| Bioactivity | (-)-Blebbistatin is a selective inhibitor of the ATPase activity of non-muscle myosin II[1][2]. |
| Target | IC50: 0.5 to 5 μM (myosin II) |
| Invitro | 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]. |
| Name | (-)-Blebbistatin |
| CAS | 856925-71-8 |
| Formula | C18H16N2O2 |
| Molar Mass | 292.33 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
| Reference | [1]. Cristina Lucas‐Lopez, et al. Absolute Stereochemical Assignment and Fluorescence Tuning of the Small Molecule Tool, (–)‐Blebbistatin. [2]. Ponsaerts R, et al. The myosin II ATPase inhibitor blebbistatin prevents thrombin-induced inhibition of intercellularcalcium wave propagation in corneal endothelial cells. Invest Ophthalmol Vis Sci. 2008 Nov;49(11):4816-27. |