ROC-325 |
| カタログ番号GC32901 |
ROC-325 は、強力な抗がん作用を持つ強力な経口活性オートファジー阻害剤です。 ROC-325 は、リソソームの脱酸、オートファゴソームの蓄積、オートファジーの流れの乱れを誘発します。 ROC-325 は、腎細胞癌のアポトーシスも誘導します。
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Cas No.: 1859141-26-6
Sample solution is provided at 25 µL, 10mM.
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ROC-325 is a novel inhibitor of autophagy.
ROC-325 is a novel inhibitor of autophagy. Treatment with ROC-325 results in a significant loss of acridine orange fluorescence. ROC-325 triggers a highly significant increase in cathepsin D (CTSD) levels. ROC-325 treatment yields pharmacodynamic effects that are consistent with inhibition of autophagy. Treatment with 5 μM ROC-325 for 24 hours leads to the formation of LC3B punctae and a robust increase in LC3B levels in both A498 and 786-0 RCC cells. Immunoblotting analysis conducted in both A498 and 786-0 cells demonstrates that ROC-325 promotes a dose-dependent increase in LC3B expression in a manner that correlated with a corresponding increase in the levels of p62 and cathepsin D[1].
ROC-325 treatment leads to significant, dose-dependent inhibition of disease progression. ROC-325 is well tolerated and no notable toxicities are observed other than a very modest, nonsignificant reduction in mean body weight at the highest dose. Immunohistochemical analysis of specimens collected from animals treated with ROC-325 demonstrates significant, dose-dependent increases in the autophagic markers LC3B and p62 and increases apoptosis[1].
[1]. Carew JS, et al. Disruption of Autophagic Degradation with ROC-325 Antagonizes Renal Cell Carcinoma Pathogenesis. Clin Cancer Res. 2017 Jun 1;23(11):2869-2879.
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