Name | ROC-325 |
Description | ROC-325 is an effective and orally active inhibitor of autophagy with anticancer activity. ROC-325 induces renal cell carcinoma apoptosis and exhibits favorable selectivity. |
In vitro | ROC-325 (5 μM) leads to the formation of LC3B punctae and a robust increase in LC3B levels in both A498 and 786-0 RCC cells. 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. ROC-325 inhibits cells growth with IC50 values of 4.9 μM, 11 μM, 4.6 μM, 5.4 μM, 7.4 μM, 11 μM, 8.2 μM, 5.8 μM, 5.0 μM, 11 μM, 8.4 μM and 6.0 μM for A498, A549, CFPAC-1, COLO-205, DLD-1, IGROV-1, MCF-7, MiaPaCa-2, NCI-H69, PC-3, RL and UACC-62 cells, respectively. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux[1]. |
In vivo | In mice bearing 786-0 RCC xenografts, ROC-325 (25, 40, and 50 mg/kg; oral) leads to significant, dose-dependent inhibition of disease progression and inhibits autophagy in vivo[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 1 mg/ml, Sonication is recommended. H2O : 0.8 mg/mL (1.59 mM), Sonication is recommended.
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Keywords | Apoptosis | anticancer | inhibit | ROC325 | ROC 325 | Autophagosomes | ROC-325 | cathepsin-D | lysosomes | oral | Autophagy | Inhibitor |
Inhibitors Related | Stavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib |
Related Compound Libraries | Bioactive Compound Library | Autophagy Compound Library | Inhibitor Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |