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

HSP

Heat shock proteins

HSP

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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.

HSP Isoform Specific Products:

HSP Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-144650
    Hsp90-Cdc37-IN-3
    		Inhibitor 98.09%
    Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis.
    Hsp90-Cdc37-IN-3
  • HY-100555
    CH5138303
    		Inhibitor 99.05%
    CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.
    CH5138303
  • HY-105063
    DiaPep277
    		99.89%
    DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes.
    DiaPep277
  • HY-N1455
    Falcarinol
    		Inhibitor ≥98.0%
    Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis. Falcarinol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Falcarinol
  • HY-11038B
    Zelavespib hydrochloride
    		Inhibitor 98.89%
    Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
    Zelavespib hydrochloride
  • HY-B0779A
    (5E,9E,13E)-Teprenone
    		99.88%
    (5E,9E,13E)-Teprenone ((5E,9E,13E)-Geranylgeranylacetone) is an isomer of Teprenone with antiulcer activity. (5E,9E,13E)-Teprenone induces transcriptional activation of HSP genes that may increase gastric mucosal defense at conditions of stress.
    (5E,9E,13E)-Teprenone
  • HY-117395
    PU-H54
    		Inhibitor 99.04%
    PU-H54, a Grp94-selective inhibitor, can be used for the research of breast cancer. Hsp90 chaperone family, comprised in humans of four paralogs, Hsp90α, Hsp90β, Grp94 and Trap-1, has important roles in malignancy. PU-H54 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PU-H54
  • 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-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-145722A
    Apatorsen
    		Inhibitor
    Apatorsen is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.
    Apatorsen
  • HY-U00398
    Bimoclomol
    		Activator 99.29%
    Bimoclomol is a heat shock protein (HSP) coinducer, used for treatment of cardiovascular diseases.
    Bimoclomol
  • HY-144867
    CCT245232
    		99.37%
    CCT245232 is a potent inhibitor of heat shock factor 1 (HSF1). HSF1 is the master regulator of the heat shock response, in which multiple genes are induced in response to temperature increase and other stresses. CCT245232 has the potential for the research of proliferative diseases, such as cancer (extracted from patent WO2015049535A1).
    CCT245232
  • HY-114413
    YZ129
    		Inhibitor 99.85%
    YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration.
    YZ129
  • 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-148215A
    Hsp90-IN-17 hydrochloride
    		Inhibitor 99.27%
    Hsp90-IN-17 (Example 5) hydrochloride is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases.
    Hsp90-IN-17 hydrochloride
  • HY-13757AS
    Tamoxifen-d5
    		Activator 99.99%
    Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
    Tamoxifen-d<sub>5</sub>
  • HY-149814
    PDK-IN-1
    		Inhibitor 99.74%
    PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass.
    PDK-IN-1
  • HY-156779
    HSP90-IN-27
    HSP90-IN-27 (compound 19) is an HSP90 inhibitor.
    HSP90-IN-27
  • HY-W010649
    Isoxazole
    		Inhibitor 99.98%
    Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor​.
    Isoxazole
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
HSP Isoform Comparison

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