rapamycin-induced autophagy

Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay.

Insecticidal agent 364 is a selective small molecule inhibitor of rapamycin kinase target protein. Insecticidal agent 364 has antitumor activity, and by inhibiting mTOR, Insecticidal agent 364 aims to disrupt signaling pathways involved in cancer cell growth and survival, thereby potentially inhibiting tumor growth.

Autogramin-1 potently inhibits autophagy induced by mTORC1 inhibition (Rapamycin; IC50: 0.44 μM) or starvation (IC50: 0.17 μM).

SAR-405 is a potent and selective PIK3C3 Vps34 inhibitor (IC50:1.2 nM; Kd:1.5 nM) that prevents autophagy and synergizes with MTOR inhibition in tumor cells. SAR405 treatment also inhibits autophagy induced either by starvation or by MTOR (mechanistic target of rapamycin) inhibition. Combining SAR405 with everolimus results in a significant synergy on the reduction of cell proliferation using renal tumor cells.

Aumitin, a diaminopyrimidine-based autophagy inhibitor, dose-dependently inhibits starvation- and rapamycin-induced autophagy with IC50s of 0.12 μM and 0.24 μM, respectively [1], and also inhibits mitochondrial respiration by targeting complex I.

Autogramin-2 (tert-butyl 2-(4-isopropoxybenzamido)-6,7-dihydrothiazolo[5,4-c]pyridine-5(4H)-carboxylate) potently inhibits autophagy induced by either starvation with IC50 of 0.27 μM, and inhibits mTORC1 (Rapamycin; IC50:0.14 μM)