(R)-(+)-Blebbistatin是一种细胞渗透性非肌肉肌球蛋白II ATP酶抑制剂，其IC50范围为2微米[1，2]。 非肌肉肌球蛋白II (NM II)，一种肌动蛋白结合蛋白，在细胞迁移、粘附和分化的调节中起着重要作用[4]。最近对NM II在这些过程中的重要性的深入了解通过基因缺失和突变方法得到了强调，这些方法发现NM II突变会影响多种蛋白质的功能并导致单基因疾病[5.6]。

    (R)-(+)-Blebbistatin是一种小分子抑制剂，优先与肌球蛋白-ADP-Pi复合物结合以减缓磷酸盐释放[2]。该抑制剂在体外完全消除了肌动蛋白激活Mg-ATPase活性的收缩和肌球蛋白II的运动性(IC50 = 0.5-5.0微米)[8，9]，但其对平滑肌肌球蛋白II (IC50 =80微米)和肌球蛋白I、V和X的作用较差[3]。此外，blebbistatin可有效抑制哺乳动物动脉平滑肌(IC50=5微米)[9]。blebbistatin阻断肌动蛋白分离状态的肌球蛋白II并防止刚性肌动球蛋白交联的特性在体内应用中是一个巨大的优势[2，11]。

在恒压格兰特灌注模型系统中，用blebbistatin (10-200 M)处理CB和TM细胞，细胞形态改变，肌动蛋白应力纤维含量降低。blebbistatin效应在24小时内完全可逆[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微米)。暴露于波长低于488 nm的紫外光下也可导致blebbistatin迅速被抑制。[8].

产品性质：

Cas No.:1177356-70-5

别名:(R)-Blebbistatin

化学名:(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

分子式:C18H16N2O2

分子量:292.34

溶解度:12.5mg/mL in DMSO &DMF

储存条件:Store at -20°C

注意事项：

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References:

[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.