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-102007
    Gamitrinib TPP
    Inhibitor
    Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
    Gamitrinib TPP
  • HY-13757S
    Tamoxifen-d3 hydrochloride
    Activator 98.99%
    Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen-d<sub>3</sub> hydrochloride
  • HY-W134007S1
    Hexadecanoate-13C16 potassium
    Activator 98.40%
    Hexadecanoate-13C16 (potassium) is the 13C-labeled Hexadecanoate sodium. Hexadecanoate potassium 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].
    Hexadecanoate-<sup>13</sup>C<sub>16</sub> potassium
  • HY-P1896
    Hsp70-derived octapeptide
    98.01%
    Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs.
    Hsp70-derived octapeptide
  • HY-13301
    MPC-3100
    Inhibitor 98.3%
    MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of Hsp90 with potential antineoplastic activity.
    MPC-3100
  • HY-155063
    TRAP1-IN-1
    Inhibitor
    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-155113
    PROTAC Hsp90α degrader 1
    Degrader
    PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively.
    PROTAC Hsp90α degrader 1
  • HY-138820
    SW02
    Activator 98.30%
    SW02 is a potent activator of ATPase activity of Hsp70, with an EC50 of 150 μM. SW02 leads to accumulation of both total tau and phosphorylated tau (pTau).
    SW02
  • HY-N6679A
    10,11-Dehydrocurvularin
    Activator 99.75%
    10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
    10,11-Dehydrocurvularin
  • HY-147696
    SMTIN-T140
    Inhibitor 99.58%
    SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells.
    SMTIN-T140
  • HY-133571
    Aminohexylgeldanamycin
    Inhibitor 99.56%
    Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities.
    Aminohexylgeldanamycin
  • HY-115781
    DN401
    Inhibitor ≥99.0%
    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-119906
    Conglobatin
    Inhibitor
    Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.
    Conglobatin
  • HY-N0830S10
    Palmitic acid-13C2
    Activator 99.54%
    Palmitic acid-13C2 is the 13C-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-<sup>13</sup>C<sub>2</sub>
  • HY-N6249
    Feretoside
    Activator 98.69%
    Feretoside, a phenolic compound extracted from the barks of E. ulmoides, is a HSP inducer which act as cytoprotective agent.
    Feretoside
  • HY-12834
    MK2-IN-1
    Inhibitor 99.04%
    MK2-IN-1 (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 impaires the phosphorylation level of serine residues in the Tfcp2l1 protein.
    MK2-IN-1
  • HY-106443
    Arimoclomol
    Activator
    Arimoclomol (BRX-220 free base) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.Arimoclomol can be used for the study of Niemann–Pick disease type C.
    Arimoclomol
  • HY-106443B
    Arimoclomol citrate
    Activator
    Arimoclomol citrate (BRX-220 citrate) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system. Arimoclomol citrate can be used for the study of Niemann–Pick disease type C.
    Arimoclomol citrate
  • HY-151137
    HSP90/mTOR-IN-1
    Inhibitor
    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-147039
    BOLD-100 free base
    Inhibitor
    BOLD-100 (NKP-1339; IT-139) free base is a ruthenium-based anticancer agent. BOLD-100 free base also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 free base interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution.
    BOLD-100 free base
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