Catalog No.
Product Name
Application
Product Information
Citations
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Hsc70 and Hsp70 inhibitor
Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14?μM, respectively, and can induce apoptosis. -
Hsp90 inhibitor
SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM. -
MAPKAPK2(MK2) inhibitor
MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. -
HSP inhibitor
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM. -
co-inducer of heat shock proteins (HSP)
Arimoclomol maleate (BRX-220) is a co-inducer of heat shock proteins (HSP). - Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs.
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DNA gyrase inhibitor/Hsp90 antagonist
Novobiocin (Albamycin) is a potent and orally active antibiotic that functions as a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. It holds potential for research into highly β-lactam-resistant pneumococcal infections and has demonstrated antiviral activity against orthopoxviruses. -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
PROTAC HSP90 Degrader
PROTAC HSP90 Degrader BP3 is a selective agent designed for targeted degradation of Heat Shock Protein 90 (HSP90) through a CRBN-dependent mechanism. This compound effectively degrades HSP90 in MCF-7 breast cancer cells, with a DC50 value of 0.99 µM, and demonstrates significant inhibition of cell growth. Additionally, BP3 features an alkyne group that enables it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile tool for advanced chemical biology applications. -
HSP90 Inhibitor
Kongensin A is a covalent inhibitor of the heat shock protein 90 (HSP90), isolated from the plant Croton kongensis. This natural product effectively inhibits RIP3-dependent necroptosis while also inducing apoptosis. Kongensin A demonstrates significant potential in research applications focused on necroptosis and inflammation, making it a valuable tool for investigating cellular death pathways and therapeutic strategies. -
Hsp90 Inhibitor
GUT-70 is a tricyclic coumarin that functions as a potent Hsp90 inhibitor. It activates caspases 2, 3, 8, and 9, leading to apoptosis in leukemic cells. Additionally, GUT-70 effectively inhibits HIV-1 replication in chronically infected cells by targeting the NF-κB signaling pathway. This compound is suitable for research applications involving leukemia, mantle cell lymphoma (MCL), and HIV-1 infection studies. -
HSP90 Inhibitor
SST0116CL1 free base is a potent inhibitor of the heat shock protein 90 (HSP90) with an IC50 of 0.21 μM. It selectively binds to the ATP binding pocket of HSP90, disrupting its chaperone activity and leading to the degradation of client proteins such as EGFR, CDK4, and AKT. SST0116CL1 free base has demonstrated significant antiproliferative effects, including the degradation of Her2 in BT-474 cells (IC50: 0.2 μM), and is applicable in the study of leukemia, gastric cancer, and ovarian carcinoma. -
HSP90 Inhibitor
SST0116CL1 is a potent HSP90 inhibitor with an IC50 of 0.21 μM. This compound binds to the ATP binding pocket of HSP90, disrupting its chaperone function and promoting the degradation of client proteins such as EGFR, CDK4, and AKT. SST0116CL1 demonstrates antiproliferative activity and is effective in reducing Her2 levels in BT-474 cells (IC50: 0.2 μM). It is suitable for research applications involving leukemia, gastric carcinoma, and ovarian carcinoma. -
HSP90 Inhibitor
DDO-6600 is a covalent inhibitor of Hsp90, targeting its interaction with the co-chaperone protein Cdc37. This mechanism leads to the degradation of client kinases, including AKT, CDK4, and c-Raf, and exhibits potent inhibitory activity against various cancer cell lines. Notably, DDO-6600 reduces migration and invasion of HCT-116 cells while inducing cell cycle arrest and apoptosis. In vivo studies demonstrate its significant efficacy in inhibiting tumor growth in the HCT-116 xenograft model, making it a valuable tool for research in colorectal cancer. -
HSP90 Inhibitor
HVH-2930 is a potent inhibitor of heat shock protein 90 (HSP90), demonstrated to significantly impair the viability of BT474 and JIMT-1 breast cancer cell lines, with IC50 values of 6.86 μM and 4.42 μM, respectively. This compound mediates its effects by downregulating critical HSP90 client proteins, including HER2, p-HER2, AKT, p-AKT, cyclin D1, and survivin. In preclinical studies, HVH-2930 has shown notable antitumor efficacy in mouse models and possesses favorable pharmacokinetic properties in vivo, positioning it as a valuable tool for cancer research focused on HSP90 inhibition. -
HSP90AB1/EEF1A1 Inhibitor
Gamendazole is a selective inhibitor targeting HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A). It effectively binds to the C-terminal nucleotide binding pocket of HSP90, leading to the downregulation of key clients such as AKT1 and ERBB2 while stabilizing the HSP90 heterocomplex. Additionally, Gamendazole specifically inhibits the actin bundling activity of EEF1A1 without affecting its ribosomal functions, making it a valuable tool for studying protein interactions and mechanisms. Furthermore, Gamendazole exhibits antispermatogenic properties, suggesting potential applications in developing reversible non-hormonal male contraceptives. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-1 is a potent dual inhibitor targeting both histone deacetylases (HDAC) with an IC50 of 194 nM and heat shock protein 90 (HSP90), specifically HSP90α with an IC50 of 153 nM. This compound induces the expression of HSP70, downregulates HSP90 client proteins, and facilitates the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-1 effectively reduces PD-L1 expression in interferon-gamma treated H1975 cells, making it a valuable tool for cancer research, particularly in lung and colon malignancies. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-2 is a dual inhibitor of histone deacetylases (HDAC) and heat shock protein 90 (HSP90), exhibiting an IC50 of 360 nM for HDAC and 77 nM for HSP90α. This compound effectively induces HSP70 expression, downregulates client proteins associated with HSP90, and enhances the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-2 reduces PD-L1 expression in H1975 cells treated with IFN-γ. Its applications are particularly relevant in cancer research, including studies focused on lung and colon cancer. -
HDAC/Hsp90 Inhibitor
HDAC/HSP90-IN-3 is a potent dual inhibitor targeting fungal Hsp90 and histone deacetylases (HDAC) with IC50 values of 0.83 μM and 0.91 μM, respectively. This compound demonstrates significant antifungal activity against azole-resistant Candida albicans. Additionally, HDAC/HSP90-IN-3 effectively suppresses key virulence factors and down-regulates drug-resistant genes such as ERG11 and CDR1, making it valuable for research in antifungal resistance and pathogenicity. -
HDAC6/HSP90 Inhibitor
HDAC6/HSP90-IN-1 is a potent dual inhibitor targeting both HDAC6 and HSP90, demonstrating IC50 values of 4.3 nM and 46.8 nM, respectively. This compound effectively down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells, contributing to its potential in cancer therapy. Additionally, HDAC6/HSP90-IN-1 has shown promising efficacy in inhibiting tumor growth in human H1975 xenograft mice models, making it a valuable tool for cancer research. -
EZH2/HSP90 Inhibitor
EZH2/HSP90-IN-29 is a dual inhibitor targeting both EZH2 and HSP90, exhibiting IC50 values of 6.29 nM for EZH2 and 60.1 nM for HSP90. This compound enhances the expression of apoptosis and necrosis-related genes, induces M-phase cell cycle arrest, and disrupts the reactive oxygen species catabolism pathway. Additionally, EZH2/HSP90-IN-29 has the capability to cross the blood-brain barrier, making it a valuable tool for research in cancer biology and neurodegenerative diseases. -
Hsp90 Inhibitor
NSC145366 monohydrochloride is an inhibitor of the Hsp90 chaperone protein, specifically targeting its C-terminal domain. By directly interacting with Hsp90, it effectively disrupts its chaperone activity, leading to a significant reduction in cellular growth. This compound has been shown to strongly inhibit the proliferation of Saccharomyces cerevisiae strains, specifically cog7Δ and cog8Δ, making it a valuable tool for research into protein homeostasis and cellular stress response pathways. -
HSP90 Inhibitor
HSP90-IN-9 is a highly potent and selective inhibitor of the heat shock protein 90 (HSP90). This compound exhibits pronounced fungicidal activity in a dose-dependent manner and effectively inhibits fungal biofilm formation and morphological alterations when used in conjunction with fluconazole (FLC). Additionally, HSP90-IN-9 enhances FLC sensitivity by down-regulating the expression of key resistance-related genes, including ERG11, CDR1, and CDR2, making it a valuable tool for research applications in antifungal resistance studies. -
Hsp90 Inhibitor
Hsp90-IN-41 is a potent inhibitor of Heat Shock Protein 90 (Hsp90) with an IC50 of 0.044 μM. This compound demonstrates significant antifungal and antitumor activity, exhibiting an IC50 of 0.049 μM in vitro. It is valuable for research applications related to cancer and fungal diseases, particularly in studying the therapeutic potential of Hsp90 modulation. -
HSP90/EGFR Inhibitor
Wighteone, a prenylated isoflavone, acts as an HSP90 and EGFR inhibitor, specifically targeting the EGFR L858R/T790M mutations. This compound effectively reduces HSP90 expression, inhibits EGF-induced phosphorylation of EGFR, and disrupts downstream signaling through ERK and AKT pathways. Wighteone demonstrates significant biological activity by inducing cell cycle redistribution, inhibiting proliferation, and triggering apoptosis in various cancer cell lines. It is relevant for research on HER2-positive breast cancer, leukemia, non-small cell lung cancer with specific mutations, and also displays antifungal properties. -
HSP90/LSD1 Inhibitor
HSP90/LSD1-IN-1 is a dual inhibitor targeting HSP90 and LSD1, effectively disrupting their interaction and function. This compound demonstrates significant antiproliferative activity in prostate cancer cell lines, exhibiting GI50 values of 0.24 μM for PC-3 and 0.30 μM for DU145. It is a valuable tool for research into therapeutic strategies against prostate cancer and the role of chaperone proteins and histone demethylases in tumor biology. -
Hsp90 Inhibitor
PU24FCl is a selective inhibitor of the heat shock protein 90 (Hsp90). This compound demonstrates significant anti-cancer activity, promoting tumor regression by disrupting chaperone activity critical for the stability and function of multiple oncogenic clients. Notably, PU24FCl selectively accumulates in tumor tissues while being rapidly eliminated from normal tissues, enhancing its therapeutic potential in cancer research applications. -
Hsp90 Inhibitor
Conglobatin is a macrolide dilactone that functions as an Hsp90 inhibitor. It selectively binds to the N-terminal domain of Hsp90, effectively disrupting the Hsp90-Cdc37 complex formation. This compound demonstrates significant apoptotic activity in human breast cancer cells and esophageal squamous cell carcinoma cells, and it exhibits notable antitumor efficacy in vivo, making it a potential candidate for cancer research applications. -
HSP90/mTOR Inhibitor
HSP90/mTOR-IN-1 is a potent inhibitor targeting both Hsp90 and mTOR, exhibiting IC50 values of 69 nM and 29 nM, respectively. This compound effectively suppresses the proliferation of SW780 cells by over-activating the PI3K/AKT/mTOR signaling pathway. In addition to inducing apoptosis and autophagy through selective inhibition, HSP90/mTOR-IN-1 demonstrates significant in vivo anti-tumor activity. It serves as a valuable reagent for research applications focused on bladder cancer. -
Hsp-Cdc Inhibitor
Hsp90-Cdc37-IN-2 is a selective inhibitor of the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). This compound exhibits potent anti-proliferative activity against cancer cell lines A549, MCF-7, HOS, and HepG2, with IC50 values ranging from 0.41 to 0.94 μM. Hsp90-Cdc37-IN-2 effectively disrupts mitochondrial membrane potential, induces apoptosis, and causes cell cycle arrest at the G0/G1 phase in A549 cells, making it a valuable tool for cancer research and therapeutic investigations. -
HSP90β Inhibitor
CCT018159 is an ATP-competitive inhibitor of the HSP90β protein, exhibiting an IC50 of 3.2 μM against human HSP90β ATPase and 6.6 μM against yeast HSP90β ATPase. This compound induces cell cycle arrest and apoptosis in various tumor cell lines while effectively inhibiting processes such as invasion and angiogenesis. CCT018159 is particularly valuable for research applications in cancer biology and therapeutic development. -
HSP90AA1 Interactor, CNR1 Interactor, DRD2 Interactor,
Terrestrosin D is a small molecule that interacts with HSP90AA1, CNR1, and DRD2, functioning as an orally active apoptosis inducer. It effectively induces cell cycle arrest at the G1 and S phases while diminishing mitochondrial membrane potential, leading to the inhibition of growth in both cancer and endothelial cells. This compound is under investigation for its potential therapeutic applications in castration-resistant prostate cancer and pulmonary fibrosis. -
HSP Inhibitor
Cucurbitacin D is a potent HSP90 inhibitor that disrupts the interaction between Hsp90 and co-chaperones Cdc37 and p23. This compound exhibits significant biological activities, including the induction of cell cycle arrest and apoptosis, showcasing its potential as an anti-tumor and anti-inflammatory agent. Cucurbitacin D is useful in research applications aimed at understanding the role of heat shock proteins in cancer and inflammation. -
Hsp70 Inhibitor
JG-231 is an allosteric inhibitor targeting heat shock protein 70 (Hsp70). By disrupting the interaction between Hsp70 and BAG family proteins, JG-231 exhibits an inhibition constant (Ki) of 0.11 μM. This compound effectively inhibits tumor cell proliferation and induces apoptosis, demonstrating significant antitumor activity. JG-231 is valuable for research into the roles of Hsp70 in cancer biology and its potential as a therapeutic target. -
HSP90 C-terminal Inhibitor
NCT-58 is a potent C-terminal inhibitor of HSP90, which effectively disrupts the chaperone’s function without inducing the heat shock response. This compound exhibits significant anti-tumor activity by simultaneously downregulating HER family members and inhibiting Akt phosphorylation. Additionally, NCT-58 demonstrates the capability to kill trastuzumab-resistant breast cancer stem-like cells and induces apoptosis in HER2-positive breast cancer cells, making it a valuable tool for research on cancer therapeutics and resistance mechanisms. -
Hsp70 Inhibitor
YK5 is a potent and selective inhibitor of the heat shock protein 70 (Hsp70). It demonstrates a strong affinity for cytosolic Hsp70s in cancer cells, disrupting the formation of active oncogenic Hsp70/Hsp90/client protein complexes. This biological activity makes YK5 a valuable tool for research applications focused on cancer biology and the study of protein homeostasis in oncogenic processes. -
HSP90 Inhibitor
KW-2478 hydrochloride is a potent HSP90 inhibitor with an IC50 value of 3.8 nM. It exhibits significant anti-proliferative effects by inducing apoptosis in chronic myeloid leukemia (CML) and liver cancer cells. KW-2478 hydrochloride disrupts the BCR/ABL and MAPK signaling pathways, resulting in elevated levels of p27 and p21, along with reduced cyclin B1 expression. Additionally, it downregulates STAT3 expression, making it a valuable tool for cancer research, particularly in the contexts of CML and liver malignancies. -
HSP90 Inhibitor
HSP90-IN-10 is a selective inhibitor of the heat shock protein 90 (HSP90) chaperone. It demonstrates significant antiproliferative activity against HCC1954 breast cancer cells, with an IC50 value of 6 µM, while sparing normal epithelial cells from growth inhibition. Additionally, HSP90-IN-10 promotes apoptosis, making it a valuable tool for research into cancer therapies targeting the HSP90 pathway. -
Hsp90 Inhibitor
CPUY201112 is a potent inhibitor of heat shock protein 90 (Hsp90), exhibiting a Kd of 27 nM. This compound induces p53-mediated apoptosis in MCF-7 cells, leading to cell cycle arrest. CPUY201112 is a valuable tool for cancer research, particularly in studies focusing on apoptosis pathways and cell cycle regulation. -
HSP70 Inhibitor
PET-16 is a selective HSP70 inhibitor that targets an allosteric site in the substrate-binding domain. By hindering the ATP-ADP cycling of HSP70, PET-16 effectively disrupts chaperone activity and promotes apoptosis, particularly in multiple myeloma cells. This compound is valuable for research focused on cancer biology, apoptosis mechanisms, and the role of heat shock proteins in disease progression. -
Hsp90 Inhibitor
WK88-1 is a potent inhibitor of Heat Shock Protein 90 (Hsp90), which promotes the degradation of various oncogenic signaling proteins, including EGFR, ErbB2, and ErbB3. This compound effectively induces growth arrest and apoptosis in the Gefitinib-resistant H1975 cell line. WK88-1 is valuable for research applications focused on cancer biology, particularly in studies targeting Hsp90-dependent pathways in drug-resistant tumor models. -
HSP90 Inhibitor
17-Demethoxy-reblastatin is a potent inhibitor of heat shock protein 90 (Hsp90), exhibiting an IC50 value of 1.82 μM for yeast Hsp90 ATPase activity. This compound effectively inhibits the proliferation of cancer cell lines, including HepG2 and SMMC7721, while also reducing colony formation. Additionally, it induces apoptosis through mitochondrial and caspase-mediated pathways, making it a valuable reagent for cancer research and therapeutic investigations targeting Hsp90 activity. -
Hsp90/HDAC6 Inhibitor
HDAC6/HSP90-IN-2 is a dual inhibitor targeting both HDAC6 and Hsp90, exhibiting IC50 values of 105.7 nM and 61 nM, respectively. This compound demonstrates significant potential in cancer research, enabling the study of mechanisms involved in tumorigenesis and the development of novel therapeutic strategies. Its ability to modulate key cellular pathways associated with cancer progression makes it a valuable tool for investigating the role of HDAC6 and Hsp90 in various malignancies. -
Hsp90 Inhibitor
HSP90-IN-18 is a potent inhibitor of heat shock protein 90 (Hsp90), exhibiting an IC50 value of 0.39 μM. This compound effectively disrupts Hsp90 function, making it valuable for research into viral infections, neurodegenerative diseases, and inflammatory conditions. Its capability to modulate Hsp90 activity provides a useful tool for studying the biological pathways influenced by this essential chaperone protein. -
Hsp90-Cdc37 PPI Inhibitor
Hsp90-Cdc37-IN-4 is a selective inhibitor of the Hsp90-Cdc37 protein-protein interaction (PPI). This compound disrupts the interaction by inhibiting casein kinase 2 (CK2), leading to reduced phosphorylation of Cdc37 at Serine 13. In cellular assays, Hsp90-Cdc37-IN-4 has been shown to induce G0/G1 cell cycle arrest and activate apoptotic pathways via the mitochondria. Additionally, it exhibits significant anti-breast cancer properties, making it a valuable tool in cancer research. -
HSP90 Inhibitor
HSP90-IN-13 is a potent inhibitor of Heat Shock Protein 90 (HSP90) with an IC50 of 25.07 nM. This compound exhibits multi-target activity, affecting key proteins such as Epidermal Growth Factor Receptor (EGFR), Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2), and Topoisomerase-2. HSP90-IN-13 promotes cell cycle arrest at the G2/M phase and induces apoptosis in MCF-7 cancer cells via a mitochondrial-mediated pathway, making it a valuable reagent for cancer research and therapeutic studies. -
HSP70 Ligand
HSP70 Ligand 1 serves as a ligand for the heat shock protein 70 (HSP70), facilitating the development of PROTAC molecules. This compound is instrumental in synthesizing PROTAC HSP70 Degrader-1, enabling targeted protein degradation studies. It is valuable for researchers investigating HSP70's role in cellular stress responses and therapeutic applications. -
Combined with Hsp90
AMP-PCP disodium is an ATP analogue that specifically targets the N-terminal domain of Hsp90, exhibiting a dissociation constant (Kd) of 3.8 μM. By binding to Hsp90, AMP-PCP disodium promotes the formation of its active homodimer, facilitating studies on protein folding and maturation. This reagent is valuable for research applications focusing on molecular chaperones and their roles in cellular stress responses.
