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Catalog No.
Product Name
Application
Product Information
Citations
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Hsp70 Inhibitor
YM-1 tosylate is a stable analog of MKT-077 that functions as an orally active inhibitor of Hsp70. This compound has been shown to induce cell death in HeLa cells, while also up-regulating p53 and p21 protein levels. YM-1 tosylate is valuable for research applications focused on cancer biology and cellular stress responses. -
HSP90 Inhibitor
DDO-6691 is a potent inhibitor of heat shock protein 90 (HSP90), targeting its role in protein folding and stabilization. This compound demonstrates significant antiproliferative activity against various tumor cell lines, particularly HCT-116 colon cancer cells, with an IC50 of 1.08 μM. DDO-6691 also effectively inhibits tumor growth in the HCT-116 xenograft mouse model, highlighting its potential for cancer research and therapeutic applications. -
HSP Inhibitor
Monorden diacetate is an effective Hsp90 inhibitor that demonstrates significant potential in the development of new fungicides. By targeting the heat shock protein 90 (HSP90), it disrupts the molecular chaperone activity essential for the stability and function of various client proteins. This compound is valuable for research applications focused on fungal biology and disease management. -
HSP Induction Inhibitor
NSC-134754 is a dehydroemetine derivative that functions as a heat shock protein induction inhibitor. It specifically targets Hsp72 and Hsp27 at the post-transcriptional level, without affecting overall protein synthesis, HSF-1 transcriptional activity, or Hsp mRNA levels. Preclinical studies indicate that NSC-134754 exhibits minimal toxicity while enhancing the sensitivity of cancer cells to proteasome and Hsp90 inhibitors. This reagent is applicable in research involving multiple myeloma, prostate carcinoma, and colon carcinoma. -
HSP90 Inhibitor
MPC-0767 is a selective and potent inhibitor of heat shock protein 90 (HSP90). As an L-alanine ester proagent of MPC-3100, it exhibits enhanced chemical stability, making it suitable for in vivo applications. MPC-0767 is primarily utilized in research applications focused on cancer biology, as it disrupts the chaperone function of HSP90 and thereby influences the stability of various oncogenic client proteins. -
Hsp90-TPR2A Interaction Inhibitor
Hsp90-IN-43 is a potent inhibitor of the Hsp90-TPR2A interaction, exhibiting an IC50 value of 360 nM and a Kd of 928 nM. This compound effectively inhibits the proliferation of BT474 breast cancer cells, making it a valuable tool for research in breast cancer biology. Its specific activity allows for deeper investigation into the role of Hsp90 in cancer progression and therapeutic response. -
Dye Tethered Hsp90 Inhibitor
HS-131 is a dye-tethered inhibitor that targets heat shock protein 90 (Hsp90). This compound exhibits the ability to selectively bind to and inhibit Hsp90, facilitating the detection of oncogene-driven breast cancers across various molecular subtypes. HS-131 is a valuable research tool for studying the role of Hsp90 in cancer biology and for developing novel therapeutic strategies targeting breast cancer. -
Hsp90α/Hsp90β Inhibitor
PU-11 is a selective inhibitor of Hsp90α and Hsp90β, targeting the ATP-binding pocket of these heat shock proteins. It exhibits IC50 values of 18.6 μM and 89.8 μM, along with Kd values of 2 μM for Hsp90α and 4.2 μM for Hsp90β, demonstrating a preference for Hsp90α due to the unique Ser52 residue. PU-11 is applicable in research related to neurodegenerative disorders, providing insights into the role of Hsp90 in cellular stress responses and protein homeostasis. -
HSP Inhibitor
HSP90-IN-28 is a selective inhibitor of heat shock protein 90 (Hsp90), demonstrating an IC50 value of 0.46 μM for Hsp90α and approximately 48-fold selectivity over Hsp90β (IC50 = 22.28 μM). This compound is instrumental in research focused on cellular stress responses, cancer biology, and protein homeostasis. Its specificity makes HSP90-IN-28 an effective tool for studying the role of Hsp90 in various physiological and pathological processes. -
FKBP51-Hsp90 Inhibitor
FKBP51-Hsp90-IN-2 is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, demonstrating IC50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. This compound has been shown to enhance cellular energy metabolism and promote neurite growth. Its efficacy makes FKBP51-Hsp90-IN-2 a valuable tool in research focused on neurodegenerative diseases and cancer. -
MAO A/HSP90 Inhibitor
MAO A/HSP90-IN-1 is a dual inhibitor targeting MAO A and HSP90, exhibiting IC50 values of 1.77 μM in glioblastoma GL26 cells and 0.019 μM for HSP90α. This compound effectively inhibits MAO A activity, disrupts HSP90 binding, and downregulates HER2 and phospho-Akt expression, leading to reduced growth of glioblastoma cells. Additionally, MAO A/HSP90-IN-1 decreases PD-L1 expression, which may hinder tumor immune escape and suppress T cell activation. This reagent serves as a valuable tool for research on brain tumor-related diseases. -
HSP90 Inhibitor
HSP90-IN-29 is a selective inhibitor of heat shock protein 90 (HSP90), exhibiting a potent IC50 value of 30 nM. This benzoxazole derivative demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its specific targeting of HSP90 allows for the exploration of its role in oncogenesis and the development of therapeutic strategies against malignancies. -
Hsp90 Inhibitor
HSP90-IN-35 is a selective Hsp90 inhibitor that exhibits potent antitumor activity, with an IC50 value for Her2 in the range of 0.05 to 0.5 μM. This compound is valuable for research applications focused on cancer biology and therapeutic development. Additionally, HSP90-IN-35 can be utilized in the synthesis of PROTACs, facilitating the exploration of targeted protein degradation strategies in cellular models. -
Hsp90 Inhibitor
C086 is a potent inhibitor of Heat Shock Protein 90 (Hsp90), a crucial chaperone involved in protein folding and stability. This compound has been shown to inhibit cell cycle progression and induce apoptosis across various cell types. It also exhibits anti-metastatic properties, making it a valuable tool for research in cancer biology and therapeutic development targeting Hsp90. -
HSP70 Inhibitor
HSP70-IN-5 is a selective inhibitor of the heat shock protein 70 (HSP70). It demonstrates an IC₅₀ of 0.6 μM in HSP70/DnaJ-mediated luciferase reconstitution assays. This compound serves as a valuable biochemical probe for investigating the functional role of HSP70 and its co-chaperone DnaJ in diverse biological processes, including protein folding and stress response pathways. -
Aha1-Hsp90 Complex Inhibitor
Hsp90-IN-34 is a potent inhibitor of the Aha1-Hsp90 chaperone complex, displaying a high affinity for Hsp90 and Aha1 with a dissociation constant (KDapp) of 23.5 µM. This compound interferes with the ATPase activity of Hsp90 by disrupting its interaction with Aha1, thereby influencing chaperone-mediated protein folding and stability. Hsp90-IN-34 is valuable for research into cancer biology and the modulation of protein homeostasis. -
HSP90 Inhibitor
ML189 is a selective inhibitor of HSP90, a critical chaperone involved in protein folding and stability. By disrupting HSP90 activity, ML189 induces the degradation of client proteins, which can affect cellular proliferation and survival. This compound is primarily utilized in research related to infectious diseases, including candidiasis, and provides insights into the role of HSP90 in pathogen biology and therapeutic development. -
HSP90 Inhibitor
ML229 is a high-affinity inhibitor of HSP90, a chaperone protein crucial for the stability and function of various client proteins. This compound demonstrates significant biological activity in modulating heat shock protein activity, making it a valuable tool for investigating the role of HSP90 in various cellular processes. ML229 has potential applications in the research of infectious diseases, including candidiasis, as it can interfere with the growth and survival of pathogenic organisms reliant on HSP90 for their virulence. -
HSP90 Inhibitor
BIIB-028 is an orally active inhibitor of heat shock protein 90 (Hsp90), primarily targeting its ATP-binding site. By disrupting Hsp90 function, BIIB-028 promotes the degradation of client proteins essential for cancer cell survival and proliferation. This compound is valuable for research in cancer biology and therapeutic development aimed at targeting Hsp90. -
Hsp70 Inhibitor
JG-48 is an inhibitor of the heat shock protein 70 (Hsp70), a molecular chaperone involved in protein folding and stabilization. This compound effectively reduces tau protein levels in various tauopathy models, making it a valuable tool for studying neurodegenerative diseases. Its specific targeting of Hsp70 provides insights into the role of protein aggregation in tau-related pathologies. -
NMT1/2 Inhibitor
IMP-1088 is a highly potent dual inhibitor of human N-myristoyltransferases NMT1 and NMT2, exhibiting IC50 values of less than 1 nM for both isoforms and a Kd of under 210 pM for NMT1. This compound effectively inhibits rhinovirus replication by blocking the N-myristoylation of the virus-encoded protein VP0, thereby preventing the virus from completing its lifecycle. In addition, IMP-1088 offers protective effects to host cells by mitigating the cytotoxic consequences associated with viral infections, making it a valuable tool for research into antiviral therapies. -
NMT Inhibitor
DDD85646 is a potent inhibitor of N-myristoyltransferase (NMT), specifically targeting the enzyme from Trypanosoma brucei with an IC50 of 2 nM and human NMT with an IC50 of 4 nM. This compound demonstrates significant potential for therapeutic applications in treating human African trypanosomiasis by disrupting lipid modifications essential for parasite survival. Its oral bioavailability further enhances its applicability in drug development for infectious diseases caused by trypanosomes. -
Lipoxygenase Inhibitor
β-Boswellic acid, a potent inhibitor of 5-lipoxygenase (5-LO), is derived from the gum resin of Boswellia serrata. This compound exhibits significant anticancer, antioxidant, anti-inflammatory, and anti-arthritic properties. Its mechanism involves direct interaction with 5-LO or inhibition of its translocation, leading to reduced synthesis of DNA, RNA, and protein in human leukemia HL-60 cells, with IC50 values ranging from 0.6 to 7.1 μM. β-Boswellic acid holds potential for research into diabetes and inflammatory disorders, particularly those related to arthritis. -
Ser/Thr Protease Inhibitor
Antipain dihydrochloride is a potent Ser/Thr protease inhibitor derived from Actinomycetes. It is known to inhibit N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation, leading to an increase in chromosomal aberrations. Additionally, Antipain dihydrochloride has been shown to restrict uterine DNA synthesis and functionality in murine models, making it a valuable tool for studying proteolytic processes and their implications in cellular biology and genetics. -
PDE1C/PDE4B Inhibitor
Sudachitin is a potent inhibitor of phosphodiesterase 1C (PDE1C) and phosphodiesterase 4B (PDE4B), exhibiting IC50 values of 5.0 μM and 15.0 μM, respectively. It enhances the expression of Sirt1 and PGC-1α in skeletal muscle, thereby influencing energy metabolism and promoting mitochondrial biogenesis. Sudachitin demonstrates beneficial effects on lipid metabolism, improves glucose tolerance and insulin sensitivity, and stimulates energy expenditure and fatty acid β-oxidation. Additionally, it activates the p38MAPK signaling pathway, influences apoptosis, and exhibits significant anti-inflammatory properties by reducing TNF-α, NO, and iNOS expression in macrophages. This compound is suitable for research in metabolic syndrome, type 2 diabetes, and psoriasis. -
PTBP1 Inhibitor
PT109 is a potent inhibitor of the protein-targeting poly(A)-binding protein 1 (PTBP1). By promoting the conversion of the pyruvate kinase isoform from PKM2 to PKM1, PT109 effectively suppresses the proliferation and migration of glioblastoma multiforme and facilitates its reprogramming into oligodendrocytes. Additionally, PT109 interacts with key signaling pathways, including JNK, SGK1, and GSK3β, conferring neuroprotective effects that enhance neurogenesis, foster synapse formation, and mitigate neuroinflammation. In models of Alzheimer's disease, PT109 demonstrates significant improvements in spatial learning, making it a valuable tool for researching metabolic reprogramming in glioblastoma and neuroprotection in neurodegenerative disorders. -
HSP60 Inhibitor
DCEM1 is a potent inhibitor of heat shock protein 60 (HSP60), disrupting its interaction with ClpP and thereby impeding the mitochondrial unfolded protein response. This compound has been shown to significantly inhibit β-catenin expression and ATP production in both PC-3 and TKO cell lines. DCEM1 is a valuable tool for investigating the role of HSP60 in prostate cancer research and understanding its impact on cellular metabolism and signaling pathways. -
Hsp90 Inhibitor
BIIB021 mesylate is a potent inhibitor of the heat shock protein 90 (Hsp90). This orally active compound effectively inhibits the proliferation of chronic myeloid leukemia (CML) cells, demonstrating IC50 values of 513.99 nM for K562, 603.53 nM for K562/G, 110.08 nM for 32Dp210, and 148.07 nM for 32Dp210-T315I cell lines. BIIB021 promotes the degradation of the BCR-ABL protein and suppresses the β-catenin/c-Myc pathway, while also inducing autophagy in CML cells. This compound serves as a valuable tool for research focused on CML and Hsp90-related pathways. -
Cathepsin L Inhibitor
Cathepsin L-IN-6 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 0.021 μM. It functions by directly binding to cathepsin L, effectively suppressing its enzymatic activity. Additionally, Cathepsin L-IN-6 inhibits pro-inflammatory cytokines IL-6 and IL-8, demonstrating significant anti-inflammatory properties. This compound is particularly relevant for research focused on acute lung injury and related inflammatory conditions. -
HSP90α Inhibitor
HSP90α-IN-1 is a selective inhibitor of HSP90α, with an IC50 value of 111 nM, demonstrating significant senolytic activity in diverse cellular senescence models. This compound is associated with the xanthinic family and plays a critical role in investigations aimed at addressing age-related inflammaging and associated diseases, including cancer. HSP90α-IN-1 is also being explored for its potential to promote healthy lifespan extension in various biological research contexts. -
PDE4 Inhibitor
Etazolate is a selective phosphodiesterase 4 (PDE4) inhibitor that exhibits anti-inflammatory properties by reducing interleukin-1 beta (IL-1β) levels. This compound demonstrates a dose-dependent effect on inflammation and edema, while also contributing to enhanced memory performance. Additionally, Etazolate's modulation of GABAA receptors suggests potential applications in research related to mood disorders, particularly in studying antidepressant-like effects. -
PKM2 Inhibitor
LIQ1 is a potent allosteric inhibitor of Pyruvate kinase M2 (PKM2), targeting Arg43 within the polyarginine pocket with an IC50 of 0.39 μM and a Kd of 4.5 μM. This flavonoid derivative effectively prevents the nuclear translocation of PKM2 and its interaction with HIF-1α, leading to the suppression of IL-1β transcription. LIQ1 is valuable for research involving endotoxemic conditions, particularly in studies of inflammation and metabolic regulation. -
PDE4 Inhibitor
PDE4-IN-8 is a potent inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 of 0.93 nM specifically for the PDE4B2 isoform. This compound exhibits selective inhibition, with minimal effects on cytokines such as IL-13 (IC50 = 4.04 nM), IL-4 (IC50 = 36.33 nM), and IFN-γ (IC50 = 2394 nM). PDE4-IN-8 is suitable for research applications focused on inflammation and other PDE4-related pathways in various biological contexts. -
PDE3A/PDE4B Inhibitor
PDE3/4-IN-4 is a potent and selective inhibitor of phosphodiesterase 3A (PDE3A) and phosphodiesterase 4B (PDE4B), exhibiting IC50 values of 10 nM and 9.4 nM, respectively. This compound modulates the cAMP/PKA/CREB signaling pathway, effectively inhibiting the pro-inflammatory cytokine IL-6 and reducing expression of inflammatory markers in liver tissue. PDE3/4-IN-4 demonstrates potential in mitigating liver fibrosis and limiting liver damage in models of cholestatic and sepsis-induced liver diseases. This reagent is suitable for research focused on liver injury and cholestatic liver disorders. -
Hsp90 Inhibitor
Pochonin D ((+)-Pochonin D) is a potent inhibitor of heat shock protein 90 (Hsp90) with demonstrated antiviral and anti-inflammatory activities. By targeting Hsp90, Pochonin D disrupts the proper folding, stabilization, and assembly of client proteins, including viral proteins, thereby impairing viral protein homeostasis and significantly reducing viral replication capacity. In addition, Pochonin D exhibits anti-inflammatory effects by attenuating inflammatory cell infiltration and suppressing the production of pro-inflammatory cytokines, such as TNF-α and IL-1β. These combined pharmacological properties highlight Pochonin D as a promising small-molecule tool for the study of human rhinovirus (HRV) infection and cancer-related pathways.
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PFKFB4 Inhibitor
5MPN is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4), exhibiting competitive inhibition at the fructose-6-phosphate binding site with a Ki of 8.6 μM. This compound does not affect PFK-1 or PFKFB3, allowing for targeted modulation of glucose metabolism in cancer cells. 5MPN has demonstrated the ability to suppress the proliferation of various human cancer cell lines, making it a valuable tool for research in cancer metabolism and therapeutic development. -
PTP1B Inhibitor
Caffeoyltryptophan is a competitive inhibitor of protein tyrosine phosphatase 1B (PTP1B), exhibiting an IC50 of 16.99 μM. Additionally, it demonstrates inhibitory effects on α-glucosidase, linoleic acid peroxidation, and hemolysis. This compound is primarily utilized in research related to type 2 diabetes, offering insights into metabolic regulation and potential therapeutic avenues. -
PFKFB3 Inhibitor
PFKFB3-IN-2 is a selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). It demonstrates key biological activity by modulating glucose metabolism, making it relevant in cancer research and neurodegenerative disorders. This compound holds potential for applications in autoimmune diseases, inflammatory conditions, multiple sclerosis, metabolic disorders, and the study of angiogenesis. -
DPP-4 Inhibitor
Antidiabetic agent 2 is a potent DPP-4 inhibitor that effectively promotes glucose uptake. This compound also inhibits PTP-1B, α-amylase, and α-glucosidase, exhibiting IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. By decreasing blood glucose levels, Antidiabetic agent 2 serves as a valuable tool for research focused on diabetes management and the modulation of glucose homeostasis. -
Phosphatase Inhibitor
Chrysophanol triglucoside is an anthraquinone with a specific inhibitory action on protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase, demonstrating IC50 values of 80.17 µM and 197.06 µM, respectively. This compound is derived from Cassia obtusifolia and has potential applications in diabetes research, particularly in the study of glucose metabolism and insulin signaling pathways. -
Carbonic Anhydrase/Alkaline Phosphatase Inhibitor
ALP/Carbonic Anhydrase-IN-1 is a dual inhibitor of carbonic anhydrase (CA) and alkaline phosphatase (ALP), selectively targeting key isoforms. It demonstrates IC50 values of 0.44 µM for CA-II, 1.61 µM for CA-IX, 0.51 µM for CA-XII, and 0.107 µM for ALP, indicating potent inhibitory activity. This compound is useful in exploring the roles of carbonic anhydrase and alkaline phosphatase in various biological processes and disease models. -
PTP1B/hMAO-A Inhibitor
Cassiaside B2 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A). This compound exhibits significant antiallergic properties and functions as a 5-HT2C receptor agonist. It serves as a valuable tool for understanding the modulation of these targets in various biological pathways and contributes to research in neuropharmacology and allergy-related studies. -
PFKFB3 Inhibitor
(E/Z)-3PO is a selective inhibitor of PFKFB3, a key regulator of glycolysis. This compound effectively inhibits glycolysis, reduces the extracellular acidification rate, and suppresses angiogenesis by impairing endothelial cell migration and capillary tube formation. Research applications of (E/Z)-3PO include investigations into cancer, acute lung injury, pulmonary fibrosis, and atherosclerosis, making it a valuable tool for exploring therapeutic strategies in these diseases. -
Hsp110-STAT3 Interaction Inhibitor
Hsp110-STAT3 PPI-IN-1 is a potent inhibitor of the Hsp110-STAT3 protein-protein interaction. This compound exhibits antiproliferative activity against the HPAEC cell line, demonstrating an IC50 value of 22.67 μM. It serves as a valuable tool for investigating the role of Hsp110-STAT3 interactions in various biological processes and therapeutic applications. -
HMG-CoA Inhibitor
HMG499 is a potent and selective inhibitor of HMG-CoA reductase, exhibiting an IC50 of 0.41 μM. This compound effectively reduces serum cholesterol levels and mitigates the statin-induced accumulation of HMGCR, making it a valuable tool for research in lipid metabolism and atherosclerosis. HMG499 is relevant for studies investigating cholesterol regulation and cardiovascular disease pathways. -
Cathepsin Inhibitor
LV-320 is a potent uncompetitive inhibitor of cathepsin ATG4B, exhibiting an IC50 of 24.5 μM and a Kd of 16 μM. This compound effectively inhibits the enzymatic activity of ATG4B, thereby obstructing autophagic flux in cellular environments. Due to its stability and low toxicity, LV-320 is suitable for in vivo applications, making it a valuable tool for research on autophagy-related pathways. -
Nampt Inhibitor
GPP78 is a potent inhibitor of nicotinamide adenine dinucleotide (NAD) biosynthesis via the enzyme Nampt, demonstrating an IC50 of 3.0 nM. It exhibits cytotoxicity in the neuroblastoma SH-SY5Y cell line, with an IC50 of 3.8 nM, primarily by inducing autophagy. GPP78 serves as a valuable tool in cancer and inflammatory research, highlighting its potential therapeutic applications in oncology. -
HMG-CoA Reductase Inhibitor
Atorvastatin hemicalcium trihydrate is an orally active inhibitor of HMG-CoA reductase, primarily utilized in the management of dyslipidemia by effectively lowering blood lipid levels. Additionally, it demonstrates inhibitory effects on human smooth muscle cell proliferation and invasion, with IC50 values of 0.39 μM and 2.39 μM, respectively. This compound is valuable for research focused on atherosclerosis, cardiovascular diseases, and cell growth regulation. -
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. -
PKM2 Inhibitor
Vitamin K5 is a specific inhibitor of pyruvate kinase M2 (PKM2), exhibiting IC50 values of 28, 191, and 120 μM against PKM2, PKM1, and PKL, respectively. It demonstrates notable biological activity by inducing apoptosis in colon 26 cells, making it relevant for cancer research. Furthermore, Vitamin K5 possesses antimicrobial properties and may be employed in studies related to infection. Its applications also extend to the preservation of pharmaceuticals, foods, and beverages.
