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Dynasore

カタログ番号GC10395

ジナソアはGTPase阻害剤として、迅速かつ可逆的にダイナミン活性を抑制し、内向き輸送を防止します。

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Dynasore 化学構造

Cas No.: 304448-55-3

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$50.00
在庫あり
10mg
$53.00
在庫あり
25mg
$103.00
在庫あり
100mg
$302.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 3 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Human OS cell lines (MNNG/HOS, MG-63, and U2-OS)

Preparation Method

Human OS cell lines (MNNG/HOS, MG-63, and U2-OS) were treated with increasing concentrations of dynasore or cisplatin (0 - 100 µM), and then the cell viability was assessed by CCK-8 kit at 24, 48, and 72 h.

Reaction Conditions

0 - 100 µM; at 24, 48, and 72 h

Applications

The cell abilities of MNNG/HOS, MG-63, and U2-OS were suppressed in a time- and concentration-dependent manner either treated with dynasore or cisplatin.

Animal experiment [2]:

Animal models

Sprague-Dawley rats

Preparation Method

Sprague-Dawley rats were randomly assigned to sham, SCI, and 1, 10, and 30 mg dynasore groups. The rat model of SCI was established using an established Allen's model. Dynasore was administered via intraperitoneal injection immediately.

Dosage form

1, 10, and 30 mg/kg; i.p.

Applications

Results of motor functional test indicated that dynasore ameliorated the motor dysfunction greatly at 3, 7, and 10 days after SCI in rats. Results of western blot showed that dynasore has remarkably reduced the expressions of Drp1, dynamin 1, and dynamin 2 and, moreover, decreased the Bax, cytochrome C, and active Caspase-3 expressions, but increased the expressions of Bcl-2 at 3 days after SCI. Results of immunofluorescent double labeling showed that there were less apoptotic neurons and proliferative astrocytes in the dynasore groups compared with SCI group. Finally, histological assessment via Nissl staining demonstrated that the dynasore groups exhibited a significantly greater number of surviving neurons compared with the SCI group.

References:

[1] Zhong B, et al. Dynasore suppresses cell proliferation, migration, and invasion and enhances the antitumor capacity of cisplatin via STAT3 pathway in osteosarcoma. Cell Death Dis. 2019 Sep 18;10(10):687.

[2] Li G, et al. Dynasore Improves Motor Function Recovery via Inhibition of Neuronal Apoptosis and Astrocytic Proliferation after Spinal Cord Injury in Rats. Mol Neurobiol. 2017 Nov;54(9):7471-7482.

Background

ジナソアは、GTPase阻害剤として作用し、エンドサイトーシスを防止するためにダイナミン活性を迅速かつ可逆的に抑制することができます[1]

ダイナソアは、約15µMのIC50でダイナミンGTPase活性とトランスフェリン摂取を阻害します[2]。in vitroでは、80µMのダイナソア処理により一般的にダイナミン1および2がブロックされます。また、低濃度範囲でもフェロプトーシスを強力に抑制します。さらに、100nMでH2O2誘発性細胞死も効果的に阻止しました[3]。in vitro実験では、100µMのダイナソア処理がVEGF誘導性カルシウム放出を妨げることが示されています[4]。ex vivoマウス眼球の眼表面では、40μMのダイナソア処理でストレス刺激による染料摂取が阻止されました。このため、ダイナソアは明らかに細胞およびその表面糖タンパク質層を保護し、酸化ストレスからの損傷や染料侵入を予防する役割があります[5]。in vitroテストでは、100µMのダイナソア処理は自発性EPSC(sEPSC)頻度を急速に増加させ、その後孤立したトラクト誘発性EPSC(ST-EPSC)および非同期EPSCの両方を抑制しました[6]。腹膜マクロファージとLLC-MK2細胞では、100µMのダイナソア処理により寄生虫内部化が劇的に減少しました[7]。

in vivoの有効性試験では、ダイナソア(10 mg/kg、腹腔内投与)がネフロ毒性や肝毒性を引き起こすことなくOS腫瘍形成を抑制することが示されました[8]。また、in vivoでの眼マウスセレニーモデルにおいては、30 mg/kgの投与量でも眼炎を減少させることはありませんでしたが、体重減少に対して有意な保護効果を提供しました[9]。

References:
[1]Preta G, et al. Dynasore - not just a dynamin inhibitor. Cell Commun Signal. 2015 Apr 10;13:24.
[2] Lee S, et al. Synthesis of potent chemical inhibitors of dynamin GTPase. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4858-64.
[3] Clemente LP, et al. Dynasore Blocks Ferroptosis through Combined Modulation of Iron Uptake and Inhibition of Mitochondrial Respiration. Cells. 2020 Oct 9;9(10):2259.
[4] Webster A, et al. Dynasore protects the ocular surface against damaging oxidative stress. PLoS One. 2018 Oct 10;13(10):e0204288.
[5] Hofmann ME, et al. Dynasore blocks evoked release while augmenting spontaneous synaptic transmission from primary visceral afferents. PLoS One. 2017 Mar 30;12(3):e0174915.
[6]Lum M, et al. Impact of dynasore an inhibitor of dynamin II on Shigella flexneri infection. PLoS One. 2013 Dec 19;8(12):e84975.
[7] Zhong B, et al. Dynasore suppresses cell proliferation, migration, and invasion and enhances the antitumor capacity of cisplatin via STAT3 pathway in osteosarcoma. Cell Death Dis. 2019 Sep 18;10(10):687.
[8] Basagiannis D, et al. Dynasore impairs VEGFR2 signalling in an endocytosis-independent manner. Sci Rep. 2017 Mar 22;7:45035.
[9] Barrias ES, et al. Dynasore, a dynamin inhibitor, inhibits Trypanosoma cruzi entry into peritoneal macrophages. PLoS One. 2010 Jan 20;5(1):e7764.

Chemical Properties

Cas No. 304448-55-3 SDF
Chemical Name (E)-N'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide
Canonical SMILES OC1=C(C(N/N=C/C(C=C2)=CC(O)=C2O)=O)C=C(C=CC=C3)C3=C1
Formula C18H14N2O4 M.Wt 322.31
溶解度 ≥ 16.12mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.1026 mL 15.513 mL 31.026 mL
5 mM 0.6205 mL 3.1026 mL 6.2052 mL
10 mM 0.3103 mL 1.5513 mL 3.1026 mL
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Related Video

    Dynasore-GlpBio

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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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