protac mcl-1 degrader-1

PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC), a selective Mcl-1 inhibitor. By hijacking the CRBN ubiquitin ligase to form a ternary complex with the target protein, it induces Mcl-1 ubiquitination. It can be used for cancer research.

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. It downregulates Pin1 substrate proteins, including Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. Additionally, P1D-34 exhibits antiproliferative activity across various acute myeloid leukemia (AML) cell lines and induces DNA damage and apoptosis by generating reactive oxygen species (ROS).

CP-07 is a selective and effective PROTAC CDK9 degrader (DC50: 43 nM), demonstrating inhibition of 22RV1 cell proliferation (IC50: 62 nM) and colony formation by attenuating levels of Mcl-1 and c-Myc. Additionally, CP-07 has been shown to impede the growth of 22RV1 xenograft tumors and is applicable in prostate cancer research [1].