(-)-Blebbistatin (GMP) 

(-)-Blebbistatin (GMP) is (-)-Blebbistatin (HY-13441) produced by using GMP guidelines. (-)-Blebbistatin (GMP) is a selective inhibitor of the ATPase activity of non-muscle myosin II^[1][2].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

292.33

C₁₈H₁₆N₂O₂

856925-71-8

CC1=CC=C(N=C(N(C2=CC=CC=C2)CC3)[C@]3(O)C4=O)C4=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]