(-)-BlebbiSTATin 是 blebbiSTATin 的 S 对映异构体。它是一种有效的选择性肌球蛋白 II 抑制剂，IC50 范围为 0.5 至 5 μM。

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

Blebbistatin completely relaxes both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction in a dose-dependent manner. 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].

Inhibition of Cox Activity: Inhibition of Cox-1 activity is measured by monitoring oxygen consumption during the conversion of arachidonic acid to PGs using a Clark-type O2-electrode. The reaction mixture contains ～0.2 units Cox-1 in 100 μL of microsome fraction derived from ram seminal vesicles as a crude source of Cox-1 (specific activity 0.2–1 units/mg protein) or 0.23 units of recombinant human Cox-2 (specific activity 43 units/mg protein). For calculation, the rate of O2 consumption is compared with a DMSO control (100% activity). Piroxicam, a nonsteroidal anti-inflammatory drug, is used as positive inhibitory substance for Cox-1 activity with an IC50 of 0.35 ± 0.05 μM (n = 2). Alternatively, nimesulide, a Cox-2 specific inhibitor, inhibits Cox-2 activity by 52 ± 5.7% (n = 2) at a concentration of 50 μM.

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].

856925-71-8

C18H16N2O2

292.338

(S)-(-)-Blebbistatin

DMSO:29.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years