1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  3. HSP

HSP

Heat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heat shock, the most prominent members of this group are a class of functionally related proteins involved in the folding and unfolding of other proteins. HSP expression is increased when cells are exposed to elevated temperatures or other stress. This increase in expression is transcriptionally regulated. The dramatic upregulation of the heat shock proteins is a key part of the heat shock response and is induced primarily by heat shock factor (HSF). HSPs are found in virtually all living organisms, from bacteria to humans. Heat shock proteins appear to serve a significant cardiovascular role. Hsp90, Hsp84, Hsp70, Hsp27, Hsp20 and alpha B crystallin all have been reported as having roles in the cardiovasculature.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-113916
    Onalespib lactate
    Inhibitor
    Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC).
    Onalespib lactate
  • HY-145559
    Cemdomespib
    Inhibitor
    Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response.
    Cemdomespib
  • HY-P1750
    Shepherdin (79-87)
    Antagonist
    Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity.
    Shepherdin (79-87)
  • HY-146420
    GRP78-IN-2
    Inhibitor
    GRP78-IN-2 (Compound FL5) is a GRP78 (Glucose Regulated Protein 78 kDa) inhibitor. GRP78-IN-2 preferentially targeting cell surface GRP78 and shows potent antiangiogenic and anticancer activities without affecting other normal cells.
    GRP78-IN-2
  • HY-149431
    NDNA4
    Inhibitor
    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-123035
    Gamendazole
    Inhibitor
    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-N3377
    Liriodendrin
    Agonist
    Liriodendrin is an HSF1 agonist can be isolated from E. ulmoides.
    Liriodendrin
  • HY-N0830S11
    Palmitic acid-d2-1
    Activator
    Palmitic acid-d2-1 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
    Palmitic acid-d<sub>2</sub>-1
  • HY-19399B
    Iroxanadine sulfate
    Activator
    Iroxanadine (BRX 005) sulfate is a vasculoprotector. Iroxanadine is a p38 kinase and HSP protein dual activator. Iroxanadine sulfate has the potential for atherosclerosis and vascular diseases research.
    Iroxanadine sulfate
  • HY-146325
    HSP90-IN-11
    Inhibitor
    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-P1887
    p5 Ligand for Dnak and DnaJ
    p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ.
    p5 Ligand for Dnak and DnaJ
  • HY-157085
    BX-2819
    Inhibitor
    BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice.
    BX-2819
  • HY-162589
    Lw13
    Degrader
    Lw13 is a Hsp90-targeting PROTAC and achieves maximum degradation at a concentration of 0.05 μM in Siha cells. Lw13 induces cell apoptosis and exhibits potent anti-tumor activity both in vitro and in vivo(Sturcture Note:(Blue: Cereblon ligand (HY-A0003), Black: linker;Pink: Hsp90 inhibitor SNX-5422 (HY-10213)).
    Lw13
  • HY-130624
    Hsp90-Cdc37-IN-2
    Inhibitor
    Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549.
    Hsp90-Cdc37-IN-2
  • HY-163288
    EZH2/HSP90-IN-29
    Inhibitor
    EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).
    EZH2/HSP90-IN-29
  • HY-15990
    CH5164840
    Inhibitor
    CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy.
    CH5164840
  • HY-139009
    HA15-Biotin
    Inhibitor
    HA15-Biotin is a chemical probe that consists of HA15 and biotin attached on the amide part of HA15. HA15-Biotin exhibits similar levels of activity to HA15. HA15-Biotin can be used for proteomic analysis.
    HA15-Biotin
  • HY-164372
    17-Demethoxy-reblastatin
    Inhibitor
    17-Demethoxy-reblastatin (17-DR) is an inhibitor for heat shock protein 90 (Hsp90), with an IC50 of 1.82 μM for yeast Hsp90 ATPase. 17-Demethoxy-reblastatin inhibits the proliferation of cancer cell HepG2 and SMMC7721, reduces the colony formation, and induces apoptosis through mitochondria and caspase mediated pathway.
    17-Demethoxy-reblastatin
  • HY-107578
    Macbecin
    Inhibitor
    Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities.
    Macbecin
  • HY-149432
    NDNA3
    Inhibitor
    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
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