hsp90α

NMS-E973 is a potent and selective Hsp90 inhibitor with a DC50 of less than 10 nM for Hsp90 binding, displaying no activity against a panel of 52 diverse protein kinases.

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

PU-H54 is a purine-based inhibitor of Grp94. It is a Grp94-selective resorcinol-based inhibitor isolated through probing of the exclusive binding region of S2 subpocket in Grp94.

Debio 0932 (CUDC-305) is a heat shock protein 90 (Hsp90) inhibitor that targets the n-terminal atp-binding pocket to promote apoptosis, and has the advantage of being orally available and able to cross the blood-brain barrier (BBB) for the treatment of cancers such as non-small-cell lung cancer (NSCLC) and neuroblastoma.

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.

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.

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

SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.

HSP90/mTOR-IN-1 is an effective and orally administrable inhibitor targeting both Hsp90 and mTOR, displaying IC50 values of 69 nM and 29 nM, respectively. This compound inhibits the proliferation of SW780 cells by overly activating the PI3K/AKT/mTOR pathway and induces apoptosis and autophagy through its selective inhibition of Hsp90 and mTOR. Additionally, HSP90/mTOR-IN-1 exhibits significant anti-tumor activity in vivo and is applicable in bladder cancer research.

PROTAC HSP90 degrader BP3 potently and selectively degrades HSP90 through a CRBN-dependent mechanism. It effectively diminishes HSP90 protein levels in MCF-7 cells with a half-maximal degradation concentration (DC50) of 0.99 µM. Additionally, this compound impedes the proliferation of breast cancer cells [1].

HSP90-IN-22 is a potent HSP90 inhibitor targeting the ATP-binding site. It induces the degradation of oncogenic client proteins, used for broad-spectrum cancer and drug resistance research.

HSP90-IN-27 (compound 19) is an effective HSP90 inhibitor for cancer research.

HSP90α-IN-1 is an HSP90α inhibitor (IC50= 111 nM) that demonstrates anti-aging activity across various cellular senescence models. Belonging to the xanthine family, HSP90α-IN-1 is involved in research focused on combating age-related inflammation, senescence, and diseases (including cancer), and it may contribute to extending healthy lifespan.

Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research. It demonstrates inhibitory effects on the proliferation of breast cancer cell lines, MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with respective IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM [1].

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Wighteone (Erythrinin B) is a small molecule compound derived from Genista ephedroides with potential antifungal and anticancer activity against EGFR L858R/T790M mutant non-small cell lung cancer.

HS-27 is a fluorescently-tethered inhibitor of Hsp90 with SNX-5422 tethered via a PEG linker to a fluorescein isothiocyanate or FITC. HS-27 can be used in see-and-treat paradigms.

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

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.

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

Ethoxyquin (Santoflex) is an antioxidant used in animal feeds.

Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

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.

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