2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. 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 Isoform Specific Products:

SWI/SNF Complex Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-145388
    AU-15330
    		Degrader 99.89%
    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.
    AU-15330
  • HY-128359
    ACBI1
    		Degrader 99.92%
    ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.
    ACBI1
  • HY-159607
    PRT3789
    		Degrader 98.08%
    PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer.
    PRT3789
  • HY-44012
    SMARCA-BD ligand 1 for PROTAC
    		Ligand 99.07%
    SMARCA-BD ligand 1 for PROTAC is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
    SMARCA-BD ligand 1 for PROTAC
  • HY-44012B
    SMARCA-BD ligand 1 for PROTAC hydrochloride
    		Ligand 99.24%
    SMARCA-BD ligand 1 hydrochloride for PROTAC is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
    SMARCA-BD ligand 1 for PROTAC hydrochloride
  • HY-185075
    FHD-909
    		Inhibitor
    FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified SMARCA4 (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders.
    FHD-909
  • HY-182987
    SMARCA2/SMARCA4 ligand-1
    SMARCA2/SMARCA4 ligand-1 is a SMARCA2/SMARCA4 ligand with KD values of 1.2 and 10.3 nM. SMARCA2/SMARCA4 ligand-1 binds SMARCA2/4 bromodomain via hydrogen bonds with asparagine and tyrosine residues, and a salt bridge with a glutamate residue. SMARCA2/SMARCA4 ligand-1 shows antiproliferative activity against cancer cells. SMARCA2/SMARCA4 ligand-1 can be used for the research of cancer, such as smarca4 mutant nonsmall cell lung cancer.
    SMARCA2/SMARCA4 ligand-1
  • HY-181909
    PROTAC SMARCA2 degrader-36
    		Degrader
    PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers.
    PROTAC SMARCA2 degrader-36
  • HY-44012A
    SMARCA-BD ligand 1 for PROTAC dihydrochloride
    		Ligand 98.08%
    SMARCA-BD ligand 1 for PROTAC dihydrochloride is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
    SMARCA-BD ligand 1 for PROTAC dihydrochloride
  • HY-170824
    SMD-3236
    		Degrader
    SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia.
    SMD-3236
  • HY-168230
    SMARCA2 ligand-9
    		Ligand
    SMARCA2 ligand-9 is the ligand of SMARCA2. SMARCA2 ligand-9 can be used to synthesize PROTAC SMARCA2 degrader-27 (HY-168229).
    SMARCA2 ligand-9
  • HY-175756
    SMARCA2/4 degrader-1
    		Degrader
    SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4DCAF16 and CRL1FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer.
    SMARCA2/4 degrader-1
  • HY-176871
    PROTAC SMARCA2 degrader-35
    		Degrader
    PROTAC SMARCA2 degrader-35 (Compound 43) is a selective SMARCA2 PROTAC degrader with a DC50 < 0.1 μM for SMARCA2. PROTAC SMARCA2 degrader-35 has anticancer activity and regulates cancer cell proliferation and growth through cell cycle arrest and DNA replication inhibition in SMARCA4-deleted cancer cells.
    PROTAC SMARCA2 degrader-35
  • HY-44824
    SMARCA2 ligand-13
    		Ligand
    SMARCA2 ligand-13 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMARCA2 ligand-13 can be used for synthesis PROTACs.
    SMARCA2 ligand-13
  • HY-170828
    SMD-1087
    		Degrader
    SMD-1087 is a PROTAC that selectively targets SMARCA2 (DC50=8 nM, Dmax=89%) and SMARCA4 with a DC50 of 1 μM. SMD-1087 consists of the E3 ligase ligand (S,R,S)-AHPC-Me (blue part) (HY-112078), the target protein ligand SMI-1074 (red part) (HY-170817), and the PROTAC linker (1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate (black part) (HY-W890392). Among them, its target protein ligand + Linker part corresponds to SMARCA2 Ligand-Linker Conjugate-1 (HY-170829).
    SMD-1087
  • 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-183007
    LJM133
    		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. (Pink: SMARCA2/PBRM1/SMARCA4 ligand (HY-182987); E3 ubiquitin ligase ligand-linker conjugate (HY-183619)).
    LJM133
SWI/SNF Complex Isoform Comparison

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