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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
    Tamoxifen (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.
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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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  • 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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  • 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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  • 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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  • 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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  • Luminespib
    T1989747412-49-3
    Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8 21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others.
    • $52
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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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  • Eupalinolide A
    T5826877822-40-7
    Eupalinolide B is a natural product ,and demonstrates potent cytotoxicity against A-549, BGC-823, SMMC-7721, and HL-60 tumour cell lines.
    • $66
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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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  • 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
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  • IPI-493
    T3218864202-81-9In house
    IPI-493 (17-amino17demethoxy) is a novel HSP90 inhibitor with antitumor activity.
    • $293
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  • Arimoclomol maleate
    T13554289893-26-1
    Arimoclomol maleate (BRX-220) (BRX-220) is a heat shock protein (HSP) co-inducer.
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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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  • Gedunin
    T218832753-30-2
    Gedunin is an important limonoid present in several genera of the Meliaceae family, mainly in seeds. Gedunin is an Hsp90 inhibitor, and inhibits ovarian cancer cell proliferation.
    • $248
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  • JG-98
    T53501456551-16-8
    JG-98 is an allosteric Hsp70 inhibitor, displays high active against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50s: 0.4 0.7 μM).
    • $102
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  • Dihydroberberine
    T8189483-15-8
    Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces Hsp90 expression and its interaction with hERG.
    • $41
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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
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  • Col003
    T10860328565-16-8
    Col003 is a selective and potent inhibitor of Hsp47, competitively binding to the collagen-binding site on Hsp47 (IC50: 1.8 μM). It is useful for researching fibrosis.
    • $39
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  • HSF1A
    T41251196723-93-9
    HSF1A is a cell-permeable activator of HSF1 that protects mammalian cells against stress-induced apoptosis (HSF1).
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  • KRIBB11
    T3652342639-96-7
    KRIBB11 is an inhibitor of Heat Shock Factor (HSF) [inhibitor].
    • $47
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  • 3-Phenyltoxoflavin
    T3612332502-63-9
    3-Phenyltoxoflavin (Phenyltoxoflavin) is an inhibitor of HSP90 (Kd = 585 nM) with anti-cancer activity.
    • $58
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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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  • HSP27 inhibitor J2
    T72652133499-85-9
    HSP27 inhibitor J2 (J2) (J2) is a HSP27 inhibitor, inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function.
    • $79
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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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  • Rocaglamide
    TQ013184573-16-0
    Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.
    • $299
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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.
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  • VER-50589
    T2258747413-08-7
    VER-50589 is a potent HSP90 inhibitor.
    • $47
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  • VER49009
    T2268940289-57-6
    VER49009 (CCT0129397) is an effective HSP90 inhibitor(IC50 =25 nM, Kd=78 nM).
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  • XL888
    T62481149705-71-4
    XL888 is an ATP-competitive inhibitor of Hsp90 ( IC50: 24 nM). Heat shock protein 90 (Hsp90) is a chaperone that maintains the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis. Through this action, specific clie
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  • Paeoniflorin
    T223023180-57-6
    Paeoniflorin (Peoniflorin) is a herbal constituent extracted from the root of Paeonia albiflora Pall.
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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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  • AMP-PCP disodium
    T13547L7414-56-4
    AMP-PCP disodium, an ATP analogue, binds to the N-terminal domain of Hsp90 with a Kd value of 3.8 μM, facilitating the formation of an active Hsp90 homodimer.
    • $64
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  • TRC051384
    T3527867164-40-7
    TRC051384 is a heat shock protein 70 (HSP70) inducer that reduces stroke-associated neuronal damage and increases survival in a rat model of transient ischemic stroke, activates heat shock factor-1 and leads to elevated molecular chaperone and anti-inflammatory activity, and enhances Hsp72 expression in neurons and glial cells.
    • $31
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  • NVP-HSP990
    T6118934343-74-5
    NVP-HSP990 (HSP990) is an effective and specific HSP90α β inhibitor (IC50: 0.6 0.8 nM).
    • $41
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  • VER-49009
    T3454558640-51-0
    VER-49009 (CCT 129397) is a potent Hsp90 inhibitor(IC50 of 25 nM and Kd of 78 nM).
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  • Teprenone
    T50086809-52-5
    Teprenone (Geranylgeranylacetone) is a anti-ulcer drug, and works as an inducer of heat shock proteins (HSPs).
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  • Pifithrin-μ
    T621064984-31-2
    Pifithrin-μ (NSC-303580) is an inhibitor of p53 and HSP70, with neuroprotective and antitumor activity.
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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.
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  • Ganetespib
    T2309888216-25-9
    Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90), exhibiting potential antineoplastic activity.
    • $61
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  • CCT018159
    T21872171009-07-7
    CCT018159 is a 3,4-diarylpyrazole resorcinol, an ATP-competitive HSP90ATPase inhibitor that inhibits human Hsp90β and yeast Hsp90 with IC50s of 3.2 and 6.6 μM, respectively.CCT018159 inhibits key endothelial and tumor cell functions associated with invasion and angiogenesis. CCT018159 caused cellular inhibition associated with G1 phase block and induced apoptosis.
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  • Apoptozole
    T32931054543-47-3
    Apoptozole (Apoptosis Activator VII) inhibits the ATPase domain of Hsc70 and Hsp70, inducing apoptosis.
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  • Pimitespib
    T169941260533-36-5
    Pimitespib (TAS-116) is an ATP-competitive and highly specific HSP90α HSP90β inhibitor with inhibition constants (Kis) of 34.7 nM and 21.3 nM, respectively.
    • $33
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  • Falcarinol
    TN236021852-80-2
    Falcarinol (Panaxynol) is an Hsp90 inhibitor and CB1 receptor antagonist that inhibits the action of amphetamine on TNF-α-stimulated keratinocytes.
    • $440
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  • HSP70-IN-1
    T34871268273-90-0
    HSP70-IN-1 is a heat shock protein (HSP) inhibitor that suppresses the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
    • $97
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  • DTHIB
    T8858897326-30-6
    DTHIB robustly inhibits the HSF1 cancer gene signature and prostate cancer cell proliferation.
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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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  • PF04929113
    T6341908115-27-5
    PF04929113 (SNX-5422) is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, PF04929113 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers.
    • $33
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  • Ethoxyquin
    T075691-53-2
    Ethoxyquin (Santoflex) is an antioxidant used in animal feeds.
    • $29
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  • Rifabutin
    T150172559-06-9
    Rifabutin (LM-427) inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing the initiation of RNA formation and leading to inhibition of RNA synthesis and transcription. Rifabutin is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties.
    • $42
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