mTOR/HDAC6-IN-1 is an effective dual inhibitor of histone deacetylase (HDAC6) and mammalian rapamycin (mTOR). The IC50 values for HDAC6 and mTOR are 56 nM and 133.7 nM respectively. MTOR/HDAC6-IN-1 can significantly induce autophagy and apoptosis and inhibit migration. MTOR/HDAC6-IN-1 has potential in the study of triple negative breast cancer (TNBC).

mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC 50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h [1]. mTOR/HDAC6-IN-1 (10 μM; 6 hours) can significantly improve the thermal stability of HDAC6 in MDA-MB-231 cells, which indicates that mTOR/HDAC6-IN-1 has a selective inhibitory effect on HDAC6 [1]. mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone [1]. mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 48 hours) induces obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells [1]. mTOR/HDAC6-IN-1 (5, 10, 20 μM) induces significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3 [1]. mTOR/HDAC6-IN-1 (5, 10, 20 μM; 48 hours) inhibited MDA-MB-231 cells migration in a dose-dependent manner, and decreases the expression of MMP-2 as well as increases the expression of E-cadherin [1]. Cell Viability Assay Cell Line: MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells [1] Concentration: 0, 20, 40, 60, 80 and 100 μM Incubation Time: 48 hours Result: Had a medium anti-proliferation activity with IC 50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h. Apoptosis Analysis Cell Line: MDA-MB-231 [1] Concentration: 5, 10, 20 μM Incubation Time: Result: Induced significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3. Cell Autophagy Assay Cell Line: MDA-MB-231 [1] Concentration: 2.5, 5, 10 μM Incubation Time: 48 hours Result: Induced obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells