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Results for "

SMARCA2/4-IN-4

" in MedChemExpress (MCE) Product Catalog:

14

Inhibitors & Agonists

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-159607

    PROTACs SWI/SNF Complex Cancer
    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-176871

    PROTACs SWI/SNF Complex DNA/RNA Synthesis Cancer
    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-153361

    PROTACs Epigenetic Reader Domain Inflammation/Immunology Cancer
    YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC) .
    YD23
  • HY-170824

    PROTACs SWI/SNF Complex Epigenetic Reader Domain Cancer
    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-175756

    Molecular Glues SWI/SNF Complex Cancer
    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 CUL4 DCAF16 and CRL1 FBXO22 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-W494890

    Epigenetic Reader Domain Cancer
    SMARCA2-IN-10 (Compound 4) is a highly selective SMARCA2 ATPase domain inhibitor (IC50=17.676 μM). SMARCA2-IN-10 induces cell death in SMARCA4-deficient tumors. SMARCA2-IN-10 is promising for research of SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma .
    SMARCA2-IN-10
  • HY-159455

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-4 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-159472); Black: Linker (HY-159478); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-4
  • HY-162835

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a PROTAC-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2 VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)) .
    PROTAC SMARCA2/4-degrader-28
  • HY-161885

    SWI/SNF Complex Cancer
    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 .
    SMARCA2/4-IN-4
  • HY-170354

    Ligands for Target Protein for PROTAC Cancer
    SMARCA2/4-ligand-4 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-ligand-4 can be used for the synthesis of PROTAC SMARCA2/4 degrader-36 (HY-170347) .
    SMARCA2/4-ligand-4
  • HY-162813

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC SMARCA2/4-degrader-25 (compound 7d) is a PROTAC targeting SMARCA2/4. PROTAC SMARCA2/4-degrader-25 is composed of E3 ligase (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and target protein ligand SMARCA2/4-ligand-3 (HY-162814) (red part). The conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845) [1] .
    PROTAC SMARCA2/4-degrader-25
  • HY-162815

    PROTACs Epigenetic Reader Domain Cancer
    PROTAC SMARCA2/4-degrader-26 (compound 6) is a PROTAC targeting SMARCA2/4. SMARCA2 and SMARCA4 are genes and cancer targets with complementary functions that catalyze nucleosome movement. PROTAC SMARCA2/4-degrader-25 is composed of PROTAC target protein ligand 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid (HY-46618) (red part), E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and the conjugate composed of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845) [1] .
    PROTAC SMARCA2/4-degrader-26
  • HY-181909

    PROTACs SWI/SNF Complex Cancer
    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-185075

    LY4050784

    SWI/SNF Complex Cancer
    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

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