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Y-27632

Catalog No. T1870   CAS 146986-50-7

Y-27632 (Y-27632) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

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Y-27632 Chemical Structure
Y-27632, CAS 146986-50-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 55.00
25 mg In stock $ 98.00
50 mg In stock $ 172.00
100 mg In stock $ 288.00
200 mg In stock $ 448.00
500 mg In stock $ 739.00
1 mL * 10 mM (in DMSO) In stock $ 43.00
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Purity: 99.87%
Purity: 99.87%
Purity: 99.83%
Purity: 99.73%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Y-27632 (Y-27632) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.
Targets&IC50 ROCKI:220 nM(ki), ROCKII:300 nM(ki)
In vitro METHODS: Human induced pluripotent stem cells, marmoset iPSC, were treated with Y-27632 (5-20 μM) for 7 days and clone formation was detected by AKP.
RESULTS: Y-27632 significantly improved the cloning efficiency of marmoset iPSC. [1]
METHODS: Adult adipose tissue-derived stem cells ADSCs were treated with Y-27632 (5 μmol/L) for 1 h. The morphological changes of ADSCs were detected.
RESULTS: Y-27632 dose-dependently induced neuronal differentiation in ADSCs. the percentage of neuron-like cells in ADSCs treated with 5 μmol/L Y-27632 for 1 h was (93.5±4.7)%. [2]
METHODS: Crab monkey embryonic stem cells cyES were routinely passaged or treated with Y-27632 (1-10 μM) for 24 h. Live-dead staining was performed using the Flow Cytometry method, and BrdU was detected using a kit.
RESULTS: Y-27632 promoted the increase of cyES surviving cells. Y-27632 did not promote cell proliferation, but protected the cells from cell death after single-cell digestion. [3]
In vivo METHODS: To investigate the therapeutic potential of Y-27632 in motor neuron disease, Y-27632 (2 or 30 mg/kg in drinking water) was administered orally to SOD1G93A mice in the ALS model for 137 days.
RESULTS: Y-27632 2 mg/kg treatment was ineffective, Y-27632 30 mg/kg treatment improved motor function in male mice, and female mice showed only limited improvement. [4]
METHODS: To investigate the effect of Y-27632 on liver fibrosis, Y-27632 (30 mg/kg) was administered orally to rats with dimethylnitrosamine (DMN)-induced liver fibrosis once a day for four weeks.
RESULTS: Y-27632 treatment significantly reduced the incidence of DMN-induced hepatic fibrosis and lowered the levels of collagen and hydroxyproline as well as the expression of α-SMA in the liver. [5]
Kinase Assay Recombinant ROCK-I, ROCK-II, 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 phosphatidyl serine, 50 ng/mL 12-O-tetradecanoylphorbol-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 Y-27632 is dissolved in water and stored[1]. HeLa cells are plated at a density of 3×104 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), Y-30141, or vehicle is added and the cells are incubated for another 30 min[1].
Molecular Weight 247.34
Formula C14H21N3O
CAS No. 146986-50-7

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 1 mg/ml (4.04 mM)

DMSO: 45 mg/mL (181.94 mM)

TargetMolReferences and Literature

1. Wu Y, et al. ROCK inhibitor Y27632 promotes proliferation and diminishes apoptosis of marmoset induced pluripotent stem cells by suppressing expression and activity of caspase 3. Theriogenology. 2016 Jan 15;85(2):302-14. 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. Takehara T, et al. Rho-associated kinase inhibitor Y-27632 promotes survival of cynomolgus monkey embryonic stem cells. Mol Hum Reprod. 2008 Nov;14(11):627-34. 4. Günther R, et al. The rho kinase inhibitor Y-27632 improves motor performance in male SOD1(G93A) mice. Front Neurosci. 2014 Oct 7;8:304. 5. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.

TargetMolCitations

1. Chen Y P, Shao Y, Chen P C, et al.Substrate nesting guides cyst morphogenesis of human pluripotent stem cells without 3D extracellular matrix overlay.Acta Biomaterialia.2023 2. Wang X, Liang X, Zhou L, et al. Yes-associated protein reacts differently in vascular smooth muscle cells under different intensities of mechanical stretch. Aging (Albany NY). 2022, 14(1): 286. 3. Xu L, Wang G, Shi R, et al.A cocktail of small molecules maintains the stemness and differentiation potential of conjunctival epithelial cells.The Ocular Surface.2023 4. He W, Zhu X, Xin A, et al. Long-term maintenance of human endometrial epithelial stem cells and their therapeutic effects on intrauterine adhesion. Cell & Bioscience. 2022, 12(1): 1-20. 5. Tao Z, Cui Y, Xu X, et al. FGFR redundancy limits the efficacy of FGFR4-selective inhibitors in hepatocellular carcinoma. Proceedings of the National Academy of Sciences. 2022, 119(40): e2208844119. 6. Schenke M, Prause H C, Bergforth W, et al. Human-Relevant Sensitivity of iPSC-Derived Human Motor Neurons to BoNT/A1 and B1. Toxins. 2021, 13(8): 585. 7. Housmans B A C, Neefjes M, Surtel D A M, et al. Synovial fluid from end-stage osteoarthritis induces proliferation and fibrosis of articular chondrocytes via MAPK and RhoGTPase signaling. Osteoarthritis and Cartilage. 2022

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Kinase Inhibitor Library Inhibitor Library TGF-beta/Smad Compound Library Bioactive Compounds Library Max Anti-Cardiovascular Disease Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compound Library Anti-Cancer Compound Library NO PAINS Compound Library

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Keywords

Y-27632 146986-50-7 Apoptosis Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK Rho-associated protein kinase ROK Inhibitor inhibit Rho-kinase Y 27632 Rho-associated kinase Y27632 inhibitor

 

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