1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
  2. ROCK

Y-27632 

Cat. No.: HY-10071 Purity: 99.65%
Handling Instructions

Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.

For research use only. We do not sell to patients.

Y-27632 Chemical Structure

Y-27632 Chemical Structure

CAS No. : 146986-50-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 564 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1032 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of Y-27632:

    Y-27632 purchased from MCE. Usage Cited in: Oncotarget. 2017; 8:82506-82530.

    SKOV3 mock-transfected control (Ctrl) and shRNA-Hic-5 knockdown (KD) (sh-S1 and sh-S2) cells were either untreated (-) or treated (+) with 10mM Y27632 over a period of 48 hr. SKOV3 mock-transfected control (Ctrl) and shRNA-Hic-5 knockdown (KD) (sh-S1 and sh-S2) clones were either untreated (-) or treated (+) with 10 mM Y27632 followed by stimulation without (-) or with (+) 5 ng/mL of TGFβ1 for 48 hr.

    Y-27632 purchased from MCE. Usage Cited in: Sci Rep. 2017 Dec 19;7(1):17770.

    Western blot analysis of pAXL level in H1299 cells treated with the indicated concentration of R428 for 1 h. Results are confirmed in three independent experiments.

    Y-27632 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 28;37(1):128.

    MHCC-97H cells are transfected with control or supervillin-specific siRNA for 48 h, exposed to hypoxia for 16 h, and lysates are assayed for the relative amounts of GTP-loaded (activated) Rac1, Cdc42, and RhoA. Cells that have been transfected with control RNAi are treated with a PD0325901 or SB239063 before assaying for GTP-Rac1, Cdc42, and RhoA levels.

    Y-27632 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 28;37(1):128.

    MHCC-97H and Huh-7 cells co-transfected with control or supervillin-specific siRNA and a RhoA(WT), RhoA(V14), or RhoA(N19) plasmids for 48 h are treated with PBS or Y27632 2HCl (10 μM) for 16 h during hypoxia, and then assayed for phosphorylated p38 and ERK by immunoblotting. β-actin is used as the loading control

    View All ROCK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.

    IC50 & Target[1]

    ROCK-I

    220 nM (Ki)

    ROCK-II

    300 nM (Ki)

    PKN

    3.1 μM (Ki)

    Citron kinase

    5.3 μM (Ki)

    PKCα

    73 μM (Ki)

    PKA

    25 μM (Ki)

    In Vitro

    Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively[1]. Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). Compared to 1.0 and 2.5 µM Y-27632 induced groups, percentages of neuroal-like cells achieved a peak in the 5.0 µM Y-27632 induced group[2].

    In Vivo

    Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group[3]. Treatment with Dimethylnitrosamine (DMN) causes a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group)[4].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (129.38 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Mice[3]
    Male, inbred Swiss albino mice (2-3 months old) weighing 25-30 g are used. Mice are injected with a sub-convulsive dose of PTZ (35 mg/kg, i.p.) (on Mondays, Wednesdays and Fridays) of each week for a total of 11 injections. After each PTZ injection, mice are observed for 30 min and the occurrence of convulsive activity is recorded. After 30 min, the mice are then injected with either Fasudil (25 mg/kg, i.p.) or Y-27632 (5 mg/kg, i.p.) and returned to their home cages until the next injection. Control mice for Fasudil and Y-27632 receives saline.
    Rats[4]
    Male Wistar Kind A rats (200-250 g) are used. DMN (1 g/mL) is diluted ten times with saline (final concentration 1%) and 10 mg/kg per day of DMN is injected intraperitoneally (i.p.) on the first 3 days of each week for 4 weeks. Y27632 is given orally once per day at a dose of 30 mg/kg for 4 weeks starting on the day of the first injection of DMN. The dose of 30 mg/kg corrects hypertension in several rat models without toxicity. Twenty rats are randomized into four experimental groups (n=5 in each group) as follows: (1) S-S (injection of saline i.p. and oral administration of saline); (2) S-Y (injection of saline i.p. and oral administration of Y27632); (3) DMN-S (DMN i.p. and oral administration of saline); (4) DMN-Y (DMN i.p. and oral administration of Y27632). The rats are weighed every week. They are sacrificed at the end of the fourth week and the liver is excised. In addition, a blood sample is taken immediately before the rats are sacrificed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    247.34

    Formula

    C₁₄H₂₁N₃O

    CAS No.

    146986-50-7

    SMILES

    O=C([[email protected]@H]1CC[[email protected]]([[email protected]](N)C)([H])CC1)NC2=CC=NC=C2

    Storage

    4°C, stored under nitrogen

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.65%

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    Product Name:
    Y-27632
    Cat. No.:
    HY-10071
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    Y-27632

    Cat. No.: HY-10071