HSP Inhibitor

Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC₅₀ of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC₅₀ of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice.

Monorden diacetate serves as a promising lead compound in the development of novel fungicides due to its potential as an Hsp90 inhibitor.

Aha1/Hsp90-IN-2 is a selective inhibitor of the Hsp90/Aha1 interaction, with its IC₅₀ being 1.46 μM. Aha1/Hsp90-IN-2 inhibits the activation of Hsp90 ATPase activity mediated by Aha1 by specifically blocking the binding of Hsp90 to Aha1, thereby reducing tau protein aggregation. Aha1/Hsp90-IN-2 can be used for the study of neurodegenerative diseases, such as Alzheimer's disease.

Grp94 Inhibitor-3 (Compound C6) is a selective glucose regulated protein 94 (Grp94) inhibitor with an affinity of 5.52 μM. Grp94 Inhibitor-3 is promising for research of primary open-angle glaucoma and metastatic cancer.

NSC-134754 (NZ-28) is a dehydroemetine derivative and heat shock protein (HSP) induction inhibitor. NSC-134754 acts at the post-transcriptional level, targets Hsp72 and Hsp27, and does not alter general protein synthesis, HSF-1 transcriptional activity, or Hsp mRNA levels. NSC-134754 can be used for the research of multiple myeloma, prostate carcinoma, colon carcinoma.

CYD0682 is an analog of Oridonin (HY-N0004). CYD0682 attenuates STAT3 activation and ECM production via an HSP90 pathway in hepatic stellate cells.

CPUY201112 is a potent heat shock protein Hsp90 inhibitor with K_d of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research.

Hsp90-IN-36 (compound 5) is a Hsp90 inhibitor with anticancer activity (MCF-7, IC₅₀=14.74 μM).

Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy.

Autophagy activator-1 (Compound B2) is an autophagy activator Autophagy. Activator-1 ultimately leads to the activation of autophagy by downregulating key members of the HSP70 family and activating the unfolded protein response.

Malonganenone A is an antimalarial marine alkaloid that disrupts the interaction between PfHsp70-x and Hsp40. Malonganenone A inhibits plasmodial and not human Hsp70 ATPase activity (Hsp40-stimulated), and hindered the aggregation suppression activity of PfHsp70-x.

Iso-PU-H54 is a purine-scaffold Grp94 inhibitor with an IC₅₀ of 1.63 μM.

Ethoxyquin (Standard) is the analytical standard of Ethoxyquin. This product is intended for research and analytical applications. Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90).

Hsp90-IN-43 (Compound 12) is a Hsp90-TPR2A interaction inhibitor with an IC₅₀ of 360 nM and a K_d of 928 nM. Hsp90-IN-43 effectively inhibits the proliferation of BT474 cells. Hsp90-IN-43 can be used for the study of breast cancer.

HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven breast cancers, including multiple different molecular subtypes of human breast cancers.

BIIB021 (CNF2024) mesylate is the mesylate of BIIB021 (HY-10212). BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC₅₀ values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML.

FKBP51-Hsp90-IN-2 (Compound E08) is a selective FKBP51-Hsp90 protein-protein interaction inhibitor with IC₅₀ values of 0.4 µM and 5 µM for FKBP51 and FKBP52, respectively. FKBP51-Hsp90-IN-2 also effectively stimulates cellular energy metabolism and neurite growth. FKBP51-Hsp90-IN-2 can be used in research on neurodegenerative diseases and cancer.

6BrCaQ is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity. 6BrCaQ can be used in the synthesis of 6BrCaQ-TPP conjugates.

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.