Bcl-2 Degrader

WH244 is a BCL-xL and BCL-2 PROTAC degrader with DC₅₀ values of 0.6 nM and 7.4 nM, and K_d values of 6.14 nM and 3.1 nM, respectively. WH244 kills cancer cells dependent on BCL-xL and BCL-2 for survival. WH244 is applicable to relevant research on leukemia.

PROTAC Bcl-2/Bcl-xL Degrader-1 is a Bcl-2/Bcl-xL PROTAC degrader with a DC₅₀ of 11.28 nM against Bcl-xL. PROTAC Bcl-2/Bcl-xL Degrader-1 promotes ubiquitination and degradation of Bcl-2/Bcl-xL. It exhibits anticancer activity against acute lymphoblastic leukemia. PROTAC Bcl-2/Bcl-xL Degrader-1 can be used in the research of BCL-2-mediated or BCL-2-dependent diseases.

BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC₅₀ of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC).

PROTAC Bcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 has strong anti-tumor activity against HepG2 cells and HUVEC cells. PROTAC Bcl-xL degrader-4 induces cells apoptosis by decreasing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly inhibits tumor growth in xenograft tumor mouse models.