1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    Cytoskeleton
    TGF-beta/Smad
    Apoptosis
  2. ROCK
    Apoptosis
  3. Y-27632 dihydrochloride

Y-27632 dihydrochloride 

Cat. No.: HY-10583 Purity: 99.83%
Handling Instructions

Dichlorhydrate Y-27632 est un inhibiteur de ROCK-I et de ROCK-II qui est actif par voie orale et ATP-compétitif, avec Kis de 220 et 300 nM, respectivement. Dichlorhydrate Y-27632 induit l'apoptose. Dichlorhydrate Y-27632 amorce les cellules souches pluripotentes induites par l'homme (hIPSC) pour se différencier sélectivement vers la lignée mésendodermique via une modulation de type transition épithéliale-mésenchymateuse.

Y-27632 Dihydrochlorid ist ein oral wirksamer, ATP-kompetitiver Inhibitor von ROCK-I und ROCK-II mit einem Kis-Wert von 220 bzw. 300 nM. Y-27632 Dihydrochlorid induziert apoptosis. Y-27632 Dihydrochlorid veranlasst humane induzierte pluripotente Stammzellen (hIPSCs), sich selektiv über epithelial-mesenchymale Übergangs-ähnliche Modulation in Richtung mesendodermale Abstammung zu differenzieren.

Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.

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

Y-27632 dihydrochloride Chemical Structure

Y-27632 dihydrochloride Chemical Structure

CAS No. : 129830-38-2

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Customer Review

Based on 47 publication(s) in Google Scholar

Other Forms of Y-27632 dihydrochloride:

Top Publications Citing Use of Products

Publications Citing Use of MCE Y-27632 dihydrochloride

    Y-27632 dihydrochloride 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

    Y-27632 dihydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 31;8(47):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 dihydrochloride purchased from MCE. Usage Cited in: Adv Sci. 2020 Jun 17;7(15):1903583.

    Immunofluorescence imaging of LNCaP cells treated with the Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl). After the cells are cultured on different substrates for 3 days, inhibitors are added and incubated for 24 h.

    Y-27632 dihydrochloride purchased from MCE. Usage Cited in: Adv Sci. 2020 Jun 17;7(15):1903583.

    Expression of CTC cluster-related (plakoglobin and CD44) and EMT-related (vimentin and E-cadherin, 4 days) proteins in LNCaP cells grown on different substrates after treatment with different inhibitors (Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl)).

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    Description

    Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation[1][2][3][4].

    IC50 & Target

    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].

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

    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].

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

    Molecular Weight

    320.26

    Formula

    C₁₄H₂₃Cl₂N₃O

    CAS No.

    129830-38-2

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 124 mg/mL (387.19 mM)

    DMSO : ≥ 32 mg/mL (99.92 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1225 mL 15.6123 mL 31.2246 mL
    5 mM 0.6245 mL 3.1225 mL 6.2449 mL
    10 mM 0.3122 mL 1.5612 mL 3.1225 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

    Purity: 99.83%

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    Keywords:

    Y-27632Y27632Y 27632ROCKApoptosisRho-associated protein kinaseRho-associated kinaseRho-kinaseROKorallyactiveATP-competitivepluripotentstemcellshIPSCsmesendodermallineageepithelial-mesenchymaltransition-likemodulationInhibitorinhibitorinhibit

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    Y-27632 dihydrochloride
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