ML-346 |
| Catalog No.GC18170 |
ML-346 est un activateur de l'expression de Hsp70 et de l'activité HSF-1, avec une EC50 de 4,6 μM pour Hsp70. ML-346 restaure le repliement des protéines dans des modèles de maladies conformationnelles, sans cytotoxicité significative ni manque de spécificité. Le ML-346 induit des augmentations spécifiques des gènes et des effecteurs protéiques de la réponse au choc thermique (HSR), y compris des chaperons tels que Hsp70, Hsp40 et Hsp27.
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Cas No.: 100872-83-1
Sample solution is provided at 25 µL, 10mM.
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ML-346 is an activator of the heat shock response that induces the expression of the heat shock proteins HSP70, HSP40, and HSP27.[1] It induces the expression of the oxidative stress response genes HO1, GCLM, and BiP in mouse embryonic fibroblasts (MEFs) and pretreatment protects cells from severe heat shock-induced death and H2O2-induced apoptosis. It promotes folding of metastable proteins in models of conformational disease, including cellular models of Huntingtin aggregation and cystic fibrosis. It reduces aggregate formation in PC12 cells expressing human Huntingtin exon 1 containing a 74 glutamine expansion when used at a concentration of 10 uM. It also corrects trafficking of cystic fibrosis transmembrane conductance regulator proteins bearing the F508 deletion (F508-CFTR) mutation carried by the majority of cystic fibrosis patients, leading to increased cell surface expression.
References
[1]. Calamini, B., Silva, M.C., Madoux, F., et al. Small-molecule proteostasis regulators for protein conformational diseases. Nat. Chem. Biol. 8(2), 185-196 (2011).
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