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.

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

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.

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.

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.

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.

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).

HSF1A is a cell-permeable activator of HSF1 that protects mammalian cells against stress-induced apoptosis (HSF1).

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.

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

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

Arimoclomol maleate (BRX-220) (BRX-220) is a heat shock protein (HSP) co-inducer.

Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces Hsp90 expression and its interaction with hERG.

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

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

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).

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.

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

KRIBB11 is an inhibitor of Heat Shock Factor (HSF) [inhibitor].

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.

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

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

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.

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.

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

IPI-493 (17-amino17demethoxy) is a novel HSP90 inhibitor with antitumor activity.

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

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

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.

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

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.

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.

TRC051384 is a heat shock protein 70 (HSP70) inducer that reduces stroke-associated neuronal damage and increases survival in a rat model of transient ischemic stroke, activates heat shock factor-1 and leads to elevated molecular chaperone and anti-inflammatory activity, and enhances Hsp72 expression in neurons and glial cells.

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

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

Apoptozole (Apoptosis Activator VII) inhibits the ATPase domain of Hsc70 and Hsp70, inducing apoptosis.

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.

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.

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

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

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.

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.

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

KW-2478 is a non-ansamycin HSP90 inhibitor with IC50 of 3.8 nM.