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HSP90 Inhibitor
AT13387 is a targeted inhibitor of Hsp90,inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival.- Boucherat O, .et al. , Am J Respir Crit Care Med, 2018, Jul 1;198(1):90-103 PMID: 29394093
- Olivier Boucherat, .et al. , Sci Rep, 2017, 7: 4546 PMID: 28674407
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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Hsp90 inhibitor
Ganetespib is a potent, synthetic, small molecule inhibitor of Hsp90, a chaperone protein that is essential to the function of certain other proteins that drive the growth, proliferation, and survival of many different types of cancer.- Dilay Karademir, .et al. , Med Oncol, 2023, Jul 11;40(8):234 PMID: 37432531
- Tung-Yun Wu, .et al. , J Adv Res, 2022, Jun 22;S2090-1232(22)00148-5 PMID: 35752438
- Aykut Ozgur, .et al. , J Chemother, 2021, Apr 2;1-10 PMID: 33794753
- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Kosinsky RL, .et al. , Cell Death Dis, 2019, Dec 4;10(12):911 PMID: 31801945
- Yamada-Kanazawa S, .et al. , Br J Dermatol, 2017, Aug;177(2):456-469 PMID: 28078663
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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Hsp90/SRC/COX-2 Inhibitor
Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2- Guangsen Li, .et al. , Pharm Biol, 2023, 61(1): 271-280 PMID: 36655371
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HSP27 inhibitor
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof.- Haruka Wakasa, .et al. , J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
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Hsp90 inhibitor
PF-04929113 (SNX-5422) is orally bioavailable heat shock protein 90 (Hsp90) inhibitor.- Henry Aceros, .et al. , Life Sci, 2019, 2019 PMID: 30986447
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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HSP90 Inhibitor
NVP-BEP800 is a novel, fully synthetic, orally bioavailable inhibitor that binds to the NH2-terminal ATP-binding pocket of Hsp90.- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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HSP90 Inhibitor
AUY922 (NVP-AUY922) is highly potent and oral inhibitor of Hsp90 with IC50=21 nM in Hsp90 FP binding assay and inhibits proliferation of various human cancer cell lines in vitro, with GI50 average 9 nM.- Linglong Yin, .et al. , Oncogene, 2025, Jun;44(21):1567-1577 PMID: 40044984
- Celia Rouges, .et al. , Microorganisms, 2023, Nov 22;11(12):2837 PMID: 38137982
- Haruka Wakasa, .et al. , J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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HSP 70 inhibitor
VER 155008 is a small molecule, ATP-derivative inhibitor of HSP70 (IC50 = 500 nM).- Linglong Yin, .et al. , Oncogene, 2025, Jun;44(21):1567-1577 PMID: 40044984
- Hiroshi Katoh, .et al. , J Virol, 2017, Mar 15; 91(6): e02220-16 PMID: 28053100
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Hsp90 inhibitor
17-DMAG is a water-soluble analog of 17-AAG and geldanamycin that binds the ATP binding site of Hsp90 and inhibits its chaperone activity. Displays more potent antitumor activity than 17-AAG.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Yool Lee, .et al. , Sci Adv, 2021, 7 PMID: 33579708
- Naoki Shiraishi, .et al. , Oncol Rep, 2020, 448-458 PMID: 33416122
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HSP90 Inhibitor
HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
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Hsp90 inhibitor
SNX-2112 is a heat shock protein 90 (Hsp90) inhibitor with anticancer properties currently in clinical trials. SNX-2112 induced autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and autophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent
- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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Hsp90 Inhibitor
PU-H71 is a potent Hsp90 inhibitor (IC50 = 50 nM).- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Kale S, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2019, Sep 14 PMID: 31522240
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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Hsp70 inhibitor
JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.- Mizuho Nosaka, .et al. , Sci Rep, 2023, Dec 16;13(1):22416 PMID: 38104135
- Siu Hong Dexter Wong, .et al. , Sci Adv, 2023, Jul 7;9(27):eadg9593 PMID: 37418519
- Shivani Patel, .et al. , iScience, 2022, Apr 22;25(5):104282 PMID: 35573186
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Hsp90 inhibitor
MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.- Nazan Goksen Tosun, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2023, Nov 2 PMID: 37917369
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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HSP90 inhibitor
BIIB021 is an oral fully synthetic Hsp90 inhibitor that selectively and potently inhibits the molecular chaperone Hsp90 thereby inhibiting the proper assembly of multiple oncogenic proteins involved in tumor growth and survival.- Nazan Gökşen Tosun, .et al. , Breast Cancer Res Treat, 2025, Apr;210(2):493-506 PMID: 39779635
- Aydemir Asdemir, .et al. , Naunyn Schmiedebergs Arch Pharmacol ., 2024, Jan 19 PMID: 38240781
- Celia Rouges, .et al. , Microorganisms, 2023, Nov 22;11(12):2837 PMID: 38137982
- C M Güven, .et al. , Eur Rev Med Pharmacol Sci, 2023, Aug;27(15):7299-7308 PMID: 37606138
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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Hsp90 inhibitor
Geldanamycin binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity.- Sunayn Cheku, .et al. , Fly (Austin), 2025, Apr 25;19(1):2497565 PMID: 40277072
- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
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HSP90 inhibitor
17-AAG is an ansamycin antibiotic which acts as an anti-tumor agent. Specifically, 17-AAG binds and inhibits Hsp90.- Yool Lee, .et al. , Sci Adv, 2021, 7 PMID: 33579708
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HSP90 inhibitor
Debio 0932 is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents.- Özlem Kaplan, .et al. , Med Oncol, 2024, Jul 3;41(8):194 PMID: 38958814
- Aykut Ozgur, .et al. , Mol Biol Rep, 2021, Apr;48(4):3439-3449 PMID: 33999319
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HSP90 Inhibitor
XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.- Özlem Kaplan, .et al. , Med Oncol, 2024, Jul 3;41(8):194 PMID: 38958814
- Ozlem Kaplan, .et al. , Med Oncol, 2023, Oct 4;40(11):318 PMID: 37794195
- Elesclomol induces oxidative stress by provoking a buildup of reactive oxygen species within cancer cells.
- Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs.
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PROTAC HSP90 Degrader
PROTAC HSP90 Degrader BP3 is a selective agent designed for targeted degradation of Heat Shock Protein 90 (HSP90) through a CRBN-dependent mechanism. This compound effectively degrades HSP90 in MCF-7 breast cancer cells, with a DC50 value of 0.99 µM, and demonstrates significant inhibition of cell growth. Additionally, BP3 features an alkyne group that enables it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile tool for advanced chemical biology applications. -
HSP90 Inhibitor
Kongensin A is a covalent inhibitor of the heat shock protein 90 (HSP90), isolated from the plant Croton kongensis. This natural product effectively inhibits RIP3-dependent necroptosis while also inducing apoptosis. Kongensin A demonstrates significant potential in research applications focused on necroptosis and inflammation, making it a valuable tool for investigating cellular death pathways and therapeutic strategies. -
Hsp90 Inhibitor
GUT-70 is a tricyclic coumarin that functions as a potent Hsp90 inhibitor. It activates caspases 2, 3, 8, and 9, leading to apoptosis in leukemic cells. Additionally, GUT-70 effectively inhibits HIV-1 replication in chronically infected cells by targeting the NF-κB signaling pathway. This compound is suitable for research applications involving leukemia, mantle cell lymphoma (MCL), and HIV-1 infection studies. -
HSP90/mTOR Inhibitor
HSP90/mTOR-IN-1 is a potent inhibitor targeting both Hsp90 and mTOR, exhibiting IC50 values of 69 nM and 29 nM, respectively. This compound effectively suppresses the proliferation of SW780 cells by over-activating the PI3K/AKT/mTOR signaling pathway. In addition to inducing apoptosis and autophagy through selective inhibition, HSP90/mTOR-IN-1 demonstrates significant in vivo anti-tumor activity. It serves as a valuable reagent for research applications focused on bladder cancer. -
Hsp-Cdc Inhibitor
Hsp90-Cdc37-IN-2 is a selective inhibitor of the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). This compound exhibits potent anti-proliferative activity against cancer cell lines A549, MCF-7, HOS, and HepG2, with IC50 values ranging from 0.41 to 0.94 μM. Hsp90-Cdc37-IN-2 effectively disrupts mitochondrial membrane potential, induces apoptosis, and causes cell cycle arrest at the G0/G1 phase in A549 cells, making it a valuable tool for cancer research and therapeutic investigations. -
DNA gyrase inhibitor/Hsp90 antagonist
Novobiocin (Albamycin) is a potent and orally active antibiotic that functions as a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. It holds potential for research into highly β-lactam-resistant pneumococcal infections and has demonstrated antiviral activity against orthopoxviruses. -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
HSP90 Inhibitor
SST0116CL1 free base is a potent inhibitor of the heat shock protein 90 (HSP90) with an IC50 of 0.21 μM. It selectively binds to the ATP binding pocket of HSP90, disrupting its chaperone activity and leading to the degradation of client proteins such as EGFR, CDK4, and AKT. SST0116CL1 free base has demonstrated significant antiproliferative effects, including the degradation of Her2 in BT-474 cells (IC50: 0.2 μM), and is applicable in the study of leukemia, gastric cancer, and ovarian carcinoma. -
HSP90 Inhibitor
SST0116CL1 is a potent HSP90 inhibitor with an IC50 of 0.21 μM. This compound binds to the ATP binding pocket of HSP90, disrupting its chaperone function and promoting the degradation of client proteins such as EGFR, CDK4, and AKT. SST0116CL1 demonstrates antiproliferative activity and is effective in reducing Her2 levels in BT-474 cells (IC50: 0.2 μM). It is suitable for research applications involving leukemia, gastric carcinoma, and ovarian carcinoma. -
HSP90 Inhibitor
DDO-6600 is a covalent inhibitor of Hsp90, targeting its interaction with the co-chaperone protein Cdc37. This mechanism leads to the degradation of client kinases, including AKT, CDK4, and c-Raf, and exhibits potent inhibitory activity against various cancer cell lines. Notably, DDO-6600 reduces migration and invasion of HCT-116 cells while inducing cell cycle arrest and apoptosis. In vivo studies demonstrate its significant efficacy in inhibiting tumor growth in the HCT-116 xenograft model, making it a valuable tool for research in colorectal cancer. -
HSP90 Inhibitor
HVH-2930 is a potent inhibitor of heat shock protein 90 (HSP90), demonstrated to significantly impair the viability of BT474 and JIMT-1 breast cancer cell lines, with IC50 values of 6.86 μM and 4.42 μM, respectively. This compound mediates its effects by downregulating critical HSP90 client proteins, including HER2, p-HER2, AKT, p-AKT, cyclin D1, and survivin. In preclinical studies, HVH-2930 has shown notable antitumor efficacy in mouse models and possesses favorable pharmacokinetic properties in vivo, positioning it as a valuable tool for cancer research focused on HSP90 inhibition. -
HSP90AB1/EEF1A1 Inhibitor
Gamendazole is a selective inhibitor targeting HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A). It effectively binds to the C-terminal nucleotide binding pocket of HSP90, leading to the downregulation of key clients such as AKT1 and ERBB2 while stabilizing the HSP90 heterocomplex. Additionally, Gamendazole specifically inhibits the actin bundling activity of EEF1A1 without affecting its ribosomal functions, making it a valuable tool for studying protein interactions and mechanisms. Furthermore, Gamendazole exhibits antispermatogenic properties, suggesting potential applications in developing reversible non-hormonal male contraceptives. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-1 is a potent dual inhibitor targeting both histone deacetylases (HDAC) with an IC50 of 194 nM and heat shock protein 90 (HSP90), specifically HSP90α with an IC50 of 153 nM. This compound induces the expression of HSP70, downregulates HSP90 client proteins, and facilitates the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-1 effectively reduces PD-L1 expression in interferon-gamma treated H1975 cells, making it a valuable tool for cancer research, particularly in lung and colon malignancies. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-2 is a dual inhibitor of histone deacetylases (HDAC) and heat shock protein 90 (HSP90), exhibiting an IC50 of 360 nM for HDAC and 77 nM for HSP90α. This compound effectively induces HSP70 expression, downregulates client proteins associated with HSP90, and enhances the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-2 reduces PD-L1 expression in H1975 cells treated with IFN-γ. Its applications are particularly relevant in cancer research, including studies focused on lung and colon cancer. -
HDAC/Hsp90 Inhibitor
HDAC/HSP90-IN-3 is a potent dual inhibitor targeting fungal Hsp90 and histone deacetylases (HDAC) with IC50 values of 0.83 μM and 0.91 μM, respectively. This compound demonstrates significant antifungal activity against azole-resistant Candida albicans. Additionally, HDAC/HSP90-IN-3 effectively suppresses key virulence factors and down-regulates drug-resistant genes such as ERG11 and CDR1, making it valuable for research in antifungal resistance and pathogenicity. -
HDAC6/HSP90 Inhibitor
HDAC6/HSP90-IN-1 is a potent dual inhibitor targeting both HDAC6 and HSP90, demonstrating IC50 values of 4.3 nM and 46.8 nM, respectively. This compound effectively down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells, contributing to its potential in cancer therapy. Additionally, HDAC6/HSP90-IN-1 has shown promising efficacy in inhibiting tumor growth in human H1975 xenograft mice models, making it a valuable tool for cancer research. -
Hsp90 Inhibitor
PU24FCl is a selective inhibitor of the heat shock protein 90 (Hsp90). This compound demonstrates significant anti-cancer activity, promoting tumor regression by disrupting chaperone activity critical for the stability and function of multiple oncogenic clients. Notably, PU24FCl selectively accumulates in tumor tissues while being rapidly eliminated from normal tissues, enhancing its therapeutic potential in cancer research applications. -
Hsp90 Inhibitor
Conglobatin is a macrolide dilactone that functions as an Hsp90 inhibitor. It selectively binds to the N-terminal domain of Hsp90, effectively disrupting the Hsp90-Cdc37 complex formation. This compound demonstrates significant apoptotic activity in human breast cancer cells and esophageal squamous cell carcinoma cells, and it exhibits notable antitumor efficacy in vivo, making it a potential candidate for cancer research applications. -
HSP90/EGFR Inhibitor
Wighteone, a prenylated isoflavone, acts as an HSP90 and EGFR inhibitor, specifically targeting the EGFR L858R/T790M mutations. This compound effectively reduces HSP90 expression, inhibits EGF-induced phosphorylation of EGFR, and disrupts downstream signaling through ERK and AKT pathways. Wighteone demonstrates significant biological activity by inducing cell cycle redistribution, inhibiting proliferation, and triggering apoptosis in various cancer cell lines. It is relevant for research on HER2-positive breast cancer, leukemia, non-small cell lung cancer with specific mutations, and also displays antifungal properties. -
HSP90/LSD1 Inhibitor
HSP90/LSD1-IN-1 is a dual inhibitor targeting HSP90 and LSD1, effectively disrupting their interaction and function. This compound demonstrates significant antiproliferative activity in prostate cancer cell lines, exhibiting GI50 values of 0.24 μM for PC-3 and 0.30 μM for DU145. It is a valuable tool for research into therapeutic strategies against prostate cancer and the role of chaperone proteins and histone demethylases in tumor biology. -
EZH2/HSP90 Inhibitor
EZH2/HSP90-IN-29 is a dual inhibitor targeting both EZH2 and HSP90, exhibiting IC50 values of 6.29 nM for EZH2 and 60.1 nM for HSP90. This compound enhances the expression of apoptosis and necrosis-related genes, induces M-phase cell cycle arrest, and disrupts the reactive oxygen species catabolism pathway. Additionally, EZH2/HSP90-IN-29 has the capability to cross the blood-brain barrier, making it a valuable tool for research in cancer biology and neurodegenerative diseases. -
Hsp90 Inhibitor
NSC145366 monohydrochloride is an inhibitor of the Hsp90 chaperone protein, specifically targeting its C-terminal domain. By directly interacting with Hsp90, it effectively disrupts its chaperone activity, leading to a significant reduction in cellular growth. This compound has been shown to strongly inhibit the proliferation of Saccharomyces cerevisiae strains, specifically cog7Δ and cog8Δ, making it a valuable tool for research into protein homeostasis and cellular stress response pathways. -
HSP90 Inhibitor
HSP90-IN-9 is a highly potent and selective inhibitor of the heat shock protein 90 (HSP90). This compound exhibits pronounced fungicidal activity in a dose-dependent manner and effectively inhibits fungal biofilm formation and morphological alterations when used in conjunction with fluconazole (FLC). Additionally, HSP90-IN-9 enhances FLC sensitivity by down-regulating the expression of key resistance-related genes, including ERG11, CDR1, and CDR2, making it a valuable tool for research applications in antifungal resistance studies. -
Hsp90 Inhibitor
Hsp90-IN-41 is a potent inhibitor of Heat Shock Protein 90 (Hsp90) with an IC50 of 0.044 μM. This compound demonstrates significant antifungal and antitumor activity, exhibiting an IC50 of 0.049 μM in vitro. It is valuable for research applications related to cancer and fungal diseases, particularly in studying the therapeutic potential of Hsp90 modulation. -
Aha1/Hsp90 Complex Inhibitor
Aha1/Hsp90-IN-1 is a potent inhibitor of the Aha1/Hsp90 complex, demonstrating an IC50 value of 3.32 μM. By disrupting the interactions between Aha1 and Hsp90, this compound effectively inhibits tau aggregation. Research applications include studies of protein folding and aggregation diseases, making it a valuable tool in the exploration of neurodegenerative disorders. -
HSF1 activation inhibitor
Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.

