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Hsp90 inhibition

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12

Inhibitors & Agonists

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Natural
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15205
    Ganetespib
    Maximum Cited Publications
    42 Publications Verification

    STA-9090

    		 HSP Apoptosis Cancer
    Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
    Ganetespib
  • HY-N6769
    Radicicol
    4 Publications Verification

    Monorden

    		 HSP Bacterial Antibiotic Parasite Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
    Radicicol
  • HY-145102
    NCT-58

    		HSP Apoptosis Cancer
    NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
    NCT-58
  • HY-151335
    KU-177

    		HSP Cancer
    KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research .
    KU-177
  • HY-115781
    DN401
    1 Publications Verification

    Panvotinib-401; Pan-401

    		 HSP Cancer
    DN401 is a potent TRAP1 inhibitor with an IC50 of 79 nM. DN401 shows a weak inhibition of Hsp90 (IC50 of 698 nM). DN401 inactivates mitochondrial TRAP1 and has potent anticancer activities .
    DN401
  • 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-W107935
    Hsp90-IN-37

    		HSP Cancer
    Hsp90-IN-37 (Z-2) is a heat shock protein 90 (Hsp90) inhibitor that inhibits Hsp90 enzymatic activity by 69%. Hsp90-IN-37 has antitumor activity .
    Hsp90-IN-37
  • HY-151137
    HSP90/mTOR-IN-1

    		mTOR HSP Apoptosis Autophagy Cancer
    HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer .
    HSP90/mTOR-IN-1
  • HY-15205R
    Ganetespib (Standard)

    STA-9090 (Standard)

    		 HSP Apoptosis Reference Standards Cancer
    Ganetespib (Standard) is the analytical standard of Ganetespib. This product is intended for research and analytical applications. Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
    Ganetespib (Standard)
  • HY-178955
    EGFR-IN-182

    		EGFR HSP PI3K Caspase Apoptosis CDK ERK Akt Cancer
    EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
    EGFR-IN-182
  • HY-176404
    DDO-6691

    		HSP Cancer
    DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC50: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model .
    DDO-6691
  • 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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