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.
Cancer Discovery. 2018 Sep 13.
Prediction of DNA Repair Inhibitor Response in Short Term Patient-Derived Ovarian Cancer Organoids.
Y-27632 dihydrochloride purchased from AbMole
Nature Microbiology. 2018 Jul;3(7):814-823.
Modelling Cryptosporidium infection in human small intestinal and lung organoids.
Y-27632 dihydrochloride purchased from AbMole
Adv Mater. 2018 Sep 10;e1801621.
Growth of Epithelial Organoids in a Defined Hydrogel.
Y-27632 dihydrochloride purchased from AbMole
Oncotarget. 2017 Dec 28;9(12):10375-10387.
The crosstalk between breast carcinoma-associated fibroblasts and cancer cells promotes RhoA-dependent invasion via IGF-1 and PAI-1.
Y-27632 dihydrochloride purchased from AbMole
Nat Protoc. 2018 Feb;13(2):235-247.
A surgical orthotopic organoid transplantation approach in mice to visualize and study colorectal cancer progression
Y-27632 dihydrochloride purchased from AbMole
Nat Protoc. 2018 Jan;13(1):59-78.
Measuring mutation accumulation in single human adult stem cells by whole-genome sequencing of organoid cultures
Y-27632 dihydrochloride purchased from AbMole
Cell. 2018 Jan 11;172(1-2):373-386.e10.
A Living Biobank of Breast Cancer Organoids Captures Disease Heterogeneity
Y-27632 dihydrochloride purchased from AbMole
Am J Clin Exp Urol. 2017 Nov 9;5(3):25-33.
Organoid culture of human prostate cancer cell lines LNCaP and C4-2B
Y-27632 dihydrochloride purchased from AbMole
Mater Sci Eng C Mater Biol Appl. 2017 Sep 1;78:443-451.
A dual-layer macro/mesoporous structured TiO2 surface improves the initial adhesion of osteoblast-like cells
Y-27632 dihydrochloride purchased from AbMole
Nature. 2016 Nov 24;539(7630):560-564.
Designer matrices for intestinal stem cell and organoid culture
Y-27632 dihydrochloride purchased from AbMole
Nat Protoc. 2016 Feb;347-58.
Organoid culture systems for prostate epithelial and cancer tissue.
Y-27632 dihydrochloride purchased from AbMole
![]() |
Source | Nature (2016). Figure 1. Y-27632 (Abmole Bioscience Inc) |
Method | Cell culture. | |
Cell Lines | single cells | |
Concentrations | 10 μM | |
Incubation Time | ||
Results |
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. |
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.
Molecular Weight | 320.26 |
Formula | C14H21N3O.2HCl |
CAS Number | 129830-38-2 |
Purity | 99.61% |
Solubility | Water ≥100 mg/mL |
Storage | at -20°C |
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 |
---|
ZINC00881524
ZINC00881524 is a potent and selective ROCK inhibitor. |
HA 1100 hydrochloride
HA 1100 hydrochloride is a cell-permeable, selective Rho-kinase inhibitor. |
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.