PROTACSMARCA2/4 degrader-38 is a SMARCA2/4 PROTAC degrader with DC50 values of 3.0 nM and 4.0 nM, respectively. It facilitates the ubiquitination and degradation of SMARCA2/4 and can block the G0/G1 phase of the cell cycle, leading to the induction of apoptosis. PROTACSMARCA2/4 degrader-38 is applicable in acute myeloid leukemia (AML) research.

SMARCA2:3.0 nM(DC50)

PROTAC SMARCA2/4 degrader-38 (Compound A11), when used at concentrations of 25-100 nM for 3 days, inhibits the proliferation of AML cells in the MV-4-11 cell line (IC₅₀: 4.9 nM) and MOLM-13 cell line (IC₅₀: 23.3 nM), as well as in diffuse large B-cell lymphoma cell lines SU-DHL-4 (IC₅₀: 87.7 nM) and WSU-DLCL-2 (IC₅₀: 336.7 nM). At concentrations of 100-1000 nM over 48 hours, PROTAC SMARCA2/4 degrader-38 induces a concentration-dependent G0/G1 phase cell cycle arrest in MV-4-11 and MOLM-13 cells. Furthermore, treatment with 100-1000 nM for 72 hours leads to apoptosis in MV-4-11 and MOLM-13 cells. Additionally, administration of 11.1-1000 nM for 24 hours results in a concentration-dependent suppression of AML oncogene transcription expression.