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smarca4-mutant cancers

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153361
    YD23

    		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-168215
    YDR1

    		PROTACs Epigenetic Reader Domain Cancer
    YDR1 is a potent PROTAC SMARCA2 degrader, with the DC50 of 7.7 nM. YDR1 plays an important role in SMARCA4 mutant cancers(Sturcture Note:(Blue: Cereblon ligand (HY-W087383), Black: linker；Pink: SMARCA2 ligand (HY-44012B)) .
    YDR1
  • HY-173351
    G-6599

    		Epigenetic Reader Domain Cancer
    G-6599 is a monovalent molecular glue-like degrader of SMARCA2/SMARCA4. G-6599 covalently binds to a specific cysteine residue of the E3 ligase FBXO22 in a biotransformation-independent manner, promotes the formation of a ternary complex with SMARCA2/A4, and achieves efficient and specific degradation of the two proteins via the ubiquitin-proteasome pathway. G-6599 is applicable to the research of androgen-dependent prostate cancer and mutant non-small cell lung cancer .
    G-6599
  • HY-W494890
    SMARCA2-IN-10

    		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-153425
    PROTAC SMARCA2/4 degrader-41

    		PROTACs Cancer
    PROTAC SMARCA2/4 degrader-41 is a SMARCA2/4 PROTAC degrader with a DC50 and IC50 both < 0.1 μM. PROTAC SMARCA2/4 degrader-41 is applicable to research on SMARCA2/4-related or SMARCA2/4-deficient cancers .
    PROTAC SMARCA2/4 degrader-41
  • HY-185075
    FHD-909

    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
  • HY-183007
    LJM133

    		PROTACs SWI/SNF Complex Cancer
    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
  • HY-182987
    SMARCA2/SMARCA4 ligand-1

    		Ligands for Target Protein for PROTAC SWI/SNF Complex Cancer
    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

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