Arimoclomol citrate (BRX-220 citrate) is a co-inducer of heat shock proteins (HSP)[1]. Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system[2].
KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research[1][2].
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity[1][2].
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy[1].
17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research[1].
Malonganenone A is a selective plasmodial Hsp70s modulator. It also has antimalarial activity.
KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
Hs-27 is a Novel Hsp90 Inhibitor, Exhibits Diagnostic and Therapeutic Potential in Triple Negative Breast Cancer.
Palmitic acid-13C16 sodium is the 13C-labeled Palmitic acid sodium. Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
Aminohexylgeldanamycin (AHGDM) hydrochloride, a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin hydrochloride shows antiangiogenic and antitumor activities[1].
YM-1 is a stable and soluble MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins[1][2].
HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity[1].
BIIB021 is an orally available, fully synthetic inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively.
17-AAG is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90.
HSP90-IN-14 (compound 4) is a potent Hsp90 (heat shock protein 90) inhibitor, with a Kd of 0.26 μM. HSP90-IN-14 shows anti-influenza virus activity in MDCK cells, with EC50 values of 2.6, 3.9, and 17 μM for influenza A/H3N2, A/H1N1, and B, respectively[1].
Ganetespib is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines.
SNX-2112 is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively.
SEW84 (SEW04784) is a first-in-class, specific inhibitor of the Aha1-stimulated Hsp90 (ASH) ATPase activity (IC50=0.3 uM) without inhibiting basal Hsp90 ATPase;SEW84 binds to the C-terminal domain of Aha1 (Kd=1.7 uM) to weaken its asymmetric binding to Hsp90.SEW84 inhibited the GR- and AR-dependent luciferase expression with IC50 of 1.3 uM and 0.7 uM respectively.SEW84 blocks Aha1-dependent Hsp90 chaperoning activities, including the in vitro and in vivo refolding of firefly luciferase, and the transcriptional activity of the androgen receptor in cell-based models of prostate cancer.SEW84 promotes the clearance of phosphorylated tau in cellular and tissue models of neurodegenerative tauopathy.
Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications[1].
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity[1].
JG-231 is an allosteric inhibitor that disrupts the Hsp70-BAG3 interaction (Ki=0.11 uM), inhibits breast cancer cells MCF-7 and MDA-MB-231 with IC50 of 0.12 and 0.25 uM, respectively; reduces tumor burden in an MDA-MB-231 xenograft model (4 mg/kg, ip).
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1[1].
KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.
HSP90-IN-20 (compound 78p) is a potent HSP90 inhibitor with an IC50 of ≤10 μM. HSP90-IN-20 has the potential for cancers research[1].
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells[1].
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[1].
YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration[1].
HSP90-IN-27 (compound 19) is an HSP90 inhibitor[1].
AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90[1].
YM-08 (Compounds 7a) is a brain-penetrant inhibitors of SIRT2,with the IC50 of 19.9 μM. YM-08 also is inhibitor of Hsp70[1].