ML-346 |
Catalog No.GC18170 |
ML-346은 Hsp70 발현 및 HSF-1 활성의 활성제이며, Hsp70에 대한 EC50은 4.6μM입니다. ML-346은 구조적 질병 모델에서 상당한 세포독성이나 특이성의 결여 없이 단백질 접힘을 복원합니다. ML-346은 Hsp70, Hsp40 및 Hsp27과 같은 샤페론을 포함하여 열 충격 반응(HSR)의 유전자 및 단백질 이펙터의 특정 증가를 유도합니다.
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Cas No.: 100872-83-1
Sample solution is provided at 25 µL, 10mM.
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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