HSP90 Inhibitor

Hsp90-IN-44 (compound 16) is a Hsp90 inhibitor with an IC₅₀ of 9.8 µM. Hsp90-IN-44 can be used for cancer research.

17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.

HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC₅₀ values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice.

HDAC6/HSP90-IN-3 (Compound 17) is an orally active dual histone deacetylase 6 (HDAC6) and heat shock protein 90 (HSP90) inhibitor with IC₅₀ values of 28 nM and 0.88 μM, respectively. HDAC6/HSP90-IN-3 is promising for research of malignant tumors such as prostate cancer.

Hsp90β-IN-2 (Compound 16B) is a selective Hsp90β inhibitor with K_Ds of 225 nM and 73.32 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer.

Grp94 Inhibitor-2 (compound 23), a cyclopropane analog, exhibits high affinity for glucose-regulated protein 94 (Grp94) with a K_d of 0.48 µM and 0.65 µM for Grp94 and Hsp90α, respectively.

17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research.

HSP90-IN-14 (compound 4) is a potent Hsp90 (heat shock protein 90) inhibitor, with a K_d of 0.26 μM. HSP90-IN-14 shows anti-influenza virus activity in MDCK cells, with EC₅₀ values of 2.6, 3.9, and 17 μM for influenza A/H3N2, A/H1N1, and B, respectively.

DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC₅₀: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model.

HSF1-IN-3 is a heat shock transcription factor 1 (HSF1) inhibitor with a K_d value of 23.8 μM against HSF1-DBD. HSF1-IN-3 inhibits the proliferation of cancer cells and induces their apoptosis, with stronger activity in androgen-dependent prostate cancer cells. HSF1-IN-3 reduces the expression of HSP70 and HSP90, downstream effectors of HSF1, and attenuates HSE-driven transcriptional activity. HSF1-IN-3 can be used in the research of cancers such as prostate cancer and leukemia.

PU24FCl is a specific inhibitor of Hsp90. PU24FCl exhibits wide-ranging anti-cancer activities. PU24FCl accumulates in tumors while being rapidly cleared from normal tissue.

GUT-70, a tricyclic coumarin, is a Hsp90 inhibitor. GUT-70 activates the caspase 2, 3, 8 and 9, and induces the apoptosis in leukemic cells. GUT-70 inhibits HIV-1 replication in chronically infected cells via suppression of the NF-κB pathway. GUT-70 can be used for the study of leukemic, mantle cell lymphoma (MCL) and HIV-1 infection.

CC-11 is an orally active small molecule drug conjugate (SMDC) that links the PI3K/mTOR inhibitor with the extracellular heat shock protein 90 (EHSP90) targeting ligand through a cleavable linker. CC-11 exhibits strong HSP90 binding activity (IC₅₀ = 15 nM) and inhibits PI3Kα kinase activity (IC₅₀ = 0.54 nM). CC-11 has anti-proliferative activity against colon cancer cells. CC-11 shows significant efficacy in the HCT-116 xenograft tumor model. CC-11 can be used for research on colon cancer.

Hsp90-IN-45 is a Hsp90 inhibitor. Hsp90-IN-45 competitively binds to the ATP-binding site of purified Hsp90α with a K_d of 70 nM, blocks ATP hydrolysis, and disrupts Hsp90 client signaling. Hsp90-IN-45 inhibits ATPase activity of purified Hsp90α. Hsp90-IN-45 will be radiolabeled with ⁷⁶/⁷⁷Br for use as a radiotheragnostic agent for PET imaging and Meitner-Auger electron therapy. Hsp90-IN-45 can be used for the research of cancer.

MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma.

PU-11 is a Hsp90α/Hsp90β inhibitor with IC₅₀ values of 18.6 μM and 89.8 μM and K_d values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders.

HSP90-IN-28 (compound 12 h) is a potent and selective Hsp90 inhibitor with an IC₅₀ of 0.46 μM for Hsp90α. HSP90-IN-28 exhibits ~48 fold selectivity versus other Hsp90β (IC₅₀ = 22.28 μM).

Hsp90-IN-42 is a heat shock protein 90 (Hsp90) inhibitor with an IC₅₀ of 15.65 nM against human targets. Hsp90-IN-42 destabilizes EGFR and inhibits the activation of the EGFR-Akt signaling pathway. Hsp90-IN-42 suppresses the proliferation and migration of cancer cells, induces cell cycle arrest by downregulating CDK12 and CDK13, and triggers mild apoptosis via downregulating Bcl-2 and upregulating Bax. Hsp90-IN-42 inhibits tumor growth in xenograft mouse models. Hsp90-IN-42 can be used in research related to colorectal cancer.

SST0116CL1 free base is a HSP90 inhibitor (IC₅₀: 0.21 μM). SST0116CL1 free base binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 free base induces degradation of Her2 in BT-474 cell (IC₅₀: 0.2 μM). SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base can be used for the study of leukemia, gastric and ovarian carcinoma.

HSP90-IN-29 (Compound 13), a benzoxazole derivative, is a potent and selective HSP-90 inhibitor with an IC₅₀ value of 30 nM. HSP90-IN-29 has antitumor activity.