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Aumitin is a novel potent autophagy inhibitor with IC50 of 124 and 244 nM against starvation- and rapamycin- induced autophagy respectively, targets mitochondrial complex I; inhibits LC3 lipidation, and p62 degradation by starvation- as well as rapamycin-induced autophagy dose-dependently in MCF7-LC3 cells, suggesting inhibition of autophagic flux; inhibits mitochondrial respiration by targeting complex I with IC50 of 0.11 uM in HeLa cells; Aumitin is a new tool compound for interrogating autophagy and mitochondrial respiration by means of complex I inhibition.



XRK3F2 is a specific ZZ-domain of ubiquitin-binding protein p62 (Sequestosome 1) inhibitor that inhibits MM cell growth and BMSC growth enhancement of human MM cells; inhibits TNFα-induced osteoclast formation, and has IC50 of 4.35 uM 5TGM1 cells and 4.6 uM for the human MM1.S cell line; induces new cortical bone formation in MMBD in vivo, and alters MM cell-BMSC cell interactions by reducing MM cell-derived TNFα in the myeloma microenvironment.




Lys05 (Lys01 trihydrochloride, PS-1001) is the water-soluble salt of Lys01, is a 10-fold more potent lysosomal autophagy inhibitor than hydroxychloroquine (HCQ); shows IC50 values of 3.6, 3.8, 6 and 7.9 uM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay; more potently accumulates within and deacidifies the lysosome, resulting in impaired autophagy and tumor growth; enhances sunitinib-mediated suppression of clear cell ovarian carcinoma (CCOC) cell viability.




ROC-325 (ROC 325, ROC325) is a novel, orally available inhibitor of lysosomal-mediated autophagy; exhibits superior in vitro anticancer effects compared with the existing autophagy inhibitor hydroxychloroquine (HCQ) in different cancer cell lines, including accumulation of autophagosomes with undegraded cargo, lysosomal deacidification, p62 stabilization, and disruption of autophagic flux; antagonizes RCC growth and survival in an ATG5/7-dependent manner, induces apoptosis and exhibited favorable selectivity; significantly more effective at inhibiting tumor progression than HCQ, and inhibited autophagy in vivo.




STF-62247 is a small molecule Autophagy inducer that induces autophagy and selectively induces lethality in VHL-deficient RCC cells; induces cytotoxicity and reduces tumor growth in VHL-deficient cells in a HIF-independent manner, PI3K and Golgi trafficking are required as initial signals in STF-62247-induced autophagy.

Kidney Cancer




DC661 (DC-661) is a novel dimeric chloroquine (CQ) that is capable of deacidifying the lysosome and inhibiting autophagy significantly better than HCQ, targets palmitoyl-protein thioesterase 1 (PPT1); inhibits autophagy and causes significant impairment of tumor growth.


1807988-47-1 IITZ-01 (Autophagy inhibitor IITZ-01) is a novel potent lysosomotropic autophagy inhibitor, exhibits >10-fold potent autophagy inhibition along with 12- to 20-fold better cytotoxic action than Chloroquine; enhances autophagosome accumulation but inhibit autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy, also abolishes mitochondrial membrane potential and triggers apoptosis through the mitochondria-mediated pathway (TNBC cells IC50=1.54 uM, 48 h); displays potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model.

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