Bioactivity | (-)-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]. |
Invitro | 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. 0 --> (-)-Blebbistatin (GMP) 相关抗体: |
In Vivo | 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. |
CAS | 856925-71-8 |
Formula | C18H16N2O2 |
Molar Mass | 292.33 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |