hsp90 inhibitor

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

Debio 0932 (CUDC-305) is a heat shock protein 90 (Hsp90) inhibitor that targets the n-terminal atp-binding pocket to promote apoptosis, and has the advantage of being orally available and able to cross the blood-brain barrier (BBB) for the treatment of cancers such as non-small-cell lung cancer (NSCLC) and neuroblastoma.

HS-27 is a fluorescently-tethered inhibitor of Hsp90 with SNX-5422 tethered via a PEG linker to a fluorescein isothiocyanate or FITC. HS-27 can be used in see-and-treat paradigms.

DN401 is a potent TRAP1 and Hsp90 Inhibitor( IC50 = 79 nM for TRAP1, IC50 = 698 nM for Hsp90) with potent anticancer activity.

SNX0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM.

IPI-493 (17-amino17demethoxy) is a novel HSP90 inhibitor with antitumor activity.

DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.

17-AEP-GA is an HSP90 antagonist, a potent inhibitor of glioblastoma cell proliferation, survival, migration, and invasion, and a toxic component of antibody-coupled activated molecules (ADCs), which can be used to study glioblastomas.

KU-177 is a Hsp90 ATPase homolog 1 (Aha1) inhibitor. By disrupting the interaction between Hsp90 and Aha1, it prevents the proliferation of primary MM and relapsed MM patient samples. It eliminates the proliferation and PI resistance induced by AHSA1 elevation.

Ethoxyquin (Santoflex) is an antioxidant used in animal feeds.

Rifabutin (LM-427) inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing the initiation of RNA formation and leading to inhibition of RNA synthesis and transcription. Rifabutin is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties.

Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor exhibiting potent anti-cancer activity. Additionally, Gamitrinib TPP functions as a mitochondrial matrix inhibitor by targeting Gamitrinib (GA).

Gamitrinib TPP hexafluorophosphate is a mitochondrial-targeted HSP90 inhibitor with anticancer activity, which can regulate cell cycle and cell homeostasis and can be used to study cancer, neurodegenerative diseases and viral infections.

Retaspimycin is a potent and water-soluble Hsp90 inhibitor(EC50s of 119 nM for both Hsp90 and Grp9).

Retaspimycin Hydrochloride is a potent and water-soluble Hsp90 inhibitor(Hsp90 and Grp9 with EC50s of 119 nM).

KU-32 is a novel and novobiocin-based Hsp90 inhibitor. It can protect against neuronal cell death.

Radicicol (Monorden) is an antifungal antibiotic and a potent inhibitor of heat shock protein 90 (Hsp90), which leads to the degradation of Hsp90 by the proteasome by binding to its ATP-binding pocket. In addition, Radicicol inhibits the growth and proliferation of several tumor cell lines. It also has anti-malarial activity and acts as an inhibitor of adipose- and obesity-related proteins (FTO). Radicicol inhibits iNOS gene expression by blocking the p38 kinase signaling pathway and NF-kB/Rel

Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8/21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others.

SST0116CL1 is an HSP90 inhibitor (IC50: 0.21 μM) that targets the ATP-binding pocket of Hsp90, disrupting its chaperone function and leading to the degradation of client proteins (EGFR, CDK4, and AKT). It induces the degradation of Her2 in BT-474 cells (IC50: 0.2 μM) and exhibits antiproliferative activity, inhibiting tumor growth.

WK88-1, an inhibitor of Hsp90, effectively induces the degradation of various oncogenic signaling molecules, including EGFR, ErbB2, and ErbB3, in the gefitinib-resistant H1975 cell line. This leads to subsequent growth arrest and apoptosis.

17-Demethoxy-reblastatin (17-DR) acts as an inhibitor of heat shock protein 90 (Hsp90). It suppresses the proliferation of HepG2 and SMMC7721 cancer cells, diminishes colony formation, and triggers apoptosis via a mitochondria and caspase-mediated pathway.

KUNG65 acts as a selective Grp94 inhibitor, demonstrating a target dissociation constant (K_d) of 540 nM. It exhibits a minimum selectivity of 73-fold compared to other Hsp90 isoforms.