(-)-BLEBBISTATIN
(-)-BLEBBISTATIN 性质
| 熔点 | 210-212°C |
|---|---|
| 沸点 | 507.3±60.0 °C(Predicted) |
| 密度 | 1.31±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 在DMSO中的溶解度为5mg/mL |
| 形态 | 黄色固体 |
| 酸度系数(pKa) | 11.15±0.20(Predicted) |
| 颜色 | 浅黄色至厚黄色 |
(-)-BLEBBISTATIN 用途与合成方法
| Target | Value |
|
non-muscle myosin II ATPases
(Cell-free assay) | 0.5 μM-5 μM |
Blebbistatin抑制细胞分裂，改变鱼角膜细胞的平滑运动，且抑制缺乏细丝蛋白的细胞系进行自发起泡。Blebbistatin抑制非肌肉肌球蛋白IIA，非肌肉肌球蛋白IIB，和兔骨骼肌肌球蛋白S1的HMM片段的酶活性，而不抑制平滑肌球蛋白。Blebbistatin快速且可逆抑制Mg-ATPase活性，也抑制非肌肉肌球蛋白IIA和IIB的体外活性，而极其微弱抑制平滑肌肌球蛋白（IC50=80 μM）。Blebbistatin有效抑制Dictyostelium肌球蛋白II，但极其微弱抑制Acanthamoeba肌球蛋白II。Blebbistatin不抑制代表性的I，V，和X型肌球蛋白超家族成员。Blebbistatin不与核苷酸竞争性结合到骨骼肌肌球蛋白亚片段-1。Blebbistatin优先结合到ATP酶，与ADP和磷酸盐在活性位点相互作用，减慢磷释放。Blebbistatin既不干扰肌球蛋白与肌动蛋白结合，也不干扰ATP诱导的肌动球蛋白解离。
Blebbistatin dose-dependently and completely relax both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction. Pre-incubation with 10 μM blebbistatin attenuates carbachol responsiveness by 65% while blocking electrical field stimulation-induced bladder contraction reaching 50% inhibition at 32 Hz.
Blebbistatin blocked myosin II-dependent cell processes. It blocks cell blebbing rapidly and reversibly. Blebbistatin also rapidly disrupted directed cell migration and cytokinesis in vertebrate cell . Blebbistatin blocks both blebbing and cytokinesis at 50-100μM. [Blebbistatin:a]D= -103 (c= 1.21 CHCl3) (-)-1-Phenyl-1,2,3,4-tetrahydro-4-hydroxypyrrolo[2,3-b]-7-methylquinolin-4-one
(-)-BLEBBISTATIN 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-13441 | (-)-BLEBBISTATIN | 856925-71-8 | 5mg | 720 |
| 2024-11-08 | S7099 | (-)-BLEBBISTATIN | 856925-71-8 | 10mg | 1385.26 |
