1. Signaling Pathways
  2. 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 相关产品 (6):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161886
    SMARCA2-IN-7 Inhibitor
    SMARCA2-IN-7 (compound 12),是 BRM 和 BRG1 的双抑制剂 (IC50 均小于 0.005),有抗肿瘤增殖的作用,抑制 BRG1 缺失的 SKMEL5 肿瘤增殖,在 SKMEL5 中的细胞增殖活力为 AAC50 为 13 nM。在 H1299 细胞中抑制 KRT880 的细胞增殖活力为 AAC50 为 42 nM。
    SMARCA2-IN-7
  • HY-144720
    BRG1-IN-1
    BRG1-IN-1 (Compound 11d) 是一种有效的 SMARCA4/BRG1 抑制剂。BRG1-IN-1 在体外使 GBM 细胞对 Temozolomide 的抗增殖和细胞死亡诱导作用敏感方面显示出比 PFI-3 更好的功效。BRG1-IN-1增强 Temozolomide 对皮下 GBM 肿瘤生长的抑制作用。
    BRG1-IN-1
  • HY-169273
    PROTAC SMARCA2 degrader-22 Degrader
    PROTAC SMARCA2 degrader-22 (Compound 5) 是一种 PROTAC 降解剂,用于降解 SMARCA2,在 100 nM 时降解效率为 94%。PROTAC SMARCA2 degrader-22 可抑制细胞 A549 的增殖,EC50 < 250 nM。
    PROTAC SMARCA2 degrader-22
  • HY-170349
    SMARCA2 ligand-11 Ligand
    SMARCA2 ligand-11 是 SMARCA2 的配体,可以作为靶蛋白配体用于合成 PROTAC SMARCA2 degrader-32 (HY-170343)。
    SMARCA2 ligand-11
  • HY-170343
    PROTAC SMARCA2 degrader-32 Degrader
    PROTAC SMARCA2 degrader-32 (Compound 27) 是 SMARCA2 的降解剂,DC50 为 1.3 nM。PROTAC SMARCA2 degrader-32 抑制肺癌细胞 NCI-H838 的增殖,GI50 为 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) 是 SMARCA2 PROTAC 降解剂,在 HeLa 细胞中的DC50 < 0.1 µM。PROTAC SMARCA2 degrader-24 在 HeLa 细胞中降解 SMARCA4DC50 > 10 μM。
    PROTAC SMARCA2 degrader-24