ROC-325

Cas No.:	1859141-26-6
Chemical Name:	ROC325,ROC 325
Synonyms:	ROC325,ROC 325
SMILES:	C1C=CC=C2SC3C(C)=CC=C(NCCN(C)CCNC4=CC=NC5=CC(Cl)=CC=C45)C=3C(=O)C=12
Formula:	C28H26N3SOCl
M.Wt:	488.04
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	ROC-325 is a novel inhibitor of autophagy.
In Vivo:	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].
In Vitro:	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].