Molecular Formula | C18H16N2O2 |
Molar Mass | 292.33 |
Density | 1.31±0.1 g/cm3(Predicted) |
Melting Point | 210-212°C |
Boling Point | 507.3±60.0 °C(Predicted) |
Solubility | DMSO: soluble5mg/mL |
Appearance | Yellow solid |
Color | Light Yellow to Yellow |
pKa | 11.15±0.20(Predicted) |
Storage Condition | -20°C |
MDL | MFCD08460907 |
Use | (−)-Blebbistatin |
In vitro study | Blebbistatin inhibits cell division, alters the smooth movement of fish keratocytes, and inhibits the spontaneous blistering of a filamin-deficient cell line. Blebbistatin inhibited the enzymatic activity of non-muscle myosin IIA, non-muscle myosin IIB, and the HMM fragment of rabbit skeletal muscle myosin S1, but not smooth muscle globin. Blebbistatin rapidly and reversibly inhibits Mg-ATPase activity and also inhibits the in vitro activity of non-muscle myosins IIA and IIB, whereas it inhibits very weakly smooth muscle myosin (IC50=80 μm). Blebbistatin effectively inhibits Dictyostelium myosin II, but extremely weakly inhibits Acanthamoeba myosin II. Blebbistatin does not inhibit representative I,V, and X-type myosin superfamily members. Blebbistatin does not competitively bind with nucleotides to skeletal muscle myosin subfragment -1. Blebbistatin preferentially binds to ATPases, interacts with ADP and phosphate at the active site, slowing phosphorus release. Blebbistatin interfered neither with myosin binding to actin nor with ATP-induced actin dissociation. |
In vivo study | 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. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.421 ml | 17.104 ml | 34.208 ml |
5 mM | 0.684 ml | 3.421 ml | 6.842 ml |
10 mM | 0.342 ml | 1.71 ml | 3.421 ml |
5 mM | 0.068 ml | 0.342 ml | 0.684 ml |
biological activity | (-)-Blebbistatin ((S)-(-)-Blebbistatin) is a kind of cell permeability inhibitor, acting on non-myosin IIATPase, IC50 is ~ 2 μm in cell-free test, does not inhibit myosin light chain kinase (MLCK), inhibits the contraction of the cleavage groove, does not interfere with the assembly of mitotic or contractile loops. |
Target | Value |
non-muscle myosin II ATPases (Cell-free assay) | 0.5 μM-5 μM |
purpose | Blebbistatin blocked myosin II-dependent cell processes. It blocks. Blebbistatin also rapidly disrupted directed cell migration and cytolysis in vertebrate cell . Blebbistatin blocks. [Blebbistatin:a]D = -103 (c = 1.21 CHCl3) (-)-1-Phenyl-1,2,3,4-tetrahydro-4-hydroxypyrrolo[2,3-b]-7-methylquinolin-4-one |