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

Y-27632 dihydrochloride 

製品番号: HY-10583 純度: 99.83%
取扱説明書

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

Y-27632 dihydrochloride 構造式

Y-27632 dihydrochloride 構造式

CAS 番号 : 129830-38-2

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 55 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 210 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 350 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 550 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 1150 在庫あり
Estimated Time of Arrival: December 31
1 g USD 1650 在庫あり
Estimated Time of Arrival: December 31
2 g USD 2650 在庫あり
Estimated Time of Arrival: December 31
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 40 publication(s) in Google Scholar

Other Forms of Y-27632 dihydrochloride:

Top Publications Citing Use of Products

    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 20.

    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 20.

    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)).

    ROCK アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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)

    体外実験

    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].

    体内実験

    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].

    分子量

    320.26

    分子式

    C₁₄H₂₃Cl₂N₃O

    CAS 番号

    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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.
    参考文献
    キナーゼ実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.83%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • モル濃度カルキュレーター

    • 希釈カルキュレーター

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

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

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

     

    タイトル

    お名前 *

     

    PC 用メールアドレス *

    電話番号 *

     

    勤務先/学校名 *

    国会或いは地域 *

     

    カスタマ需要量 *

    必ず会社名を記載ください。個人への返信は行いません。

    メッセージ

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Y-27632 dihydrochloride
    製品番号:
    HY-10583
    数量:
    MCE 日本正規代理店: