cIAP-1 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.

PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC₅₀ values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma.

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.

BCPyr is a PROTAC degrader targeting cIAP1 and BTK, with a K_d of 262 nM for human cIAP1, and K_d values of 262 nM and 692 nM for human BTK. BCPyr binds to the Bir3 domain of cIAP1, recruits BTK to cIAP1, and mediates the ubiquitination and degradation of BTK. BCPyr acts as a degrader, ternary complex stabilizer, cooperative binder, and higher-order assembly inducer. BCPyr can be used in studies related to leukemia and lymphoma.