Protein Polybromo-1 Degrader

ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC₅₀s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.

G-6599 is a covalent molecular glue degrader targeting SMARCA2/SMARCA4, with DC₅₀ values of 0.017 nM and 0.057 nM against SMARCA2 and SMARCA4 in SW1573 cells, respectively. G-6599 exhibits proteome selectivity for SMARCA2, SMARCA4, and PBRM1. G-6599 induces the assembly of the SMARCA2-FBXO22 ternary complex, enabling ubiquitination and proteasomal degradation of both proteins via the ubiquitin-proteasome pathway without the need for biotransformation. G-6599 shows antiproliferative effects in relevant cancer cell models. G-6599 can be used for research on androgen-dependent prostate cancer and SMARCA4-mutant non-small cell lung cancer.

BRM/BRG1 ATP degrader-1 is a phenol derivative that effectively degrades the BRM protein. BRM/BRG1 ATP degrader-1 exerts degradation-inhibiting effects on BRM IF and BRG1 IF in SW1573 cells. BRM/BRG1 ATP degrader-1 can be used in studies related to BRM-mediated diseases, such as non-small cell lung cancer.