|N'-(3,4-二羟基亚苄基)-3-羟基-2-萘甲酰肼|CsnPharm

CAS No.: 304448-55-3

Dynasore/3-羟基-萘-2-羧酸（3,4-二羟基-亚苄基）-酰肼 Catalog No. CSN17241

Synonyms: Dynasore

Dynasore is an inhibitor of the GTPase activity of dynamin with an IC50 of 15 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Dynamin1/2

IC50:15μM
描述Dynamin is a GTPase responsible for clathrin-coated vesicle formation in endocytosis. Dynasore acts as a noncompetitive inhibitor of dynamin1 and dynamin2 in vitro with an IC50 of 15 μM. Dynasore at 80 μM inhibits the enzymatic activity of mitochondrial dynamin Drp1 at ambient temperature. The pre-incubation of 80 μM dynasore for 30 min inhibited the uptake, trafficking, and intracellular accumulation of transferrin in HeLa cells. The blockage of transferrin uptake by dynasore in HeLa cells is dose-dependent with an IC50 of ~15 μM. The treatment of 80 μM dynasore for 30 min in Hela cells also strongly blocked the receptor-mediated endocytosis of low density lipoprotein (LDL), as demonstrated by the internalization and endosomal accumulation of Alexa-546 LDL. When HeLa cells were loaded with 200 μg/mL LDL for 24 hours followed by 6-hour incubation with 80 μM dynasore, both the number and the size of endosomal structures loaded with Dil-AcLDL were increased. Under the same condition, dynasore also decreased the production of cholesterol esters that were induced by the pre-incubation of LDL. When HeLa cells underwent sterol starvation for 48 hours followed by the incubation of 200 μg/mL LDL and 80 μM dynasore, LDL-induced suppression of HMGCoAR expression were largely inhibited. The treatment of 80 μM dynasore and 100 μg/mL AcLDL on human monocytes-derived macrophages resulted in a significant reduction of cholesterol efflux to apoA-1 (40%) and HDL (70%).
作用机制Dynasore acts as a noncompetitive inhibitor of dynamin by blocking the basal and stimulated rates of GTP hydrolysis mediated by isolated GTPase domain of dynamin, thereby impeding clathrin-mediated endocytosis in cells.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
COS7 cells	-	Function assay	-	Inhibition of transferrin uptake in african green monkey COS7 cells by microscopic TexasRed imaging, IC50=15 μM	20621477

动物研究
剂量
Mice: 10 mg/kg^[3] (s.c.); 1 mg/kg^[4] (i.p.), 30 mg/kg^[5] (i.p.)

给药途径
s.c., i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[3] (s.c.); 1 mg/kg^[4] (i.p.), 30 mg/kg^[5] (i.p.)
给药途径	s.c., i.p.

[1] Mues MB, Cheshenko N, et al. Dynasore disrupts trafficking of herpes simplex virus proteins. J Virol. 2015 Jul;89(13):6673-8
[2] Macia E, Ehrlich M,et al. Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006 Jun;10(6):839-50.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1026 mL
- 15.5128 mL
- 31.0256 mL
- 5 mM
- 0.6205 mL
- 3.1026 mL
- 6.2051 mL
- 10 mM
- 0.3103 mL
- 1.5513 mL
- 3.1026 mL

技术信息

CAS号

304448-55-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H14N2O4

运输

蓝冰

分子量

322.31

别名

Dynasore

溶解度

DMSO	200.0 mg/mL (620.5 mM)
Water	insoluble

动物实验配方

5% DMSO+30% PEG 300+5% Tween 80+water

4 mg/mL

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Dynasore/3-羟基-萘-2-羧酸（3,4-二羟基-亚苄基）-酰肼 Catalog No. CSN17241

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