ErbB3/HER3 Degrader

TX2-121-1 is a bifunctional hydrophobic tag Her3 degrader and also a Her3 inhibitor with an IC₅₀ of 49 nM. TX2-121-1 covalently binds to Cys721 of Her3, induces Her3 degradation via the Hsp70/Hsp90-assisted proteasomal pathway, interferes with the heterodimerization of Her3 with Her2/c-Met, and attenuates downstream Erk/Akt signaling, thereby inhibiting Her3-dependent cancer cell growth. TX2-121-1 can be used for the research of non-small cell lung cancer, ovarian cancer and Her3-driven breast cancer.

CZY43 is a HER3 degrader with a DC₅₀ of 559 nM. CZY43 induces HER3 degradation via autophagy, inhibits HER3-dependent signaling pathways, suppresses downstream PI3K/Akt signaling, and thereby inhibits tumor cell proliferation and cell adhesion. CZY43 can be used in studies of breast cancer and non-small cell lung cancer.

PROTAC Her3 Degrader-8 (Compound PP2) is a Her3 PROTAC degrader. PROTAC Her3 Degrader-8 promotes the ubiquitination and degradation of Her3. PROTAC Her3 Degrader-8 can be used in the study of lung adenocarcinoma and ovarian cancer.

TX2-120-1 possesses the ability to bind to Her3, with an IC₅₀ value of 56 nM for Her3. TX2-120-1 can be used for the synthesis of TX2-121-1 (HY-118998).

PROTAC Her3 Degrader-2 is a Her3 PROTAC degrader with an IC₅₀ < 10 nM. PROTAC Her3 Degrader-2 recruits Her3 to E3 ubiquitin ligase to achieve selective degradation. PROTAC Her3 Degrader-2 can be used in the research of breast cancer, lung cancer, head and neck cancer, and prostate cancer.