SWI/SNF Complex Inhibitor

PROTAC SMARCA2 degrader-7 (Compound I-428) is a PROTAC degrader for SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A (SMARCA) SMARCA2. PROTAC SMARCA2 degrader-7 degrades SMARCA2 and SMARCA4 in MV411 with DC₅₀ of <100 and 100-500 nM. (Pink: Ligand for target protein (HY-159542); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))

SMARCA2-IN-7 (compound 12), a dual inhibitor of BRM and BRG1 (IC₅₀ < 0.005 for both), has an anti-tumor proliferation effect that inhibits BRG1-deleted SKMEL5 tumor proliferation with a cell proliferation activity AAC₅₀ of 13 nM in SKMEL5. The cell proliferation activity AAC₅₀ of KRT880 in H1299 cells was 42 nM.

SGC-BRDVIII-NC (Compound 35) is a negative control compound of SMARCA2/4 and PB1 bromodomain (BRD) inhibitor. SGC-BRDVIII-NC completely abolishes protein-ligand binding capacity with the methylation of the phenolic hydroxyl moiety. SGC-BRDVIII-NC can be used for adipogenesis research.

BRM/BRG1 ATP-IN-8 (Compound Cpd14) is an orally active BRG1/BRM ATPase domain inhibitor. BRM/BRG1 ATP-IN-8 exerts antitumor effects by disrupting aberrant chromatin remodeling in cancer cells, inducing apoptosis and growth arrest. BRM/BRG1 ATP-IN-8 is promising for research of BRG1/BRM-dependent malignancies, including hematological cancers, prostate cancer, breast cancer, and Ewing's sarcoma.

PROTAC SMARCA2 degrader-3 is a PROTAC degrader of the SWI/SNF ATPase subunits, SMARCA2. PROTAC SMARCA2 degrader-3 has anticancer effects (WO2023244764A1; Compound 153).

SMARCA2 ligand-12-3-methylazetidin is a target protein ligand-linker conjugate that incorporates a ligand for SMARCA2 (HY-169487), and a PROTAC linker (HY-W052601), which recruit E3 ligases. SMARCA2 ligand-12-3-methylazetidin can be used to synthesize PROTAC SMARCA2 degrader-25 (HY-169276).

PROTAC SMARCA2 degrader-30 (example 85) is a PROTAC SMARCA2 degrader with a DC₅₀ less than 100 nM in H1299 cells.

BRD4-BD1-IN-3 (Compound 4g) is a BRD4-BD1 inhibitor. BRD4-BD1-IN-3 can be used for research of inflammatory disease.

DCSM06-05 is a potent SMARCA2-BRD inhibitor with an IC₅₀ value of 9 µM, a K_d value of 22.4 µM.

SMARCA2/4-IN-1 (compound 1) is a potent SMARCA2 inhibitor with IC₅₀ values of 3.8, 1.7 µM for SMARCA2, SMARCA4, respectively.

C620-0696 is an inhibitor targeting the brom domain of BPTF, with a K_D value of 35.5 μM. C620-0696 can exert cytotoxic effects on A549 and H358 cells, inhibiting the expression of c-Myc. C620-0696 inhibits cell migration and colony formation, and induces apoptosis and cell cycle arrest. C620-0696 can be used in the research of non-small cell lung cancer.

PBRM1-BD2-IN-4 is a PBRM1-BD2 inhibitor with an IC₅₀ of 0.2 μM, and its K_d values for PBRM1-BD2 and PBRM1-BD5 are 5.5 μM and 11.1 μM, respectively. PBRM1-BD2-IN-4 selectively inhibits the proliferation of PBRM1-dependent prostate cancer cells. PBRM1-BD2-IN-4 can be used in studies related to prostate cancer.

SMARCA2-IN-4 (Compound 26) is an inhibitor for SWI/SNF chromatin remodeling complexe SMARCA by targeting the bromodomains. SMARCA2-IN-4 exhibits high affinity for PB1(5), SMARCA2B and SMARCA4 with K_d of 124, 262 and 417 nM.

SMARCA2/4-IN-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-IN-3 can be used for synthesis PROTAC SMARCA2/4-degrader-19 (HY-163877).

SMARCA2-IN-9 (compound 11) is a SMARCA2, PBRM1 bromodomains 2 (PBRM1(2)), and PBRM1 bromodomains 5 (PBRM1(5)) inhibitor with K_d values of 1.6 μM, 2.5 μM, and 3.95 μM, respectively.

BRM/BRG1 ATP-IN-6 (Compound 105) is a BRG1/BRM inhibitor. BRM/BRG1 ATP-IN-6 acts on the BAF complex, which is involved in chromatin regulation and gene expression via ATP-dependent chromatin remodeling. BRM/BRG1 ATP-IN-6 demonstrates anti-tumor potential, particularly in cancers associated with BAF complex disorders.

SMARCA2-IN-6 is a SMARCA2 and SMARCA4 inhibitor, with an IC₅₀ value of <0.005 μM for both SMARCA2 and SMARCA4. SMARCA2-IN-6 exerts anticancer activity against BRG1-mutant melanoma. SMARCA2-IN-6 can be used for research related to Brg1/Smarca4-mutant cancers.

SMI-1074, a SMARCA bromodomain inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMI-1074 can be used for synthesis SMD-3236 (HY-170824) and SMD-1087 (HY-170828). SMI-1074 can be used for the research of smarca4-deficient cancers.

SMARCA2 Ligand-Linker Conjugate-4 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for SMARCA2 (HY-178414) and a PROTAC linker, which recruits E3 ligases. SMARCA2 Ligand-Linker Conjugate-4 can be used for synthesis of PROTAC SMARCA2 degrader-35 (HY-176871).

Bromodomain inhibitor-13 (Compound 1) is an analog of PFI-3 (HY-12409). Bromodomain inhibitor-13 is a bromodomain-containing protein (BCP) inhibitor. Bromodomain inhibitor-13 targets SMARCA2, SMARCA4, PB1(5), and second bromodomain of PB1 (PB1(2)) with K_D values of 37, 53, 30, and 190 nM, respectively.