2. Signaling Pathways
  3. SWI/SNF Complex

SWI/SNF Complex

SWI/SNF Family of Chromatin-Remodelling Complexes

The SWI/SNF family of chromatin-remodelling complexes, also known as BRG1/BRM-associated factor (BAF) complexes (BOX 1), are key regulators of nucleosome positioning. The SWI/SNF family chromatin remodeling complexes are multi-subunit, ATP-dependent molecular machines that slide and evict nucleosomes. They play a major role in control of the chromatin structure and regulate gene transcription in eukaryotic cells. Mutations of the human complexes are often found in cancers and neurodevelopmental disorders. Mammalian SWI/SNF complexes belong to three broad subfamilies: canonical BAF (cBAF); polybromo-associated BAF (PBAF); and the GLTSCR1 or GLTSCR1L-containing and BRD9-containing (GBAF) complex. All three complexes contain the core subunits including SMARCC1, SMARCC2, and either of the ATPases SMARCA4 or SMARCA2, but also contain numerous variable subunits that provide each of the complexes with a distinct identity.
The human SWI/SNF complexes are frequently mutated in cancer. Loss of the peripheral subunits, such as SMARCB1, PBRM1, and SMARCE1, results in formation of defective complexes, which delocalize on chromatin, deregulate gene transcription, and potentially are oncogenic. Cancer genome-sequencing studies have revealed a remarkably high prevalence of mutations in genes encoding subunits of the SWI/SNF chromatin-remodelling complexes, with nearly 25% of all cancers harbouring aberrations in one or more of these genes. Consequently, increasing research interest is being focused on understanding the prognostic and, in particular, the potential therapeutic implications of mutations in genes encoding SWI/SNF subunits[1][2].

SWI/SNF Complex Related Products (6):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-170349
    SMARCA2 ligand-11
    		Ligand
    SMARCA2 ligand-11 is the ligand for SMARCA2, and can be used for synthesis of PROTAC SMARCA2 degrader-32 (HY-170343) as ligand for target protein.
    SMARCA2 ligand-11
  • HY-161886
    SMARCA2-IN-7
    		Inhibitor
    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.
    SMARCA2-IN-7
  • HY-170343
    PROTAC SMARCA2 degrader-32
    		Degrader
    PROTAC SMARCA2 degrader-32 (Compound 27) is the degrader for SMARCA2 with a DC50 of 1.3 nM. PROTAC SMARCA2 degrader-32 inhibits the proliferation of lung cancer cell NCI-H838 with a GI50 of 34 nM. (Pink: ligand for target protein SMARCA2 ligand-11 (HY-170349); Black: linker (HY-W895794); Blue: ligand for E3 ligase VHL (HY-170348))
    PROTAC SMARCA2 degrader-32
  • HY-169275
    PROTAC SMARCA2 degrader-24
    		Degrader
    PROTAC SMARCA2 degrader-24 (Compound 34) is a PROTAC degrader for SMARCA2 with a DC50 < 0.1 µM in HeLa. PROTAC SMARCA2 degrader-24 degrades SMARCA4 with a DC50 > 10 μM in HeLa.
    PROTAC SMARCA2 degrader-24
  • HY-169273
    PROTAC SMARCA2 degrader-22
    		Degrader
    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-22
  • HY-144720
    BRG1-IN-1
    BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors.
    BRG1-IN-1