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TargetMol | Tags Cytoskeletal Signaling
TargetMol | Tags Metabolism

HSP

Heat shock proteins (HSP) are a family of proteins that are produced by cells in response to exposure to stressful conditions. They were first described in relation to heat shock, but are now known to also be expressed during other stresses including exposure to cold, UV light and during wound healing or tissue remodeling. Many members of this group perform chaperone functions by stabilizing new proteins to ensure correct folding or by helping to refold proteins that were damaged by the cell stress.

  • Tamoxifen
    T690610540-29-1
    • $39
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  • Luminespib
    T1989747412-49-3
    Luminespib (VER-52296) is a new-type inhibitor of HSP90 (IC50s: 7.8/21 nM for HSP90α/β in cell free assay).
    • $52
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  • Elesclomol
    T6170488832-69-5
    Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.
    • $34
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  • IPI-493
    T3218864202-81-9In house
    IPI-493 (17-amino17demethoxy) is a novel HSP90 inhibitor with antitumor activity.
    • $293
    In Stock
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  • PF-04929113 Mesylate
    T43421173111-67-5
    PF-04929113 Mesylate (SNX-5422 Mesylate), a prodrug of SNX-2112, is an orally available Hsp90 inhibitor (Kd: 41 nM) and also induces Her-2 degradation (IC50: 37 nM).
    • $71
    In Stock
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  • DN401
    T271932135749-60-7In house
    DN401 is a potent TRAP1 and Hsp90 Inhibitor( IC50 = 79 nM for TRAP1, IC50 = 698 nM for Hsp90) with potent anticancer activity.
    • $195
    In Stock
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  • Arimoclomol
    T13553289893-25-0
    Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP) and can be used in studies about the treatment of amyotrophic lateral sclerosis (ALS).
    • $195
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  • Shepherdin 79-87 acetate
    T12896L
    Shepherdin 79-87 acetate is a peptidomimetic antagonist of the complex between Hsp90 and survivin, another key regulator of tumor cell viability.
    • $148
    In Stock
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  • TRC051384 HCl
    T35151333327-56-2
    TRC051384 is an inducer of heat shock protein Hsp70, activating heat shock factor-1 and enhancing Hsp72 expression in neurons and glial cells.
    • $45
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  • Novobiocin
    T20510303-81-1
    Novobiocin is an orally active and potent antibiotic.Novobiocin is a DNA gyrase inhibitor and heat shock protein 90 (Hsp90) antagonist with inhibitory effects on gyrase and Hsp90. Novobiocin has anti-positive activity and can be used to study highly resistant pneumococcal infections.
    • $30
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  • p5 Ligand for Dnak and DnaJ acetate
    TP1496L
    p5 Ligand for Dnak and DnaJ acetate is a nonapeptide. It is a high-affinity ligand for DnaK (E. coli Hsp70) and DnaJ (E. coli Hsp40).
    • $133
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  • PU-H71 HCl
    T6960L2095432-24-7
    PU-H71 HCl (Zelavespib HCl) is a novel Hsp90 inhibitor, a novel purine-based analog, and a radiosensitizer that may be a promising agent for CIRT. PU-H71 HCL shows antitumor activity in many preclinical models of malignancy. PU-H71 HCL has an inhibitory effect on the protein expression levels of Rad51 and Ku70, which may be associated with the double chain break repair in the homologous recombination pathway and non-homologous end-joining pathway.
    • $195
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  • SNX0723
    T288241073969-18-2In house
    SNX0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM.
    • $82
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  • Debio 0932
    T150881061318-81-7In house
    Debio 0932 is an orally active inhibitor of HSP90 (IC50s: 100 and 103 nM for HSP90α and HSP90β, respectively).
    • $64
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  • HS-27
    T180181562024-11-6In house
    HS-27 is a fluorescently-tethered inhibitor of Hsp90 with SNX-5422 tethered via a PEG linker to a fluorescein isothiocyanate or FITC. HS-27 can be used in see-and-treat paradigms.
    • $92
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  • Grp94 Inhibitor-1
    T72612234897-35-7
    Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor (IC50 : 2 nM).
    • $41
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  • HA15
    T68551609402-14-3
    HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.
    • $34
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  • VER-50589
    T2258747413-08-7
    VER-50589 is a potent HSP90 inhibitor.
    • $47
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  • Ganetespib
    T2309888216-25-9
    Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
    • $61
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  • Onalespib
    T6284912999-49-6
    Onalespib (AT13387) is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.
    • $41
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  • Tanespimycin
    T629075747-14-7
    Tanespimycin (KOS 953) (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM).
    • $38
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  • Geldanamycin
    T634330562-34-6
    Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.
    • $39
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  • KW-2478
    T6558819812-04-9
    KW-2478 is a non-ansamycin HSP90 inhibitor with IC50 of 3.8 nM.
    • $51
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  • Triptolide
    T217938748-32-2
    Triptolide (PG490) belongs to the tricyclic diterpenoid group of natural products and is an inhibitor of NF-κB activation. Triptolide exhibits immunosuppressive, anti-rheumatic, anti-inflammatory, anti-proliferative and anti-tumor activities.
    • $37
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  • SNX2112
    T6305908112-43-6
    SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.
    • $68
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  • MKT-077
    T5152147366-41-4
    MKT-077 (FJ-776) is a cationic rhodacyanine dye that demonstrates antiproliferative activity against cancer cell lines (EC50s: 1.4-2.2 μM in vitro) through its ability to inhibit members of the Hsp70 family of molecular chaperones.
    • $31
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  • Col003
    T10860328565-16-8
    Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen-binding site on Hsp47 (IC50: 1.8 μM). It can be used for the investigation of fibrosis.
    • $39
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  • VER-155008
    T70101134156-31-2
    VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.
    • $39
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  • Palmitic acid
    T290857-10-3
    Palmitic acid (Cetylic acid) is a natural product, a common saturated fatty acid found in animals, plants and microorganisms. Palmitic acid has antitumor activity.
    • $48
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  • Gamitrinib TPP
    T113551131626-46-4
    Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor exhibiting potent anti-cancer activity. Additionally, Gamitrinib TPP functions as a mitochondrial matrix inhibitor by targeting Gamitrinib (GA).
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  • TRAP1-IN-1
    T79285
    TRAP1-IN-1 (compound 35) is a potent, selective TRAP1 inhibitor affecting the mitochondrial variant of Hsp90. It exhibits over 250-fold greater selectivity for TRAP1 compared to Grp94, destabilizes TRAP1 tetramers, and promotes the degradation of TRAP1 client proteins. Additionally, TRAP1-IN-1 impedes mitochondrial complex I activity involved in oxidative phosphorylation OXPHOS, compromises the mitochondrial membrane potential, and augments glycolytic metabolism [1].
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  • AT-533
    T67836908112-37-8
    AT-533 is a potent inhibitor of Hsp90 and HSV. AT-533 blocks the HIF-1α/VEGF/VEGFR-2 signaling pathway, leading to suppress tumor growth and angiogenesis. AT-533 also inhibits the activation of the downstream pathways, including Erk1/2, FAK, Akt/mTOR/p70S6K,. AT-533 inhibits the cell migration, invasion, and the tube formation of human umbilical vein endothelial cells (HUVECs).
    • $78
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  • Radicicol
    T1671912772-57-5
    Radicicol is an antifungal antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB. Radicicol is an inhibitor of Hsp90 (IC50: 1 μM). Radicicol binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients,
    • $78
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  • Zelavespib hydrochloride
    T80742
    Zelavespib (PU-H71) hydrochloride is a potent inhibitor of Hsp90, exhibiting an IC50 value of 51 nM in MDA-MB-468 cells.
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  • HSP90-IN-27
    T82166525577-38-2
    HSP90-IN-27, also known as compound 19, is an inhibitor of HSP90 [1].
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  • HSP70/SIRT2-IN-2
    T821671796557-72-6
    HSP70/SIRT2-IN-2 (Compounds 1a), a dual inhibitor of SIRT2 and HSP70, exhibits an IC50 of 45.1±5.0 μM against SIRT2 and demonstrates antitumor activity [1].
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  • NCT-58
    T99962411429-33-7
    NCT-58 is a potent C-terminal HSP90 inhibitor. NCT-58 does not induce the heat shock response (HSR). NCT-58 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.
    • $55
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  • Gamitrinib TPP hexafluorophosphate
    T113561131626-47-5
    Gamitrinib TPP hexafluorophosphate is a potent HSP90 inhibitor that specifically targets the mitochondria, demonstrating notable anti-cancer activity. It functions by inhibiting the mitochondrial matrix, making it an effective compound in cancer treatment.
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  • Feretoside
    TQ028027530-67-2
    Feretoside is a natural product extracted from the barks of E. ulmoides. Feretoside shows inducible activity on the heat shock factor 1 (HSF1).
    • $77
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  • BX-2819
    T828021184181-50-7
    BX-2819 is an Hsp90 inhibitor that exhibits potent antiproliferative activity with an IC50 of 41 nM . It effectively suppresses the growth of NCI-N87 and HT-29 tumor cells in nude mice[1].
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  • Chetomin
    T68041403-36-7
    Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.
    • $98
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  • H2-Gamendazole
    T72076877768-84-8
    H2-Gamendazole is a novel compound for spermatogenesis inhibition and cancer therapy as an inhibitor of heat shock proteins and/or elongation factor 1 alpha, and is an Hsp90 regulator.
    • $119
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  • Myricanone
    TN460432492-74-3
    Myricanone has antioxidant, and anticancer activities, it has apoptosis-promoting ability by triggering caspase activation, and suppression of cell proliferation by down-regulation of NF-κB and STAT3 signalling cascades. Myricanone shows in vitro testost
    • $670
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  • HSP90-IN-23
    T78942
    HSP90-IN-23 (Comp 12-1), a heat shock protein 90 (HSP90) inhibitor, exhibits potent activity with an IC50 of 9nM. It promotes apoptosis in tumor cells and arrests their cell cycle at the G0/G1 phase, making it applicable for cancer research [1].
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  • CC-99677
    T393211887069-10-4
    CC-99677 (Gamcemetinib) is a selectively targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune diseases that translates biochemical potency into cellular potency as demonstrated by potent inhibition of heat shock protein 27 (HSP1) phosphorylation in LPS-activated monocyte THP-27 cells via a nucleophilic aromatic substitution (SNAr) mechanism.CC-99677 in Rat experiments demonstrated potency in both biochemical (IC 50 =156.3 nM) and cellular assays (EC 50 =89 nM).
    • $123
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  • 2',4'-DIHYDROXYCHALCONE
    T88291776-30-3
    2',4'-DIHYDROXYCHALCONE (2',4'-DHC) as a compound with Hsp90 inhibitory and antifungal effects
    • $50
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  • NPX800
    T98041693734-80-3
    NPX800 is an inhibitor of heat shock factor 1 (HSF1) and can be used in studies about the treatment of cancer.
    • $97
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  • KNK437
    T2444218924-25-5
    KNK437 (Heat Shock Protein Inhibitor I), a pan-HSP inhibitor, suppresses the synthesis of inducible HSPs(HSP105, HSP72, and HSP40).
    • $52
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  • GRP78-IN-3
    T678972707510-30-1
    GRP78-IN-3, a potent small-molecule-competitive inhibitor of Hsp70 substrate binding and is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM).
    • $44
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  • DDO-5936
    T92022355377-13-6
    DDO-5936 is a potent and specific HSP90-Cdc37 PPI inhibitor.
    • $51
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