HSP Inhibitor

SST0116CL1 free base is a HSP90 inhibitor (IC₅₀: 0.21 μM). SST0116CL1 free base binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 free base induces degradation of Her2 in BT-474 cell (IC₅₀: 0.2 μM). SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base can be used for the study of leukemia, gastric and ovarian carcinoma.

Alvespimycin (Standard) is the analytical standard of Alvespimycin (HY-10389). This product is intended for research and analytical applications. Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC₅₀ of 62 nM.

Luminespib (Standard) is the analytical standard of Luminespib. This product is intended for research and analytical applications. Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.

HSP90-IN-29 (Compound 13), a benzoxazole derivative, is a potent and selective HSP-90 inhibitor with an IC₅₀ value of 30 nM. HSP90-IN-29 has antitumor activity.

HS-72 is a selective allosteric inducible heat shock protein 70 Hsp70i inhibitor. HS-72 reduces ATP affinity of Hsp70i, elevates caspase 3/7 apoptotic activity, and promotes degradation of Hsp70 client proteins, including HER2 and Akt, and blocks DENV entry by disrupting Hsp70i association with the DENV receptor complex. HS-72 can be used for breast cancer and dengue virus infection research.

HA15 (Standard) is the analytical standard of HA15 (HY-100437). This product is intended for research and analytical applications. HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.

2-Chloro-ADP (2-Chloroadenosine 5′-diphosphate) sis a Adenosine 5'-diphosphate (ADP; HY-W010918) derivative that induces human platelet aggregation and inhibits stimulated adenylate cyclase. 2-Chloro-ADP inhibits mortalin nucleotide-binding domain (NBD) with a K_i of 45.05 μM.

VER-82576 (Standard) is the analytical standard of VER-82576 (HY-10942). This product is intended for research and analytical applications. VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC₅₀ of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC₅₀s of 4.1 and 5.5 μM, respectively.

C086, a novel potent Hsp90 inhibitor, could inhibit cell cycle progression and induce cell apoptosis and anti-metastasis by regulating various mechanisms in different cell types.

Ganetespib (Standard) is the analytical standard of Ganetespib. This product is intended for research and analytical applications. Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3.

NSC145366 monohydrochloride is a Hsp90 C-terminal inhibitor. NSC145366 monohydrochloride directly interacts with the C-terminus of Hsp90 and inhibits its chaperone activity. NSC145366 monohydrochloride strongly inhibits the growth of Saccharomyces cerevisiae cog7Δ and cog8Δ strains.

SU086 is a chalcone-derived HSP90 inhibitor. SU086 interacts with HSP90, reduces HSP90 protein levels, and suppresses glycolysis in prostate cancer cells. SU086 can be used in research related to advanced prostate cancer and castration-resistant prostate cancer (CRPC).

Pifithrin-μ (Standard) is the analytical standard of Pifithrin-μ. This product is intended for research and analytical applications. Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

STA-1474 sodium is an orally active and highly selective HSP90 inhibitor, as well as a phosphate prodrug of the HSP90 inhibitor STA-9090 (HY-15205). STA-1474 sodium disrupts the chaperone function of HSP90 and promotes the degradation of client proteins. STA-1474 sodium inhibits the phosphorylation of Met, Akt and STAT3, thereby blocking related signaling pathways. STA-1474 sodium induces apoptosis and inhibits proliferation of osteosarcoma cells, and triggers the up-regulation of HSP70 and HSP90. STA-1474 sodium induces tumor regression and caspase-3 activation in mouse osteosarcoma xenograft models. STA-1474 sodium can be used in the research of osteosarcoma.

Pochonin D ((+)-Pochonin D) is an inhibitor of heat shock protein 90 (Hsp90) with antiviral and anti-inflammatory activities. Pochonin D inhibits Hsp90, affects the homeostasis, folding and assembly processes of viral proteins, and reduces the replication capacity of viruses. Pochonin D is a copper ion carrier that can induce cuproptosis in triple-negative breast cancer cells by targeting PRDX1. Pochonin D reduces the infiltration of inflammatory cells, decreases the secretion of inflammatory cytokines such as TNF-α and IL-1β, and alleviates inflammatory responses. Pochonin D is a promising candidate for research on human rhinovirus (HRV) infection and cancer.

EG36 is a selective E. coli DnaK inhibitor that inhibits DnaK ATPase activity at a concentration of 100 μM. EG36 directly binds to the nucleotide-binding domain (NBD) of E. coli DnaK by disrupting the DnaK-DnaJ interaction. EG36 can be used for research on bacterial infectious diseases.

HSP70-IN-5 is a HSP70 inhibitor. HSP70-IN-5 exhibits IC₅₀ value for HSP70/DnaJ-mediated luciferase reconstitution of 0.6 μM. HSP70-IN-5 can be used as a biochemical probe to study the role of HSP70/DnaJ in various biological processes.

19-epi-Scholaricine is an orally active indole alkaloid. 19-epi-Scholaricine downregulates the expression of profibrotic/apoptotic proteins (HRAS, HSP90AA1, KDR) and upregulates the expression of cell cycle-related protein (CDK2). 19-epi-Scholaricine suppresses ROS production and reduces the release of inflammatory mediators, thereby attenuating podocyte apoptosis, renal inflammation and oxidative stress by inhibiting AKT/mTOR. 19-epi-Scholaricine can be used in the research of chronic glomerulonephritis and membranous nephropathy.

Caesappanin C, a biphenyl dimer from the ethanolic extract of the heartwood of Indonesian Caesalpinia sappan L., shows strong proliferation stimulating activity against the primary osteoblastic cells in vitro. Caesappanin C has the potential to stimulate bone formation and regeneration. Caesappanin C can effectively deactivate HSV particles and bind HSV surface glycoprotein B (gB) to inhibit membrane fusion.

Hsp90-IN-34 (compound HAM-1) is a compound that inhibits the Aha1-Hsp90 chaperone complex with a high affinity for Hsp90/Aha1 (K_Dapp=23.5 µM). Hsp90-IN-34 modulates the ATPase activity of Hsp90 by affecting the interaction between Hsp90 and Aha1.