(-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases and the active enantiomer of (+)-blebbistatin. It rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50 = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM?).








Cat No : CM05239

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Non muscle myosin II ATPase provides contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly during the cell division completion process of cytokinesis. (-)-Blebbistatin is a cell-permeable non muscle myosin II ATPase inhibitor with IC50 of 2μM, which does not inhibit myosin light chain kinase. (-)-Blebbistatin is shown to inhibit the enzymatic activities of HMM fragments of nonmuscle myosin IIA, nonmuscle myosin IIB and of rabbit skeletal muscle myosin S1, but not smooth muscle myosin. (-)-Blebbistatin potently inhibited the activity of fast rabbit skeletal muscle S1 with a half maximal inhibition at 0.5μM concentration while Porcine b-cardiac myosin S1 and scallop striated muscle S1 were inhibited with slightly higher IC50 values of 1.2 and 2.3μM, respectively. The IC50 values for non muscle myosin IIA and IIB HMM fragments were 5.1 and 1.8 μM, respectively. In contrast, the actin activated MgATPase required considerably higher (-)-blebbistatin concentrations for inhibition (IC50 of about 80μM). No inhibition was observed with rat myosin Ib, mouse myosin Va S1 and bovine myosin X S1 at 100μM. For skeletal myosin (S1), the acto-S1 ATPase activity was almost totally inhibited with half-maximal inhibition at 0.4 ± 0.1 μM. Nevertheless, actin activated the low inhibited basal S1 ATPase even in 50μM to a maximum of 0.45±0.02 /s (about 2% of the uninhibited activity). At low concentrations, the onset of the blebbistatin-inhibited steady-state of the acto-S1 ATPase was preceded by a slow exponential phase whose observed rate constant fell between 0.02 and 0.07/s with the concentration range of 0.5–4μM, and indicated that the blebbistatin off-rate constant from S1 during ATP turnover is below. Besides, blebbistatin will bind to a nucleotide bound S1 ATPase intermediate slowly but with high affinity (Kd = 3.1± 0.8 μM) which is accompanied by a quench in both tryptophan and mant fluorescence. The inhibitor preferentially binds to the ATPase intermediate with ADP and phosphate bound at the active site, and it slows down phosphate release.

CAS号 856925-71-8
分子式 C18H16N2O2
主要靶点 Myosin
主要通路 Cytoskeleton
分子量 292.3318
MDL NO MFCD08460907
Pubchem ID 5287792.0
纯度 98%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
粉末 -20°C 3年
液体 -80°C 1年
运输条件 Shipped in cold pack
别名 (S)-(-)-Blebbistatin


Myosin IIA (non-muscle)IC50=0.5-5μM
Myosin IIB (non-muscle)IC50=0.5-5μM


DMSO46 mg/mL


剂量Mice: min = 1 mg/kg[3]


2% DMSO+40% PEG 300+5% Tween 80+water5 mg/mL

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