Dynasore |
Catalog No.GC10395 |
Dynasore, as a GTPase inhibitor, can rapidly and reversibly inhibit dynamin activity, which prevents endocytosis.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 304448-55-3
Sample solution is provided at 25 µL, 10mM.
Dynasore, as a GTPase inhibitor, can rapidly and reversibly inhibit dynamin activity, which prevents endocytosis[1].
Dynasore inhibits dynamin GTPase activity and transferrin uptake with IC50 of approximately 15 µM[2]. In vitro, treatment with 80 µM dynasore commonly block dynamin 1 and 2, dynasore also has a potent inhibition on ferroptosis at a range of lower concentrations. Dynasore also potently blocked H2O2-induced cell death at 100 nM[3]. In vitro experiment it demonstrated that treatment with 100 µM dynasore impairs VEGF-induced calcium release[4]. At the ocular surface of ex vivo mouse eyes, 40 uM dynasore blocked stress-stimulated dye uptake. Dynasore is obviously protective of cells and their surface glycocalyx, preventing damage due to oxidative stress, and thus precluding dye entry[5]. In vitro test it exhibited that treatment with 100 µM dynasore rapidly increased the spontaneous EPSC (sEPSC) frequency which was followed by inhibition of both solitary tract-evoked EPSCs (ST-EPSC) as well as asynchronous EPSCs[6]. In peritoneal macrophages and LLC-MK2 cells, treatment with 100 µM dynasore drastically diminished the parasite internalization[7].
In vivo efficacy test it shown that dynasore (10 mg/kg, intraperitoneally) inhibits OS tumorigenesis without inducing nephrotoxicity and hepatotoxicity[8]. In vivo, the ocular mouse Sereny model was administrated 30 mg/kg intraperitoneally did not reduce ocular inflammation, it did provide significant protection against weight loss[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.
Average Rating: 5
(Based on Reviews and 37 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *