Hydroxy-Dynasore是一种抑制动力蛋白 1 和 2 的抑制剂,IC50 分别为 0.38 μM 和 2.6 µM,能够防止多种细胞类型中的动力蛋白介导的内吞作用。
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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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| 产品名称 | Dynamin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Dynasore |
++
Dynamin1/2, IC50: ~15 μM |
98% | |||||||||||||||||
| Mdivi-1 | 99%+ | ||||||||||||||||||
| Hydroxy-Dynasore |
++++
DynI (brain), IC50: 0.38 μM DynI (rec), IC50: 2.3 μM |
99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Dynamin is a large GTPase enzyme that severs membrane‐bound clathrin‐coated vesicles. Dyngo-4a inhibits both dynamin I and II with IC50s for sheep brain dynamin I of 380 ± 0.05 nM (n = 5) and for recombinant rat dynamin II of 2.3 ± 0.2 μM (n = 3). It inhibits dynamin‐dependent endocytosis of transferrin in multiple cell types with IC50 value of 5.7 μM. Inhibition of non‐neuronal clathrin‐mediated endocytosis (CME) was observed with as little as 5‐min preincubation with 10 μM Dyngo-4a in U2OS cells. 70% of normal non‐neuronal CME levels was observed at ten minutes after the removal of 10 μM 4a indicating its endocytic block activity was rapid and reversible [3]. The ability of Dyngo-4a to prevent the muscle paralysis induced by purified BoNT/A was tested in a rat hemidiaphragm twitch model. Both the decline in contraction and the time to reach 50% of decline were significantly increased in the Dyngo-4a-treated muscles compared with the BoNT/A control group demonstrating that Dyngo-4a provides significant protection against BoNT/A-induced muscle paralysis. CD-1 mice were given an intraperitoneal injection of Dyngo-4a (1 mg) or vehicle followed by a booster 4.5–8 h later. Mice injected with Dyngo-4a took significantly longer to exhibit clear signs of botulism, 860 ± 65 min compared with 656 ± 55 min indicating that Dyngo-4a pretreatment provides significant protection against botulism [4]. |
| Concentration | Treated Time | Description | References | |
| Neuro2A cells | 30 µM | 30 minutes | Inhibited OGD-induced KOR internalization | Anesthesiology. 2017 May;126(5):842-854. |
| HEK293 cells | 30 µM | 15 min | To assess the effects of Dyngo on β2-AR internalization and cAMP accumulation. | Nat Chem Biol. 2014 Dec;10(12):1061-5. |
| Rat Mesenchymal Stem Cells | 20 µM | 15 minutes | To investigate the effect of Dyngo-4a on the internalization of S100B-Alexa488, results showed that Dyngo-4a significantly reduced the number and mean fluorescence intensity of S100B-Alexa488-positive vesicles. | Front Cell Dev Biol. 2021 Jul 26;9:674995. |
| Xenopus laevis oocytes | 10 µM | 20 hours | Dyngo-4a significantly increased TMEM175 currents, indicating that it enhanced the expression of TMEM175 on the plasma membrane by inhibiting dynamin. | Int J Mol Sci. 2021 Sep 29;22(19):10515. |
| HEK293T cells | 80 µM | 20 hours | Dynasore increased the expression of TMEM175 on the plasma membrane, validating its functional expression on the cell surface. | Int J Mol Sci. 2021 Sep 29;22(19):10515. |
| Human foreskin keratinocytes (HFK) | 10 µM | 24 hours | Dyngo-4a-treated shIRF6 keratinocytes showed increased levels of E-cadherin at the membrane to the levels of the wild-type cells. | J Invest Dermatol. 2022 Feb;142(2):314-322. |
| HUVECs | 30 µM | 30 minutes | To evaluate the effect of dyngo 4a on VEGFR2 internalization and signaling, results showed that dyngo 4a significantly inhibited VEGFR2 phosphorylation. | Cells. 2021 Apr 23;10(5):997. |
| Inner hair cells (IHCs) | 30 µM | Pharmacological intervention with dynamin-mediated endocytosis; no significant effect observed on cumulative exocytic ΔCm. | J Neurosci. 2014 Jan 15;34(3):705-16. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.96mL 0.59mL 0.30mL |
14.78mL 2.96mL 1.48mL |
29.56mL 5.91mL 2.96mL |
|
| CAS号 | 1256493-34-1 |
| 分子式 | C18H14N2O5 |
| 分子量 | 338.31 |
| SMILES Code | O=C(N/N=C/C1=CC(O)=C(O)C=C1O)C2=C(O)C=C3C=CC=CC3=C2 |
| MDL No. | MFCD23704787 |
| 别名 | Dyngo-4a |
| 运输 | 蓝冰 |
| 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: 50 mg/mL(147.79 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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