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(-)-Blebbistatin

Catalog No. T6038   CAS 856925-71-8
Synonyms: (S)-(-)-Blebbistatin

(-)-Blebbistatin is an S enantiomer of blebbistatin. It is a potent and selective myosin II inhibitor with IC50 ranging from 0.5 to 5 μM.

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(-)-Blebbistatin, CAS 856925-71-8
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description (-)-Blebbistatin is an S enantiomer of blebbistatin. It is a potent and selective myosin II inhibitor with IC50 ranging from 0.5 to 5 μM.
Targets&IC50 non-muscle myosin II ATPases:0.5 μM-5 μM
In vivo Blebbistatin completely relaxes both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction in a dose-dependent manner. 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].
Kinase Assay Inhibition of Cox Activity: Inhibition of Cox-1 activity is measured by monitoring oxygen consumption during the conversion of arachidonic acid to PGs using a Clark-type O2-electrode. The reaction mixture contains ~0.2 units Cox-1 in 100 μL of microsome fraction derived from ram seminal vesicles as a crude source of Cox-1 (specific activity 0.2–1 units/mg protein) or 0.23 units of recombinant human Cox-2 (specific activity 43 units/mg protein). For calculation, the rate of O2 consumption is compared with a DMSO control (100% activity). Piroxicam, a nonsteroidal anti-inflammatory drug, is used as positive inhibitory substance for Cox-1 activity with an IC50 of 0.35 ± 0.05 μM (n = 2). Alternatively, nimesulide, a Cox-2 specific inhibitor, inhibits Cox-2 activity by 52 ± 5.7% (n = 2) at a concentration of 50 μM.
Cell Research 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].
Synonyms (S)-(-)-Blebbistatin
Molecular Weight 292.338
Formula C18H16N2O2
CAS No. 856925-71-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 29.2 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Straight AF, et al. Science, 2003, 299(5613), 1743-1747. 2. Limouze J, et al. J Muscle Res Cell Motil, 2004, 25(4-5), 337-341. 3. Kovács M, et al. J Biol Chem, 2004, 279(34), 35557-35563 4. Zhang X, et al. In vitro and in vivo relaxation of urinary bladder smooth muscle by the selective myosin IIinhibitor, blebbistatin. BJU Int. 2011 Jan;107(2):310-7. 5. Tian X, Gao M, Li A, et al. Protocol for Isolation of Viable Adult Rat Cardiomyocytes with High Yield[J]. STAR Protocols. 2020: 100045.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library Ion Channel Inhibitor Library Mitochondria-Targeted Compound Library Kinase Inhibitor Library Stem Cell Differentiation Compound Library Bioactive Lipid Compound Library Cardiotoxicity Compound Library Bioactive Compound Library

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Keywords

(-)-Blebbistatin 856925-71-8 离子通道 细胞骨架 ATPase Myosin inhibit Inhibitor (S)-(-)-Blebbistatin ( ) Blebbistatin ()Blebbistatin inhibitor