008 Dec;17(6):1079-85. PMID: 19006455.

Effects of rho-associated protein kinase inhibitor Y-27632 on intraocular pressure and outflow facility.
Honjo M, et al. Invest Ophthalmol Vis Sci. 2001 Jan;42(1):137-44. PMID: 11133858.

Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases.
Ishizaki T, et al. Mol Pharmacol. 2000 May;57(5):976-83. PMID: 10779382.

Related ROCK Products
Ripasudil (K-115) dihydrate

Ripasudil (K-115) hydrochloride dihydrate is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

SR 3677

SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.

GSK180736A

GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.

GSK269962A

GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively.

Y-39983 dihydrochloride

Y-39983 Hcl is a selective ROCK inhibitor derived from Y-27632, inhibited ROCK more potently than Y-27632.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Y-27632 dihydrochloride, Y-27632 supplier, ROCK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.