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-N17756
    Withanolide D
    Withanolide D (Compound 2) is a steroidal ester found in Withania somnifera (L.) Dunal, with anticancer activity. Withanolide D can activate the heat-shock factor 1 (HSF1)-dependent stress response. Withanolide D can be used for the research of cancer such as lymphoma.
    Withanolide D
  • HY-181727
    AR/AR-V7 degrader-1
    		Inhibitor
    AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer.
    AR/AR-V7 degrader-1
  • 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.
    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-181147
    PROTAC HSP70 Degrader-1
    		Degrader
    PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia.
    PROTAC HSP70 Degrader-1
  • 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-156566
    PROTAC BRD4 Degrader-21
    		Degrader
    PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma.
    PROTAC BRD4 Degrader-21
  • 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-P11052
    A8 peptide
    		Antagonist
    A8 peptide is a Hsp72 antagonist. A8 peptide inhibits tumor progression and metastasis as well as enhances the cancer cells' sensitivity to apoptosis induced by chemotherapeutic agents (such as Cisplatin (HY-17394)) by blocking the Hsp72-TLR2 interaction and the subsequent activation of MDSCs. A8 peptide can be used for cancers research.
    A8 peptide
  • 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-181062
    VWK147
    		Inhibitor
    VWK147 is a second-generation HSP90 C-terminal domain (CTD) inhibitor. VWK147 targets the CTD dimerization interface, prevents HSP90 CTD dimerization, disrupts co-chaperone PPID binding to HSP90 CTD, and inhibits HSP90 chaperone function dependent on dimerization. VWK147 reduces protein levels of HSP90 client proteins ULK1, RIPK1, and CDK4 without inducing a heat shock response. VWK147 induces cell death, including apoptosis, in Cisplatin (HY-17394)-sensitive and -resistant urothelial carcinoma cells. VWK147 induces LC3-II accumulation, inhibits autophagosome-lysosome fusion to block canonical autophagy, and induces non-canonical LC3 lipidation independent of ULK1 and PIK3C3 complexes. VWK147 can be used for the research of urothelial carcinoma.
    VWK147
  • 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-182979
    HSP70 ligand 2
    		Ligand
    HSP70 ligand 2 is an HSP70 ligand and serves as a ligand for PROTAC target proteins. HSP70 ligand 2 can be used to synthesize Hsp70TAC BRD4 Degrader-1 (HY-182958) and Hsp70TAC PD-1 Degrader-2 (HY-182959).
    HSP70 ligand 2
  • 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
  • HY-152028
    HSP90-IN-19
    		Inhibitor
    HSP90-IN-19 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-19 has effective Hsp90 inhibitory activity with an IC50 value of 0.27 μM. HSP90-IN-19 can be used for the research of viral infection, neurodegenerative disease, and inflammation.
    HSP90-IN-19
Cat. No. Product Name / Synonyms Application Reactivity
HSP Isoform Comparison

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