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client protein degradation

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-107577

    HSP Infection Inflammation/Immunology Cancer
    Gedunin is a limonoid with anti-cancer, anti-viral, anti-inflammatory and insecticidal activities. Gedunin acts as a potent Hsp90 inhibitor and induces the degradation of Hsp90-dependent client proteins. Geduni may obstructs the entry of SARS-CoV-2 virus into human host cells and can be used for COVID-19 research .
    Gedunin
  • HY-155063

    HSP Mitochondrial Metabolism Cancer
    TRAP1-IN-1 (compound 35) is a potent and selective inhibitor of TRAP1,a mitochondrial isoform of Hsp90. TRAP1-IN-1 has >250-fold TRAP1 selectivity over Grp94,and disrupts TRAP1 tetramer stability,induces TRAP1 client protein degradation. TRAP1-IN-1 also inhibits mitochondrial complex I of oxidative phosphorylation OXPHOS,disrupts the mitochondrial membrane potential,and enhances glycolysis metabolism .
    TRAP1-IN-1
  • HY-147125

    HSP Akt CDK Raf Cancer
    DDO-6600 is a covalent Hsp90 inhibitor. DDO-6600 disrupts the interaction between Hsp90 and its co-chaperone protein Cdc37, thereby inducing the degradation of kinase client proteins (such as AKT, CDK4, c-Raf). DDO-6600 has inhibitory activity against various cancer cells. DDO-6600 inhibits the migration and invasion of HCT-116 cells, and induces cell cycle arrest and apoptosis. DDO-6600 significantly inhibits tumor growth in the HCT-116 xenograft tumor model. DDO-6600 can be used for research on colorectal cancer .
    DDO-6600
  • HY-12933

    HSP Cancer
    BIIB-028 is an orally active inhibitor for heat shock protein 90 (Hsp90). BIIB-028 targets the ATP-binding site of Hsp90, disrupts the function of Hsp90, leads to the degradation of client proteins, that are crucial for cancer cell survival and proliferation .
    BIIB-028
  • HY-149431

    HSP Potassium Channel Cancer
    NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
    NDNA4
  • HY-164399

    HSP EGFR CDK Akt Cancer
    SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth. SST0116CL1 can be used for the study of leukemia, gastric and ovarian carcinoma .
    SST0116CL1
  • HY-149432

    HSP Potassium Channel Cancer
    NDNA3 (compound 14) is a selective inhibitor of Hsp90α (IC50: 0.51 μM). NDNA3 is a permanently charged analog with low membrane permeability and low toxicity to Ovcar-8 (IC50: 12.66 μM) and MCF-10A (IC50: 11.72 μM) cells. NDNA3 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
    NDNA3
  • HY-146325

    HSP Cancer
    HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
    HSP90-IN-11
  • HY-171334A

    PROTACs PIN1 CDK Akt c-Myc Apoptosis Reactive Oxygen Species (ROS) Cancer
    P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883) .
    P1D-34

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