(-)-Blebbistatin

Catalog No.S7099 Batch:S709905

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Technical Data

Formula

C18H16N2O2
Molecular Weight 292.33 CAS No. 856925-71-8
Solubility (25°C)* In vitro DMSO 58 mg/mL (198.4 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description (-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.
Targets
non-muscle myosin II ATPases [2]
(Cell-free assay)
0.5 μM-5 μM
In vitro

Blebbistatin, inhibits cytokinesis, alters the smooth movement of fish keratocytes and inhibits the spontaneous blebbing of a cell line lacking filamin. Blebbistatin is shown to inhibit the enzymatic activities of HMM fragments of nonmuscle myosin IIA, nonmuscle myosin IIB and of rabbit skeletal muscle myosin S1, but not smooth muscle myosin[1]

Blebbistatin rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species, while poorly inhibiting smooth muscle myosin (IC50 = 80 μM). Blebbistatin potently inhibits Dictyostelium myosin II, but poorly inhibits Acanthamoeba myosin II. Blebbistatin does not inhibit representative myosin superfamily members from classes I, V, and X. [2]

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. Blebbistatin interferes neither with binding of myosin to actin nor with ATP-induced actomyosin dissociation. Instead, it blocks the myosin heads in a products complex with low actin affinity. [3]
In vivo

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase.

Protocol (from reference)

Kinase Assay:

[2]
  • Actin-activated MgATPase assay

    Actin-activated MgATPase activity is measured using an NADH-coupled assay in a Beckman DU 640 spectrophotometer. Blebbistatin [a racemic mixture of the (+) and (-) enantiomers] is added from stocks dissolved in DMSO and the DMSO concentration is maintained at a constant concentration of 5% in all samples.
Cell Assay:

[4]
  • Cell lines

    MDCK and U2OS cells

  • Concentrations

    25 µM

  • Incubation Time

    2-4 h

  • Method

    Cells were treated with vlebbistatin for 2-4 hours.
Animal Study:

[5]
  • Animal Models

    Male Sprague–Dawley rats (TBI model)

  • Dosages

    10 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , J Leukoc Biol, 2016, 143-53]

Data from [Data independently produced by , , Biomed Res Int, 2018, 2018:2174824]

Data from [Data independently produced by , , J Vasc Res, 2016, 53(3-4):206-215]

Selleck's (-)-Blebbistatin has been cited by 55 publications

Canonical and non-canonical integrin-based adhesions dynamically interconvert [ Nat Commun, 2024, 15(1):2093] PubMed: 38453931
Cooperative sensing of mitochondrial DNA by ZBP1 and cGAS promotes cardiotoxicity [ Cell, 2023, 186(14):3013-3032.e22] PubMed: 37352855
Cooperative sensing of mitochondrial DNA by ZBP1 and cGAS promotes cardiotoxicity [ Cell, 2023, 186(14):3013-3032.e22] PubMed: 37352855
Cooperative sensing of mitochondrial DNA by ZBP1 and cGAS promotes cardiotoxicity [ Cell, 2023, 186(14):3013-3032.e22] PubMed: 37352855
Hydrogels with tunable mechanical plasticity regulate endothelial cell outgrowth in vasculogenesis and angiogenesis [ Nat Commun, 2023, 14(1):8307] PubMed: 38097553
Drug specificity and affinity are encoded in the probability of cryptic pocket opening in myosin motor domains [ Elife, 2023, 12e83602] PubMed: 36705568
Extracellular flux analysis in intact cardiac tissue slices - a novel tool to investigate cardiac substrate metabolism in mouse myocardium [ Acta Physiol (Oxf), 2023, e14004.] PubMed: 37227741
Antagonistic interactions among structured domains in the multivalent Bicc1-ANKS3-ANKS6 protein network govern phase transitioning of target mRNAs [ iScience, 2023, 26(6):106855] PubMed: 37275520
Myokine Musclin Is Critical for Exercise-Induced Cardiac Conditioning [ Int J Mol Sci, 2023, 24(7)6525] PubMed: 37047496
HER2 inhibition increases non-muscle myosin IIA to promote tumorigenesis in HER2+ breast cancers [ PLoS One, 2023, 18(5):e0285251] PubMed: 37200287

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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