HSP

Tamoxifen (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

Triptolide (PG490) belongs to the tricyclic diterpenoid group of natural products and is an inhibitor of NF-κB activation. Triptolide exhibits immunosuppressive, anti-rheumatic, anti-inflammatory, anti-proliferative and anti-tumor activities.

Palmitic acid (Cetylic acid) is a natural product, a common saturated fatty acid found in animals, plants and microorganisms. Palmitic acid has antitumor activity.

Paeoniflorin (Peoniflorin) is a herbal constituent extracted from the root of Paeonia albiflora Pall.

2',4'-DIHYDROXYCHALCONE (2',4'-DHC) as a compound with Hsp90 inhibitory and antifungal effects

AMP-PCP disodium, an ATP analogue, binds to the N-terminal domain of Hsp90 with a Kd value of 3.8 μM, facilitating the formation of an active Hsp90 homodimer.

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.

Feretoside is a natural product extracted from the barks of E. ulmoides. Feretoside shows inducible activity on the heat shock factor 1 (HSF1).

Eupalinolide B is a natural product ,and demonstrates potent cytotoxicity against A-549, BGC-823, SMMC-7721, and HL-60 tumour cell lines.

Rosolutamide (ALZ-003) is a curcumin analog, an orally active Nrf1 and Nrf2 activator.Rosolutamide modulates oxidative homeostasis, improves mitochondrial function and promotes autophagy, reduces mutant protein aggregation, and decreases intracellular mitochondrial reactive oxygen species (ROS) levels.Rosolutamide has been used in the study of neurodegeneration such as spinal cerebellar ataxia and Huntington disease. neurodegenerative diseases such as Huntington's disease. Regulates oxidative homeostasis.

Tanespimycin (KOS 953) (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM).

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.

Arimoclomol (BRX-220 free base), a co-inducer of heat shock proteins (HSP), is utilized in studies on the treatment of amyotrophic lateral sclerosis (ALS).

Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90), exhibiting potential antineoplastic activity.

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.

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

Gedunin is an important limonoid present in several genera of the Meliaceae family, mainly in seeds. Gedunin is an Hsp90 inhibitor, and inhibits ovarian cancer cell proliferation.

Onalespib (AT13387) is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.

CC-99677 (Gamcemetinib) is a selectively targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune diseases that translates biochemical potency into cellular potency as demonstrated by potent inhibition of heat shock protein 27 (HSP1) phosphorylation in LPS-activated monocyte THP-27 cells via a nucleophilic aromatic substitution (SNAr) mechanism.CC-99677 in Rat experiments demonstrated potency in both biochemical (IC 50 =156.3 nM) and cellular assays (EC 50 =89 nM).

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.

HA15 targets specifically BiP GRP78 HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

CCT018159 is a 3,4-diarylpyrazole resorcinol, an ATP-competitive HSP90ATPase inhibitor that inhibits human Hsp90β and yeast Hsp90 with IC50s of 3.2 and 6.6 μM, respectively.CCT018159 inhibits key endothelial and tumor cell functions associated with invasion and angiogenesis. CCT018159 caused cellular inhibition associated with G1 phase block and induced apoptosis.

Pimitespib (TAS-116) is an ATP-competitive and highly specific HSP90α HSP90β inhibitor with inhibition constants (Kis) of 34.7 nM and 21.3 nM, respectively.

Teprenone (Geranylgeranylacetone) is a anti-ulcer drug, and works as an inducer of heat shock proteins (HSPs).

Pifithrin-μ (NSC-303580) is an inhibitor of p53 and HSP70, with neuroprotective and antitumor activity.

MKT-077 (FJ-776) is a cationic rhodacyanine dye that demonstrates antiproliferative activity against cancer cell lines (EC50s: 1.4-2.2 μM in vitro) through its ability to inhibit members of the Hsp70 family of molecular chaperones.

Novobiocin is an orally active and potent antibiotic.Novobiocin is a DNA gyrase inhibitor and heat shock protein 90 (Hsp90) antagonist with inhibitory effects on gyrase and Hsp90. Novobiocin has anti-positive activity and can be used to study highly resistant pneumococcal infections.

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.

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.

3-Phenyltoxoflavin (Phenyltoxoflavin) is an inhibitor of HSP90 (Kd = 585 nM) with anti-cancer activity.

Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR) HSP association.

XL888 is an ATP-competitive inhibitor of Hsp90 ( IC50: 24 nM). Heat shock protein 90 (Hsp90) is a chaperone that maintains the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis. Through this action, specific clie

HSP27 inhibitor J2 (J2) (J2) is a HSP27 inhibitor, 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.

NPX800 is an inhibitor of heat shock factor 1 (HSF1) and can be used in studies about the treatment of cancer.

Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.

DTHIB robustly inhibits the HSF1 cancer gene signature and prostate cancer cell proliferation.

JG-98 is an allosteric Hsp70 inhibitor, displays high active against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50s: 0.4 0.7 μM).

VER-49009 (CCT 129397) is a potent Hsp90 inhibitor(IC50 of 25 nM and Kd of 78 nM).

Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM.

NVP-HSP990 (HSP990) is an effective and specific HSP90α β inhibitor (IC50: 0.6 0.8 nM).

VER49009 (CCT0129397) is an effective HSP90 inhibitor(IC50 =25 nM, Kd=78 nM).

HSP70-IN-1 is a heat shock protein (HSP) inhibitor that suppresses the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

PU-H71 HCl (Zelavespib HCl) is a novel Hsp90 inhibitor, a novel purine-based analog, and a radiosensitizer that may be a promising agent for CIRT. PU-H71 HCL shows antitumor activity in many preclinical models of malignancy. PU-H71 HCL has an inhibitory effect on the protein expression levels of Rad51 and Ku70, which may be associated with the double chain break repair in the homologous recombination pathway and non-homologous end-joining pathway.

Alvespimycin hydrochloride (BMS 826476) is a potent HSP90 inhibitor with IC50 of 62 nM. Phase 2.

Col003 is a selective and potent inhibitor of Hsp47, competitively binding to the collagen-binding site on Hsp47 (IC50: 1.8 μM). It is useful for researching fibrosis.

Shepherdin 79-87 acetate is a peptidomimetic antagonist of the complex between Hsp90 and survivin, another key regulator of tumor cell viability.

H2-Gamendazole is a novel compound for spermatogenesis inhibition and cancer therapy as an inhibitor of heat shock proteins and or elongation factor 1 alpha, and is an Hsp90 regulator.