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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
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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
- Naoki Shiraishi, .et al. , Oncol Rep, 2020, 448-458 PMID: 33416122
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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.- 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
- Elesclomol induces oxidative stress by provoking a buildup of reactive oxygen species within cancer cells.
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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.- 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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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
Geldanamycin binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity.- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
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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
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
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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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
IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90). -
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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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.- Aykut Ozgur, .et al. , Mol Biol Rep, 2021, Apr;48(4):3439-3449 PMID: 33999319
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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. -
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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GA mitochondrial matrix inhibitor
Gamitrinib TPP is a GA mitochondrial matrix inhibitor. Gamitrinib TPP is offered as the hexafluorophosphate salt.
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HSP 70 inhibitor
VER 155008 is a small molecule, ATP-derivative inhibitor of HSP70 (IC50 = 500 nM).- Hiroshi Katoh, .et al. , J Virol, 2017, Mar 15; 91(6): e02220-16 PMID: 28053100
- Geranylgeranylacetone can induce expression of HSP70, HSPB8, and HSPB1.
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Hsp90 inhibitor
Alvespimycin is a selective Hsp90 inhibitor with a GI50 of 53 nM. -
Hsp90 inhibitor
Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9. -
HSP90 inhibitor
Macbecin I is an ansamycin antibiotic compound that inhibits Hsp90 activity with IC50 value of μM by binding to the ATP-binding site. -
HSP70 inducer
TRC 051384, belonging to substituted 2-propen-1-one class, is a potent inducer of heat shock protein 70 (HSP70) [1]. Induction of HSP70 is a natural response of stressed cells that protects neuronal cells from a variety of insults including acute ischemia. -
Antioxidant
Ethoxyquin is an antioxidant that is widely used in animal feed to protect against lipid peroxidation and fat rancidity in chicken, salmon, and beef. -
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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cell motility and cell invasion inhibitor
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life. -
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-Cdc37 interaction disruptors
Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptors that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.