Y-27632 (dihydrochloride) [129830-38-2]

Katalog-Nummer HY-10583-50mg

Size : 50mg

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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 and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.

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Y-27632 dihydrochloride Chemische Struktur

CAS. Nr. : 129830-38-2

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WB
IF
    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.
    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)).
    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
    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.
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    Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.

    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 (1-5 μM; 0-60 min) promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs) .
    Y-27632 (1-5 μM; 0-60 min) induces the expression of NSE, MAP-2 and nestin in ADSCs .

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

    Western Blot Analysis

    Cell Line: Adipose tissue-derived stem cells (ADSCs)
    Concentration: 20 μM
    Incubation Time: 24 hours
    Result: Resulted in the up-regulation of NSE, MAP-2 and nestin protein levels by 25.3, 3.1 and 2.5 fold, respectively, compared to control cells not treated by Y-27632.
    In Vivo

    Y-27632 (oral gavage; 30 mg/kg; once daily; 4 w) prevents dimethylnitrosamine-induced hepatic fibrosis in rats.
    Y-27632 (oral gavage; 5-10 mg/kg; once) shows antiepileptic effects in epilepsy induced by PTZ and MES.

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

    Animal Model: Male Wistar rats injected with dimethylnitrosamine
    Dosage: 30 mg/kg
    Administration: Oral gavage; 30 mg/kg; once daily; 4 weeks
    Result: Decreased the occurrence of dimethylnitrosamine-induced hepatic fibrosis and reduced the collagen and hydroxyproline content and α-smooth muscle actin expression in the liver.
    Animal Model: Male Swiss albino mice injected with PTZ (pentylenetetrazole) or induced by MES (maximal electroconvulsive shock)
    Dosage: 5-10 mg/kg
    Administration: Oral gavage; 5-10 mg/kg; once
    Result: Prolonged the onset time of myoclonic jerks when compared with those observed in the saline group (P<0.05).
    Prolonged the onset time of clonic convulsions when compared with saline group (P<0.05).
    Prevented the occurrence of tonic hindlimb extensions and death.

    320.26

    C14H23Cl2N3O

    129830-38-2

    Solid

    White to off-white

    O=C([C@@H]1CC[C@]([C@H](N)C)(16)CC1)NC2=CC=NC=C2.16Cl.16Cl

    Room temperature in continental US; may vary elsewhere.

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    In Vitro: 

    H2O : 100 mg/mL (312.25 mM; Need ultrasonic)

    DMSO : 33.33 mg/mL (104.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molaritätsrechner

    • Verdünnungsrechner

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 3

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 4

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 1.25 mg/mL (3.90 mM); Clear solution

    • Protocol 5

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.25 mg/mL (3.90 mM); Clear solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 220 mg/mL (686.94 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    • [1]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.  [Content Brief]

      [2]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.  [Content Brief]

      [3]. 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.  [Content Brief]

      [4]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.  [Content Brief]

    • [1]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.

      [2]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.

      [3]. 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.

      [4]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 3.1225 mL 15.6123 mL 31.2246 mL 78.0616 mL
    5 mM 0.6245 mL 3.1225 mL 6.2449 mL 15.6123 mL
    10 mM 0.3122 mL 1.5612 mL 3.1225 mL 7.8062 mL
    15 mM 0.2082 mL 1.0408 mL 2.0816 mL 5.2041 mL
    20 mM 0.1561 mL 0.7806 mL 1.5612 mL 3.9031 mL
    25 mM 0.1249 mL 0.6245 mL 1.2490 mL 3.1225 mL
    30 mM 0.1041 mL 0.5204 mL 1.0408 mL 2.6021 mL
    40 mM 0.0781 mL 0.3903 mL 0.7806 mL 1.9515 mL
    50 mM 0.0624 mL 0.3122 mL 0.6245 mL 1.5612 mL
    60 mM 0.0520 mL 0.2602 mL 0.5204 mL 1.3010 mL
    80 mM 0.0390 mL 0.1952 mL 0.3903 mL 0.9758 mL
    100 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7806 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
    • Organoid ROCK
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Y-27632129830-38-2Y27632Y 27632OrganoidROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKantiepileptic effectadipose tissue-derived stem cellsADSCsInhibitorinhibitorinhibit

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    Y-27632 dihydrochloride
    Art. -Nr.:
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