2. Cytoskeleton
  3. Myosin
  4. (-)-Blebbistatin

(-)-Blébbistatine est un inhibiteur de l'activité ATPase de la myosine II non musculaire.

(-)-Blebbistatin ist ein Inhibitor der ATPase-Aktivität von Nicht-Muskel-myosin II.

(-)-Blebbistatin is a selective inhibitor of the ATPase activity of non-muscle myosin II.

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

(-)-Blebbistatin Chemical Structure

(-)-Blebbistatin Chemical Structure

CAS No. : 856925-71-8

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of (-)-Blebbistatin:

(-)-Blebbistatin Related Antibodies

Top Publications Citing Use of Products

    (-)-Blebbistatin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.  [Abstract]

    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)).

    (-)-Blebbistatin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.  [Abstract]

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    (-)-Blebbistatin is a selective inhibitor of the ATPase activity of non-muscle myosin II[1][2].

    IC50 & Target

    IC50: 0.5 to 5 μM (myosin II)[1]
    In Vitro

    Blebbistatin potently inhibits several striated muscle myosins as well as vertebrate nonmuscle myosin IIA and IIB with IC50 values ranging from 0.5 to 5 μM. Smooth muscle myosin is only poorly inhibited (IC50=80 μM)[1]. Blebbistatin does not compete with nucleotide binding to the skeletal muscle myosin subfragment-1. The inhibitor preferentially binds to the ATPase intermediate with ADP and phosphate bound at the active site, and it slows down phosphate release. It blocks the myosin heads in a products complex with low actin affinity[2]. In culture-activated hepatic stellate cells, blebbistatin is found to change both cell morphology and function. Stellate cells become smaller, acquire a dendritic morphology and have less myosin IIA-containing stress fibres and vinculin-containing focal adhesions. Blebbistatin impairs silicone wrinkle formation, reduces collagen gel contraction and blocks endothelin-1-induced intracellular Ca2+ release. It promotes wound-induced cell migration[3].

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

    (-)-Blebbistatin Related Antibodies
    In Vivo

    Blebbistatin dose-dependently and completely relax both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction. Pre-incubation with 10 μM blebbistatin attenuates carbachol responsiveness by 65% while blocking electrical field stimulation-induced bladder contraction reaching 50% inhibition at 32 Hz[4].

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

    292.33

    Formula

    C18H16N2O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC1=CC=C(N=C(N(C2=CC=CC=C2)CC3)[C@]3(O)C4=O)C4=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (34.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4208 mL 17.1040 mL 34.2079 mL
    5 mM 0.6842 mL 3.4208 mL 6.8416 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    • Molarity Calculator

    • Dilution Calculator

    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 In Vitro approach 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: ≥ 1 mg/mL (3.42 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: 1 mg/mL (3.42 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *The compound is unstable in solutions, freshly prepared is recommended.

    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.42%

    COA (256 KB) HNMR (180 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    Freshly isolated HSCs are replated on 96-well plate. At day 3, medium is replaced by serum-free medium and cells are starved overnight, treated with or without blebbistatin (25 μM) for 2 h followed by stimulation with platelet-derived growth factor-BB (20 ng/mL). After an overnight incubation, the WST-1 cell proliferation assay are performed[3].

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.4208 mL 17.1040 mL 34.2079 mL 85.5198 mL
    5 mM 0.6842 mL 3.4208 mL 6.8416 mL 17.1040 mL
    10 mM 0.3421 mL 1.7104 mL 3.4208 mL 8.5520 mL
    15 mM 0.2281 mL 1.1403 mL 2.2805 mL 5.7013 mL
    20 mM 0.1710 mL 0.8552 mL 1.7104 mL 4.2760 mL
    25 mM 0.1368 mL 0.6842 mL 1.3683 mL 3.4208 mL
    30 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8507 mL
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    (-)-Blebbistatin Related Classifications

    Help & FAQs
    • 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:

    (-)-Blebbistatin856925-71-8MyosinInhibitorinhibitorinhibit

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