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(-)-Blebbistatin

(-)-Blebbistatin ((S)-(-)-Blebbistatin) 是 blebbistatin 的 S 对映异构体。(-)-Blebbistatin 是一种肌球蛋白 II 抑制剂 (IC50=0.5-5 μM)，具有有效性和选择性。(-)-Blebbistatin 可以用于抑制心肌肌球蛋白、非肌肉肌球蛋白II和骨骼肌肌球蛋白。

CAS号

856925-71-8

分子式

C18H16N2O2

主要靶点

Myosin|ATPase

仅限科研使用

Cat No : CM05239

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Synonyms

Inhibitor|inhibit|non-muscle myosin II ATPases|Myosin|()Blebbistatin|( ) Blebbistatin|(S)-(-)-Blebbistatin|Blebbistatin

验证数据展示

  • CAS No.: 856925-71-8

    (-)-Blebbistatin
    CAS#: 856925-71-8

产品信息

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is the S enantiomer of blebbistatin. (-)-Blebbistatin is a potent and selective myosin II inhibitor (IC50=0.5-5 μM). (-)-Blebbistatin can be used to inhibit cardiac myosin, non-muscle myosin II, and skeletal muscle myosin.

CAS号 856925-71-8
分子式 C18H16N2O2
主要靶点 Myosin|ATPase
主要通路 离子通道|细胞骨架
分子量 292.33
纯度 99.61%， 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 Store at low temperature,Keep away from moisture,Keep away from direct sunlight Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature.
别名 Inhibitor|inhibit|non-muscle myosin II ATPases|Myosin|()Blebbistatin|( ) Blebbistatin|(S)-(-)-Blebbistatin|Blebbistatin

靶点活性

non muscle myosin II ATPase (cell-free assays):2 μM|Smooth muscle myosin:80 μM|Non-muscle myosin II ATPases:0.5 μM-5 μM

体内活性

方法：为研究对动脉血栓形成的作用，将 (-)-Blebbistatin (1 mg/kg) 腹腔注射给 C57BL/6J 小鼠，30 min 后用 FeCl3 构建颈动脉血栓形成模型。 结果：(-)-Blebbistatin 通过小鼠动脉血管组织中的 GSK3β-NF-κB 信号通路，显著减少 FeCl3 溶液诱导的小鼠颈动脉血栓形成，抑制 NMMHC IIA 的表达并阻碍 TF 的表达。[3]

体外活性

方法：小鼠肝星状细胞 HSCs 用 (-)-Blebbistatin (12.5-50 µM) 处理 2 h，使用 microscopy 观察细胞形态。 结果：当用 (-)-Blebbistatin 处理 2 h，细胞变得更小，获得更多的树突形态，并且具有更少的应力纤维和片状足。[1] 方法：猪 TM 细胞用 (-)-Blebbistatin (25-100 µM) 处理 2 h，使用 Western Blot 检测靶点蛋白表达水平。 结果：对照样品和药物处理样品之间的 MLC 磷酸化状态没有差异。[2]

溶解度

DMSO:105 mg/mL (359.18 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.93 mg/mL (10.02 mM)

细胞实验

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].

参考文献

1.Liu Z, et al. Blebbistatin inhibits contraction and accelerates migration in mouse hepatic stellate cells. Br J Pharmacol. 2010 Jan 1;159(2):304-15.
2.Zhang M, et al. Blebbistatin, a novel inhibitor of myosin II ATPase activity, increases aqueous humor outflow facility in perfused enucleated porcine eyes. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4130-8.
3.Zhang Y, et al. The Myosin II Inhibitor, Blebbistatin, Ameliorates FeCl3-induced Arterial Thrombosis via the GSK3β-NF-κB Pathway. Int J Biol Sci. 2017 May 15;13(5):630-639.
4.Zhang X, et al. In vitro and in vivo relaxation of urinary bladder smooth muscle by the selective myosin IIinhibitor, blebbistatin. BJU Int. 2011 Jan;107(2):310-7.
5.Tian X, Gao M, Li A, et al. Protocol for Isolation of Viable Adult Rat Cardiomyocytes with High Yield[J]. STAR Protocols. 2020: 100045.

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