TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research.
TD1092 (0.1 μM-10 μM; 0.5-6 h) potently degrades cIAP1, cIAP2, and XIAP in a dose- and time-dependent manner[1].TD1092 (0.01, 0.1 and 1 μM; 18 h) activates caspase 3/7 in MCF-7 cells[1].TD1092 (1 μM; 48 h and 72 h) promotes cancer cell death[1].TD1092 (0.1 μM; 24 h) inhibits TNFα-induced migration and invasion against triple-negative breast cancer cells[1].TD1092 (1 μM; 6 h) inhibits TNFα-induced NF-κB signaling pathway and epithelial-mesencmal transition (EMT) via IAP degradation[1].TD1092 (1 μM; 72 h) inhibits MCF-7 cells growth with an IG50 value of 0.395 μM[1].
References:
[1]. Park S, et al. Discovery of pan-IAP degraders via a CRBN recruiting mechanism. Eur J Med Chem. 2023 Jan 5;245(Pt 2):114910.