| Bioactivity | ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis[1]. | ||||||||||||
| Invitro | ROC-325 antagonizes renal cell carcinoma (RCC) growth and survival in an ATG5/7-dependent manner, induces apoptosis, and exhibits favorable selectivity. 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 hallmark features of autophagy inhibition and antagonizes autophagic flux[1].ROC-325 triggers a highly significant increase in cathepsin D (CTSD) levels. 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]. | ||||||||||||
| Name | ROC-325 | ||||||||||||
| CAS | 1859141-26-6 | ||||||||||||
| Formula | C28H27ClN4OS | ||||||||||||
| Molar Mass | 503.06 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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ROC-325
CAS: 1859141-26-6 F: C28H27ClN4OS W: 503.06
ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidi
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