Hydroxy Dynasore is an inhibitor of dynamin1 and dynamin2 with IC50 of 0.38 μM and 2.6 µM respectively. It can prevent dynamin-mediated endocytosis in multiple cell types.
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HazMat fee for 500 gram (Estimated)
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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].
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