SMARCA4 Degrader

PROTAC SMARCA2/4 degrader-28 is a heterobifunctional PROTAC degrader targeting SMARCA2 and SMARCA4. PROTAC SMARCA2/4 degrader-28 forms a ternary complex with CRL2_VHL E3 ligase and SMARCA2 or SMARCA4, mediating the ubiquitination and degradation of SMARCA2, while acting as a partial degrader of SMARCA4. PROTAC SMARCA2/4-degrader-28 can be used in cancer-related research.

PROTAC BRM degrader-1 is a VHL-recruiting PROTAC degrader that exhibits higher selectivity for the degradation of SMARCA2 (BRM) over its highly homologous protein SMARCA4 (BRG1). The K_D values of PROTAC BRM degrader-1 for BRM and BRG1 are 72 nM and 108 nM, respectively. PROTAC BRM degrader-1 can be used in studies related to selective SMARCA2 degradation, SWI/SNF function, and SMARCA4-mutant non-small cell lung cancer.

PROTAC SMARCA2/4 degrader-11 is a PROTAC degrader targeting SMARCA2 and SMARCA4. PROTAC SMARCA2/4 degrader-11 induces protein ubiquitination and subsequent proteasome-mediated degradation. PROTAC SMARCA2/4-degrader-11 can be used in cancer-related research.

PROTAC SMARCA2/4 degrader-44 is a PROTAC-based protein degrader targeting SMARCA2/4, which induces ubiquitination and subsequent degradation of the target proteins. PROTAC SMARCA2/4 degrader-44 is applicable for cancer-related research.

PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2_VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research^[1].

PROTAC SMARCA2/4 degrader-26 is a SMARCA2/4 PROTAC degrader with selective anti-tumor activity against lung cancer cells. PROTAC SMARCA2/4 degrader-26 degrades SMARCA2 and SMARCA4 via the PROTAC-mediated proteasomal pathway. It induces DNA damage and apoptosis in tumor cells, while inhibiting migration and colony formation of lung cancer cells; in addition, it damages normal vascular endothelial cells and exhibits significant off-target-related cytotoxicity. PROTAC SMARCA2/4 degrader-26 serves as the parent scaffold to construct the GSH-responsive prodrug PROTAC SMARCA2/4 degrader-25 (HY-162813), a derivative that shows drastically reduced cytotoxicity against normal cells. PROTAC SMARCA2/4 degrader-26 can be used in lung cancer-related research.

PROTAC SMARCA2/4 degrader-30 is a SMARCA2 and SMARCA4 PROTAC degrader. PROTAC SMARCA2/4 degrader-30 induces ubiquitination and proteasome-mediated degradation of proteins. PROTAC SMARCA2/4 degrader-30 is applicable for cancer-related research.

PROTAC SMARCA2/4 degrader-8 is a SMARCA2/SMARCA4 PROTAC degrader. PROTAC SMARCA2/4 degrader-8 induces ubiquitination, proteasome-mediated degradation, and recruits the E3 ubiquitin ligase complex. PROTAC SMARCA2/4 degrader-8 is applicable for cancer-related research.

PROTAC SMARCA2/4 degrader-3 is a SMARCA2 and SMARCA4 PROTAC degrader. It is applicable to cancer-related research.

PROTAC SMARCA2/4 degrader-2 is a PROTAC degrader targeting SMARCA2 and SMARCA4, with a DC₅₀ of < 100 nM for both proteins. PROTAC SMARCA2/4 degrader-2 induces ubiquitination and subsequent proteasome-mediated degradation of SMARCA2 and SMARCA4 proteins. PROTAC SMARCA2/4 degrader-2 can be used in cancer-related research.

PROTAC SMARCA2 degrader-13 is a PROTAC degrader targeting SMARCA2 and SMARCA4. PROTAC SMARCA2 degrader-13 induces ubiquitination of SMARCA2 and SMARCA4 and mediates their degradation via the proteasome. PROTAC SMARCA2 degrader-13 can be used in cancer-related research.