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Dynasore (Dynamin Inhibitor I) 是一种高选择性、可逆的小分子动力蛋白(Dynamin)抑制剂,其 IC50 为 15 μM。Dynasore 同时可以抑制线粒体动力蛋白 Drp1,而对其他小 GTPase 没有影响。Dynasore 通过抑制 Dynamin 的 GTP 酶活性,阻断其在膜裂解过程中的功能,从而抑制网格蛋白介导的内吞作用(clathrin-mediated endocytosis)。Dynasore 可用于细胞内吞、膜转运、病毒入侵、受体信号调控等领域研究。
别名 Dynamin Inhibitor I
Dynasore (Dynamin Inhibitor I) 是一种高选择性、可逆的小分子动力蛋白(Dynamin)抑制剂,其 IC50 为 15 μM。Dynasore 同时可以抑制线粒体动力蛋白 Drp1,而对其他小 GTPase 没有影响。Dynasore 通过抑制 Dynamin 的 GTP 酶活性,阻断其在膜裂解过程中的功能,从而抑制网格蛋白介导的内吞作用(clathrin-mediated endocytosis)。Dynasore 可用于细胞内吞、膜转运、病毒入侵、受体信号调控等领域研究。


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| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 163 | 现货 | |
| 5 mg | ¥ 359 | 现货 | |
| 10 mg | ¥ 578 | 现货 | |
| 25 mg | ¥ 1,070 | 现货 | |
| 50 mg | ¥ 1,860 | 现货 | |
| 100 mg | ¥ 2,630 | 现货 | |
| 200 mg | ¥ 3,960 | 待询 | |
| 500 mg | ¥ 6,360 | 待询 | |
| 1 mL x 10 mM (in DMSO) | ¥ 638 | 现货 |
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| 产品描述 | Dynasore (Dynamin Inhibitor I) is a highly selective, reversible small-molecule dynamin inhibitor with an IC₅₀ of 15 μM. Dynasore also inhibits the mitochondrial dynamin Drp1 without affecting other small GTPases. By inhibiting the GTPase activity of dynamin, Dynasore blocks its function in membrane fission, thereby inhibiting clathrin-mediated endocytosis. Dynasore can be used in research on endocytosis, membrane transport, viral entry, and receptor signaling regulation. |
| 靶点活性 | Dynamin1/2:15 μM, moderate potenc:~15 μM (vitro) |
| 体外活性 | 方法:小鼠骨髓来源巨噬细胞加入 5, 10, 25, 50 μM Dynasore 预处理 1 小时,然后用 100 ng/mL LPS 刺激 24 小时,收集上清和细胞裂解液。实时定量 PCR 检测促炎细胞因子表达水平。 |
| 体内活性 | 方法:C57BL/6J 小鼠通过气管内滴注 LPS(10 mg/kg) 建立 ALI 模型,Dynasore (10, 30, 50 mg/kg)在 LPS 刺激前 3 小时通过腹腔注射单次给药预处理,LPS 刺激 24 小时后处死小鼠。 |
| 激酶实验 | RIP1 kinase assay: Phosphorylation of RIP1 requires its kinase activity. Expression constructs of FLAGtagged wild-type (WT) or a kinase-inactive point mutant of RIP1 (K45M) are are transfected into 293T cells and RIP1 kinase assay is performed as described in the Methods in the presence of [γ-32P]ATP for 30 min at 30℃. Samples are subjected to SDS-PAGE and RIP1 band is visualized by autoradiography. Relative intensities of radioactive bands are quantified and are shown (ratio) in this and all other autoradiographs. In parallel to kinase reactions, a sample of beads is subjected to western blot analysis using anti-RIP1 antibody to ensure equal protein amounts in kinase reactions. |
| 细胞实验 | Mouse ventricular myocytes are isolated from male adult C6/Black mouse. Cardiomyocytes subjects to 2 hours of drug treatment followed by oxidative stress (30 μM Water2 for 35 min). For ATP supplement experiments, the cells are treated with 3 mM ATP for 30 min before exposure to Water2. Cardiomyocyte survival and viability are analyzed by trypan blue exclusion (TBE) assay[3]. |
| 别名 | Dynamin Inhibitor I |
| 分子量 | 322.31 |
| 分子式 | C18H14N2O4 |
| CAS No. | 304448-55-3 |
| Smiles | Oc1ccc(C=NNC(=O)c2cc3ccccc3cc2O)cc1O |
| 密度 | 1.36g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 | ||||||||||||||||||||||||||||||||||||||||
| 溶解度信息 | Ethanol: 1.6 mg/mL (4.96 mM), Sonication is recommended. DMSO: 120 mg/mL (372.31 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (12.41 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。 | |||||||||||||||||||||||||||||||||||||||||
对于不同动物的给药剂量换算,您也可以参考 更多