(-)-Blebbistatin (GMP) 

(-)-Blebbistatin (GMP) is (-)-Blebbistatin (HY-13441) produced by using GMP guidelines. (-)-Blebbistatin (GMP) is a selective inhibitor of the ATPase activity of non-muscle myosin II^[1][2].

Blebbistatin 有效抑制多种横纹肌肌球蛋白以及脊椎动物非肌肉肌球蛋白 IIA 和 IIB，IC₅₀ 值范围为 0.5 至 5 μM。平滑肌肌球蛋白仅受到微弱抑制 (IC₅₀=80 μM)^[1]。
Blebbistatin 不与核苷酸结合到骨骼肌肌球蛋白 subfragment-1 上竞争。该抑制剂优先与 ATP 酶中间体结合，ADP 和磷酸盐结合在活性位点，并减缓磷酸盐释放。它阻断具有低肌动蛋白亲和力的产物复合物中的肌球蛋白头部^[2]。
在培养激活的肝星状细胞中，Blebbistatin 被发现可以改变细胞形态和功能。星状细胞变得更小，获得树突状形态并且具有更少的含有肌球蛋白 IIA 的应力纤维和含有纽蛋白的粘着斑。Blebbistatin 会破坏硅胶皱纹的形成，减少胶原凝胶收缩并阻断内皮素 1 诱导的细胞内 Ca²⁺ 释放。它促进伤口诱导的细胞迁移^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Blebbistatin 以剂量依赖性方式完全松弛 KCl 和卡巴胆碱诱导的大鼠逼尿肌和内皮素 1 诱导的人膀胱收缩。与 10 μM Blebbistatin 预孵育可将卡巴胆碱反应性减弱 65%，同时阻断电场刺激诱导的膀胱收缩，在 32 Hz 下达到 50% 的抑制^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

292.33

C₁₈H₁₆N₂O₂

856925-71-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Cristina Lucas‐Lopez, et al. Absolute Stereochemical Assignment and Fluorescence Tuning of the Small Molecule Tool, (–)‐Blebbistatin.

  [2]. Ponsaerts R, et al. The myosin II ATPase inhibitor blebbistatin prevents thrombin-induced inhibition of intercellularcalcium wave propagation in corneal endothelial cells. Invest Ophthalmol Vis Sci. 2008 Nov;49(11):4816-27.  [Content Brief]