(-)-Blebbistatin
CAS No. : 856925-71-8

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  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: (-)-Blebbistatin; (S)-(-)-Blebbistatin
Cat. No. : CS-4983
CAS No. : 856925-71-8
Formula: C18H16N2O2
M. Wt. : 292.33
Solubility: DMSO: 5.2 mg/mL (Need ultrasonic and warming)

Activity:

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

Protocol:

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].

References:

Liu Z, et al. Blebbistatin inhibits contraction and accelerates migration in mouse hepatic stellate cells. Br J Pharmacol. 2010 Jan 1;159(2):304-15.

Kovács M, et al. Mechanism of blebbistatin inhibition of myosin II. J Biol Chem. 2004 Aug 20;279(34):35557-63.

Limouze J, et al. Specificity of blebbistatin, an inhibitor of myosin II. J Muscle Res Cell Motil. 2004;25(4-5):337-41.

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.

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