(-)-Blebbistatin

产品信息

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
储存条件	粉末 -20°C 3年 液体 -80°C 1年
运输条件	Shipped in cold pack
别名	(S)-(-)-Blebbistatin

靶点

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

溶解度

DMSO	46 mg/mL
Water	insoluble

动物研究

剂量	Mice: min = 1 mg/kg[3]
给药途径	i.p.

动物实验配方

Administration	Formulation	Solubility	Status
	2% DMSO+40% PEG 300+5% Tween 80+water	5 mg/mL