hsp90β

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.

7-Aminocephalosporanic acid is an HSP90β inhibitor used in the synthesis of cephalosporin antibiotics and their intermediates.

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.

VER-82576 (NVP-BEP800), a synthetic HSP90β inhibitor (IC50: 58 nM), exhibits >70-fold selectivity against Hsp90 family members Trap-1 and Grp94.

VER-50589 is a potent HSP90 inhibitor.

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

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.

Hsp90β-IN-1 (Compound 7b) is a selective biotinylated inhibitor of heat shock protein 90β (HSP90β) with an IC50 value of 0.33 μM.

Hsp90β-IN-2 (Compound 16B) is a selective inhibitor of Hsp90β, with dissociation constants (KD) of 225 nM for Hsp90β and 73.32 μM for Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231, A549, and SKOV-3 cells, and is applicable in research on triple-negative breast cancer.

Hsp90β decapeptide, a C-terminal peptide of Hsp90β, contains the conserved TPR domain sequence MEEVD. It binds tightly to the Tah1 protein with a dissociation constant (Kd) of 1.0 μM.

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.