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Results for "

Client proteins

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-120909
    YK5

    		HSP Apoptosis Cancer
    YK5 is a potent and selective Hsp70 inhibitor. YK5 selectively and tightly binds to the cytosolic Hsp70s in cancer cells. YK5 has biological activity partly by interfering with the formation of active oncogenic Hsp70/Hsp90/client protein complexes .
    YK5
  • HY-120548
    KBU2046

    		HSP Cancer
    KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life .
    KBU2046
  • HY-107577
    Gedunin

    		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-176763
    KZR-261

    		Sec61 Apoptosis Caspase Cancer
    KZR-261 is a Sec61 inhibitor. KZR-261 directly binds to the Sec61 channel to potently inhibit the biogenesis of a subset of Sec61 client proteins. KZR-261 has a broad antitumor activity (such as colorectal pancreas and prostate cancer), along with the activation of an endoplasmic reticulum stress response, with minimal adverse effects on normal cells. KZR-261 significantly induces apoptosis of H929 cells. KZR-261 potently inhibits tumor growth in multiple xenograft tumor mice models with good tolerance .
    KZR-261
  • HY-12933
    BIIB-028

    		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-155064
    TRAP1-IN-2

    		HSP Metabolic Disease
    TRAP1-IN-2 (compound 36) is a selective degrader of TRAP1 downstream proteins without affecting Hsp90's cytoplasmic downstream proteins. TRAP1-IN-2 also inhibits OXPHOS and alters cellular glycolysis metabolism. TRAP1-IN-2 destabilizes TRAP1 tetramers and disrupts mitochondrial membrane potential.
    TRAP1-IN-2
  • HY-149431
    NDNA4

    		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-146212
    HDAC/HSP90-IN-4

    		HDAC HSP Cancer
    These compounds have strong hdac and hsp90 inhibitory activities. Compound 20 (HDAC ic50   =   194   nm; Hsp90 α < b> Ic50 =   153   nm) and compound 26 ((HDAC ic50=   360   nm; Hsp90 α < b> Ic50   =   77   nm) shows the strongest HDAC and HSP90 α Inhibitory activity. Both compounds can induce hsp90 expression and down regulate hsp90 client proteins, which play an important role in regulating the survival and invasion of cancer cells.
    HDAC/HSP90-IN-4
  • HY-149432
    NDNA3

    		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-164399
    SST0116CL1

    		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
  • HY-155063
    TRAP1-IN-1

    		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-146325
    HSP90-IN-11

    		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-161781
    HVH-2930

    		HSP EGFR Akt Survivin Cancer
    HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab (HY-P9907) sensitive) and JIMT-1 (Trastuzumab (HY-P9907) resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclin D1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice .
    HVH-2930
  • HY-123035
    Gamendazole

    		HSP Akt EGFR Endocrinology
    Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research .
    Gamendazole
  • HY-171334A
    P1D-34

    		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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