hsp90β

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.

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.

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

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

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

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

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.

Tamoxifen is an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM).

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

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.

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

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.

BIIB021 (CNF2024) is an orally-available, fully synthetic inhibitor of HSP90(Ki=1.7 nM, EC50=38 nM).

PF04929113 (SNX-5422) is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, PF04929113 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers.

VER-50589 is a potent HSP90 inhibitor.

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.

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.

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

Anticanceragent 249 (Compound 89) is an inhibitor of Hsp90β, exhibiting an IC50 of 16.5 μM in PC3MM2 cells. It suppresses the proliferation of various cancer cell lines including MCF-7, T47D, MDA-MB-231, MDA-MB-468, and SKBr3, with IC50 values ranging from 1.8 to 5.3 μM. Additionally, Anticanceragent 249 induces apoptosis in MDA-MB-231 cells and demonstrates antitumor activity in mice.

HSP90-IN-33 (compound 24e) is an effective Hsp90 inhibitor, demonstrating dissociation constants (Kd) of ≥200 µM for Hsp90α and 7.3 µM for Hsp90β. This compound induces cellular apoptosis (apoptosis) and arrests the cell cycle at the G0 G1 phase. Additionally, HSP90-IN-33 reduces the protein expression of ERα, CDK4, and Akt.

KUNB31 is a potent and selective inhibitor of Hsp90β.