Dynarrestin是一种氨基噻唑类细胞质动力蛋白 1 和 2 的抑制剂,可快速且可逆地抑制体外动力蛋白 1 驱动的微管滑行,并在不影响 ATP 水解或干扰纤毛生成的情况下抑制细胞中的多种动力蛋白依赖过程。


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| 描述 | Dynarrestin is an aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits microtubule gliding driven by dyneins 1 in vitro, as well as a range of intracellular processes dependent on dyneins 1 and 2, without affecting ATP hydrolysis or interfering with ciliogenesis. Dynarrestin inhibits Hh-dependent proliferation of neuronal precursors and tumour cells[1]. |
| Concentration | Treated Time | Description | References | |
| NIH3T3 cells | 1 μM | 8 hours | Evaluate Smo trafficking, found Smo accumulated in cilia | Cell Chem Biol. 2018 Apr 19;25(4):357-369. e6 |
| IMCD3 cells | 25 μM | Evaluate endomembrane translocation, found movement was profoundly inhibited | Cell Chem Biol. 2018 Apr 19;25(4):357-369. e6 | |
| Cos7 cells | 25 μM | 60 minutes | Evaluate endomembrane translocation, found long-range, bidirectional movement was profoundly inhibited | Cell Chem Biol. 2018 Apr 19;25(4):357-369. e6 |
| mouse hippocampal neurons | 100 μM or 200 μM | 30 minutes | Investigated the effect of dynarrestin on synaptic cargo transport, finding that dynarrestin decreased the FPU for retrograde transport more than for anterograde transport. | Biophys J. 2021 May 4;120(9):1605-1614 |
| Administration | Dosage | Frequency | Description | References | ||
| Mouse | Ptch−/+ medulloblastoma model | In vitro culture | 0.35 μM | Evaluate tumor cell proliferation inhibition, found Dynarrestin inhibits Hh-dependent tumor cell proliferation | Cell Chem Biol. 2018 Apr 19;25(4):357-369. e6 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.32mL 0.46mL 0.23mL |
11.59mL 2.32mL 1.16mL |
23.17mL 4.63mL 2.32mL |
|
| CAS号 | 2222768-84-3 |
| 分子式 | C22H23F2N3O2S |
| 分子量 | 431.5 |
| SMILES Code | O=C(C1=C(C2=CC=C(N(CC)CC)C=C2)N=C(NC3=CC=C(F)C=C3F)S1)OCC |
| MDL No. | MFCD32174341 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | UZNNDDDSGCMQOQ-UHFFFAOYSA-N |
| Pubchem ID | 137919864 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 85 mg/mL(196.99 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
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