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HyT and Linkers

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-164807
    SARD279

    		PROTACs Androgen Receptor Cancer
    SARD279 is a potent and selective Androgen Receptor degrader with DC50 value of 1099 nM. SARD279 can be used in prostate cancer research .(Structure Note: Pink: target protein ligand (HY-117486); Blue,: Hyt (HY-W001578); Black: linker (HY-W004896))
    SARD279
  • HY-168682
    Adamantane-Butyl alcohol

    		Target Protein Ligand-Linker Conjugates Cancer
    Adamantane-Butyl alcohol is a selective and persistent degrader targeting the CDK8-cyclin C complex. Adamantane-Butyl alcohol is the linker for LL-K8-22 (PROTAC CDK8-cyclin C, HY-149209) and HyT .
    Adamantane-Butyl alcohol
  • HY-175527
    ALK degrader 2

    		HyT Anaplastic lymphoma kinase (ALK) Apoptosis Inflammation/Immunology Cancer
    ALK degrader 2 is an orally active ALK HyT degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .
    ALK degrader 2
  • HY-161972
    ZX782

    		HyT Ferroptosis Glutathione Peroxidase Cancer
    ZX782 is a HyT GPX4 degrader and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination . ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).
    ZX782
  • HY-181908
    5-Norbornene-2-methylamine-C10-NH2

    		HyT Inflammation/Immunology
    5-Norbornene-2-methylamine-C10-NH2 is a Keap1-targeting hydrophobic tag (HyT)-linker conjugates, containing a HyT (HY-W022007) and a linker (HY-W014831). 5-Norbornene-2-methylamine-C10-NH2 can be used for synthesis of NBE5 (HY-181907) .
    5-Norbornene-2-methylamine-C10-NH2
  • HY-182796
    JNK1 degrader-1

    		HyT JNK Cancer
    JNK1 degrader-1 is a JNK1 HyT degrader. JNK1 degrader-1 can induce JNK1 degradation through the HyT-mediated ubiquitin-proteasome system and autophagy-lysosome pathway. JNK1 degrader-1 inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT). JNK1 degrader-1 can be used for research on fibrotic diseases and cancer metastasis. (Pink: JNK1 ligand (HY-183006); Blue: Hyt hydrophobic group (HY-W037848); Black: Linker (HY-B1008)) .
    JNK1 degrader-1
  • HY-170376
    2-(2-Aminoethoxy)ethyl 2-(adamantan-1-yl)acetate

    		E3 Ligase Ligand-Linker Conjugates Others
    2-(2-Aminoethoxy)ethyl 2-(adamantan-1-yl) acetate is a conjugate of an Hyt hydrophobic group and a linker, which can be used in the synthesis of SARD279 (HY-164807) .
    2-(2-Aminoethoxy)ethyl 2-(adamantan-1-yl)acetate
  • HY-161974
    Adamantan-C-amide-PEG2-C-Br

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Adamantan-C-amide-PEG2-C-Br is a conjugate of a Hyt hydrophobic group and a linker. Adamantan-C-amide-PEG2-C-Br can be used to synthesize ZX782 (HY-161972) .
    Adamantan-C-amide-PEG2-C-Br
  • HY-181460
    PARP1 degrader-2

    		HyT PARP Cancer
    PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC50: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)) .
    PARP1 degrader-2
  • HY-181907
    NBE5

    		HyT Keap1-Nrf2 HSP Inflammation/Immunology
    NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C) .
    NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
    NBE5

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