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(-)-Blebbistatin
| Product Name | (-)-Blebbistatin |
| Price: | Inquiry |
| Catalog No.: | CN00186 |
| CAS No.: | 856925-71-8 |
| Molecular Formula: | C18H16N2O2 |
| Molecular Weight: | 292.33 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | Cc1ccc2c(c1)C(=O)[C@]1(C(=N2)N(CC1)c1ccccc1)O |
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| Description | (-)-Blebbistatin is an S enantiomer of blebbistatin. Blebbistatin is a potent and selective myosin II inhibitor with IC50s ranging from 0.5 to 5 μM. |
| 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]. |
| Cell Assay | 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]. |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 486.7±55.0 °C at 760 mmHg |
| Flash Point | 248.1±31.5 °C |
| PSA | 52.90000 |
| LogP | 0.93 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Storage condition | Desiccate at +4°C |