cIAP-2 Degrader

TD1092 is a pan-inhibitor of apoptosis protein (IAP) PROTAC degrader that targets cIAP1, cIAP2, and XIAP for degradation. TD1092 induces cell apoptosis by activating caspase. TD1092 inhibits the NF-κB signaling pathway induced by TNFα. TD1092 suppresses TNFα-induced epithelial-mesenchymal transition, cancer cell migration, and invasion. TD1092 is suitable for research on breast cancer, ovarian cancer, melanoma, and inflammation-related diseases.

CST626 is a PROTAC degrader targeting IAP, with DC₅₀ values of 0.7 nM, 2.4 nM and 6.2 nM against XIAP, cIAP1 and cIAP2, respectively. This compound recruits the VHL E3 ubiquitin ligase to form a heterotrimeric complex, thereby inducing ubiquitination and proteasomal degradation of the target proteins. CST626 also exhibits certain degrading activity against VHL30 and VHL19. CST626 inhibits the proliferation and induces apoptosis of various hematologic tumor cell lines, and its anti-tumor effect is further enhanced when used in combination with TNF-α. CST626 can be used in research related to multiple myeloma, acute myeloid leukemia and diffuse large B-cell lymphoma.

SM-122 is a monovalent Smac mimetic targeting cellular inhibitor of apoptosis protein (cIAP)-1/2. SM-122 can induce cIAP-1/2 degradation and weakly induce apoptosis in tumor cells. SM-122 can be used for the research of cancer, such as breast cancer.