SWI/SNF Complex Degrader

LJM133 is a SMARCA2/PBRM1/SMARCA4 PROTAC degrader with DC₅₀ values of 3.5 nM, 7 nM, and 6.4 nM. LJM133 induces ternary complex formation with VHL E3 ligase to drive proteasome-mediated degradation of target proteins. LJM133 suppresses cell proliferation and exhibits significant antitumor efficacy in a SMARCA4 mutant cancer xenograft model. LJM133 can be used for the research of cancer, such as SMARCA4 mutant non-small cell lung cancer.

PROTAC SMARCA2 degrader-22 (Compound 5) is a PROTAC degrader for SMARCA2 with a degradation efficacy of 94% at 100 nM. PROTAC SMARCA2 degrader-22 inhibits the proliferation of cell A549 with an EC₅₀ < 250 nM.

PROTAC SMARCA2 degrader-29 (Example 87) is a PROTAC SMARCA2 (BRM) degrader, with DC₅₀ of 10-100 nM (BRM) and > 1 μM (BRG1, also known as SMARCA2) respectively.

PROTAC BRM/BRG1 degrader-4 (example 047) is a potent BRM and BRG1 PROTAC degrader, with DC₅₀ values of 0.21 nM and 3.4 nM in SW1573 cells, respectively.

PROTAC SMARCA2 degrader-27 (compound 4) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-27 has the potential to be used in cancer research.

NEP202 is a SMARCA2 PROTAC degrader designed based on the GID4 E3 ligase. NEP168 can be used for cancer research.

PROTAC SMARCA2/4-degrader-5 (Compound I-437) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-5 degrades SMARCA2 in MV411 and in A549 with DC₅₀ <100 nM, degrades SMARCA4 in MV411 with DC₅₀ of 100-500 nM.

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 BRM/BRG1 degrader-3 is a BRM/BRG1 PROTAC degrader, exhibiting a DC₅₀ of less than 1 nM for BRM degradation and a DC₅₀ of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 shows moderate inhibitory activity against CYP2D6 and hERG. PROTAC BRM/BRG1 degrader-3 inhibits cancer cell proliferation and tumor tissue growth, and exhibits favorable metabolic stability in liver microsomes. PROTAC BRM/BRG1 degrader-3 can be used in non-small cell lung cancer-related research.

PROTAC BRM/BRG1 degrader-2 (Example.004) is a PROTAC BRM/BRG1 degrader (DC₅₀: < 10 nM in A549 cell; IC₅₀: 15 nM for A549).

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 degrader-5 (Compound I-425) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2 degrader-5 degrades SMARCA2 in MV411 and in A549 with DC₅₀ <100 nM, degrades SMARCA4 with DC₅₀ of 100-500 nM. (Pink: Ligand for target protein (HY-159531); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))

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.

PROTAC A515 is a SMARCA2 PROTAC degrader. PROTAC A515 promotes the ubiquitination and degradation of SMARCA2. PROTAC A515 can be used in cancer research.

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.

PROTAC SMARCA2/4 degrader-37 (Example 4) is a PROTAC-based SMARCA2/4 degrader, with an IC₅₀ of ≤0.1 μM (Pink: SMARCA2/4 lignad (HY-172446); Black: CRBN ligand (HY-41547); Linker (HY-N2407)).

AU-15330 (Standard) is the analytical standard of AU-15330 (HY-145388). This product is intended for research and analytical applications. AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.