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HSP inhibitors

Conformational maturation of targets in signal transductions is related to Heat shock protein 90 (Hsp90). Hsp90 keeps these unstable signalling proteins, including HER-2/ErbB2, Akt, Raf-1, Bcr-Abl and mutated p53, poised for activation until they are stabilized by conformational changes associated with signal transduction. HSP90 is also related to cell cycle because HSP90 can regulator the cell cycle regulator proteins such as CDK1.Inhibition of HSP90 can block cancer related pathways such as EGF-R and Her-2, Flt3, PI3K/PDK1/AKT, Ras, MEK, ERK, the Wnt/β-catenin pathway, and JAK-STAT pathway.

Other Cytoskeletal Signaling Related Inhibitors

Kinesin Microtubule Associated Integrin PAK Dynamin MLCK TACC3 Gap-Junction Actin Cardiac Myosin
Cat.No. Product Name Information Product Use Citations Product Validations
S2492 Novobiocin Sodium (Cathomycin, Albamycin) Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.
Redox Biol, 2025, 85:103672
J Transl Med, 2025, 23(1):1079
Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433
Verified customer review of Novobiocin Sodium (Cathomycin, Albamycin)
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Autophagy, 2025, 1-23.
Cell Commun Signal, 2025, 23(1):331
Verified customer review of Tanespimycin (17-AAG)
S3604 Triptolide Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.
Mol Cell, 2025, S1097-2765(25)00316-8
Mol Cell, 2025, 85(15):2839-2853.e8
Chin Med, 2025, 20(1):122
Verified customer review of Triptolide
S1238 Tamoxifen Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Cell Discov, 2025, 11(1):89
Nat Genet, 2025, 57(9):2192-2202
Cell Metab, 2025, 37(8):1715-1731.e11
Verified customer review of Tamoxifen
S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand and inhibits FDX1-mediated Fe-S cluster biosynthesis.Elesclomol (STA-4783) is a potent copper ionophore and can be used in the research of copper-dependent cell death (cuproptosis).
Nat Commun, 2025, 16(1):212
Cell Prolif, 2025, e70101.
J Transl Med, 2025, 23(1):127
Verified customer review of Elesclomol (STA-4783)
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, exhibits weaker potency against the HSP90 family members GRP94 and TRAP-1, and demonstrates the tightest binding of any small-molecule HSP90 ligand. It effectively downregulates and destabilizes the IGF-1Rβ protein, resulting in growth inhibition, autophagy and apoptosis. Phase 2.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Autophagy, 2025, 1-23.
Cancers (Basel), 2025, 17(8)1341
Verified customer review of Luminespib (NVP-AUY922)
S1159 Ganetespib (STA-9090) Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
Nat Neurosci, 2025, 28(6):1174-1184
Redox Biol, 2025, 85:103672
J Nucl Med, 2025, jnumed.124.268961
Verified customer review of Ganetespib (STA-9090)
S1142 Alvespimycin (17-DMAG) Hydrochloride Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay.
Theranostics, 2025, 15(8):3589-3609
Biomolecules, 2025, 15(1)76
bioRxiv, 2025, 2025.07.17.665404
Verified customer review of Alvespimycin (17-DMAG) Hydrochloride
S7751 VER155008 VER155008 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 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. This compound inhibits autophagy and causes reduced levels of HSP90 client proteins.
Nat Cell Biol, 2025, 27(9):1448-1464
Biomolecules, 2025, 15(1)76
J Microbiol Biotechnol, 2025, 35:e2508015
Verified customer review of VER155008
S1163 Onalespib (AT13387) Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.
J Nucl Med, 2025, jnumed.124.268961
Front Oncol, 2025, 15:1451156
J Labelled Comp Radiopharm, 2025, 68(4):e4144
Verified customer review of Onalespib (AT13387)

Signaling Pathway Map