| CAS NO: | 1177356-70-5 |
| 包装: | 1mg |
| 市场价: | 3760元 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 292.34 |
| Cas No. | 1177356-70-5 |
| Formula | C18H16N2O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | (R)-3a-hydroxy-6-methyl-1-phenyl-3,3a-dihydro-1H-pyrrolo[2,3-b]quinolin-4(2H)-one |
| Canonical SMILES | O[C@]12CCN(C3=CC=CC=C3)C1=NC4=CC=C(C)C=C4C2=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
(R)-(+)-Blebbistatin是一种细胞可透过性的非肌肉肌球蛋白II型ATP酶抑制剂,IC50值为2 μM [1,2].
非肌肉肌球蛋白II(NM II)是一种肌动蛋白结合蛋白,在调节细胞迁移\黏附及分化中发挥主要作用[4].用基因缺失和突变的方法更加证实了NM II在这些过程中的重要性,NM II突变影响了大范围的蛋白功能,且引发单基因病[5.6].
(R)-(+)-Blebbistatin是一种小分子抑制剂,与肌球蛋白-ADP-Pi复合体优先结合以放慢磷酸盐的释放[2].该抑制剂完全消除肌动蛋白激活的Mg-ATP酶的收缩活性和体外几种物种的肌球蛋白II的运动性(IC50 = 0.5-5.0 μM) [8,9],但是,它对平滑肌肌球蛋白II (IC50 =80 μM)\肌球蛋白I\V及X的效果差[3].此外,blebbistatin能够强效抑制哺乳动物动脉平滑肌(IC50=5 μM) [9].在体内应用中,blebbistatin所具有的阻滞处于肌动蛋白分离状态的肌球蛋白II及阻止刚性肌动球蛋白交联的特性是一个巨大优势[2,11].
在恒压灌注模型系统中,CB和TM细胞用blebbistatin (10-200 M)处理后,细胞形态有所变化,肌动蛋白应力纤维含量减少.经过24小时的冲刷,Blebbistatin效果是完全可逆的[10].Blebbistatin抑制单细胞收缩而不改变细胞内钙瞬变的形态(IC50 = 0.43 μM).暴露于波长小于488 nm的紫外光下也可迅速抑制blebbistatin[8].
参考文献：
[1]. Straight AF, Cheung A, Limouze J, et al. Dissecting temporal and spatial control of cytokinesis with a myosin II Inhibitor. Science, 2003, 299:1743–1747.
[2]. Kovacs M, Toth J, Hetenyi C, Malnasi-Csizmadia A, Sellers JR. Mechanism of blebbistatin inhibition of myosin II. J Biol Chem, 2004, 279:35557–35563.
[3]. Limouze J, Straight AF, Mitchison T, Sellers JR. Specificity of blebbistatin, an inhibitor of myosin II. J Muscle Res Cell Motil, 2004, 25:337–341.
[4]. Miguel Vicente-Manzanares, Xuefei Ma, Robert S. Adelstein,Alan Rick Horwitz. Non-muscle myosin II takes centre stage in cell adhesion and migration.Nat Rev Mol Cell Biol, 2009 Nov, 10(11): 778–790.
[5]. Burt RA, Joseph JE, Milliken S, Collinge JE, Kile BT. Description of a novel mutation leading to MYH9-related disease. Thrombosis Research, 2008, 122(6): 861-863.
[6]. Butcher DT, Alliston T, Weaver VM. A tense situation: forcing tumour progression. Nature Reviews Cancer, 2009 Feb, 9(2):108-122.
[7]. Chen Y, Boukour S, Milloud R, Favier R, Saposnik B, Schlegel N, et al. The abnormal proplatelet formation in MYH9-related macrothrombocytopenia results from an increased actomyosin contractility and is rescued by myosin IIA inhibition. Journal of thrombosis and haemostasis : JTH , 2013, 11:2163-2175.
[8]. Fedorov VV, Lozinsky IT, Sosunov EA, Anyukhovsky EP, Rosen MR, Balke CW, et al. Application of blebbistatin as an excitation-contraction uncoupler for electrophysiologic study of rat and rabbit hearts. Heart rhythm: the official journal of the Heart Rhythm Society, 2007, 4:619-626.
[9]. Zhang X-h, Aydin M, Kuppam D, Melman A, DiSanto ME. In Vitro and In Vivo Relaxation of Corpus Cavernosum Smooth Muscle by the Selective Myosin II Inhibitor, Blebbistatin. The Journal of Sexual Medicine, 2009, 6:2661-2671.
[10]. Zhang M, Rao PV. Blebbistatin, a novel inhibitor of myosin II ATPase activity, increases aqueous humor outflow facility in perfused enucleated porcine eyes. Investigative ophthalmology & visual science, 2005, 46:4130-4138.
[11]. Lucas-Lopez C, Allingham JS, Lebl T, Lawson CP, Brenk R, Sellers JR, et al. The small molecule tool (S)-(-)-blebbistatin: novel insights of relevance to myosin inhibitor design.
Organic & biomolecular chemistry, 2008, 6:2076-2084.
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