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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Nampt Inhibitor
Daporinad hydrochloride is a potent non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki of 0.3 nM. It induces cellular effects such as depletion of NAD+ and ATP levels, suppression of the mTORC1 and MAPK/ERK signaling pathways, and activation of TFEB, leading to enhanced autophagy. Additionally, Daporinad hydrochloride disrupts the endoplasmic reticulum calcium pool, impairing T cell activation through diminished mitogen-induced calcium signaling. This compound is valuable for research in myeloma, liver cancer, and immunosuppression, with effects including cell cycle arrest and apoptosis in various cancer cell lines. -
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. -
TrxR1 Inhibitor
LW-216 is a potent inhibitor of Thioredoxin Reductase 1 (TrxR1), known to induce apoptosis in cancer cells. This compound exhibits significant anti-tumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its mechanism of action and biological effects position LW-216 as an important reagent for studying redox regulation and cell death pathways in oncological contexts. -
NAMPT Inhibitor
Nampt-IN-8 is a selective inhibitor of Nicotinamide Adenine Dinucleotide Phosphate (NAMPT) with an IC50 value of 0.183 μM. This compound effectively induces apoptosis in cultured cells and enhances reactive oxygen species (ROS) production. It is a valuable tool for research on metabolic regulation and cellular stress responses, particularly in studies related to cancer and neurodegenerative diseases. -
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. -
PARP/NAMPT Inhibitor
PARP1/NAMPT-IN-2 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 0.8 nM and 18 nM, respectively. This compound effectively inhibits cell proliferation and migration, while inducing apoptosis in breast cancer cells. PARP1/NAMPT-IN-2 is particularly relevant for investigating therapeutic strategies in triple-negative breast cancer research. -
PDE4/7 Inhibitor
BC-54 is a selective inhibitor of phosphodiesterase 4 (PDE4) and phosphodiesterase 7 (PDE7). It exhibits potent anti-inflammatory effects and can induce apoptosis in cancer cells, making it a valuable tool for research focused on cancer and inflammation. BC-54 is particularly relevant in studies investigating chronic lymphocytic leukemia and other conditions associated with these pathways. -
TrxR Inhibitor
TrxR-IN-8 is a selective inhibitor of thioredoxin reductase (TrxR), exhibiting an IC50 value of 10.2 μM. This compound induces apoptosis in cancer cells through the generation of reactive oxygen species (ROS), depletion of intracellular thiols, and alteration of the glutathione/glutathione disulfide ratio. TrxR-IN-8 demonstrates considerable cytotoxic effects in non-small cell lung cancer (NSCLC) cells, making it a valuable tool in cancer research and therapeutic studies focused on oxidative stress and cell death mechanisms. -
PDE4 Inhibitor
CC-3052 is a selective phosphodiesterase 4 (PDE4) inhibitor exhibiting immunomodulatory properties. It effectively reduces neutrophil apoptosis in HIV-positive contexts, highlighting its potential in the study of HIV-related diseases. This compound serves as a valuable tool for researchers investigating the modulation of immune responses in viral infections. -
NAMPT Inhibitor
CHS-828 (nicotinate) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), exhibiting an IC50 of less than 25 nM. This compound effectively reduces cellular levels of NAD+, leading to cytotoxic effects on cancer cells. CHS-828 is primarily utilized in cancer research applications, studying its anti-tumor properties and mechanisms of action in various malignancies. -
IDH1 Inhibitor
IDH1 Inhibitor 9 is a selective inhibitor targeting isocitrate dehydrogenase 1 (IDH1), exhibiting IC50 values of 124.4 nM and 95.7 nM for the R132H and R132C mutations, respectively. This compound effectively induces apoptosis and promotes cell cycle arrest at the S phase. Due to its anti-tumor properties, IDH1 Inhibitor 9 is valuable for research in cancer biology and the development of targeted therapies in IDH1-mutated cancers. -
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. -
Lactate Dehydrogenase Inhibitor
Galloflavin potassium is a selective inhibitor of lactate dehydrogenase, primarily targeting the conversion of pyruvate to lactate. This compound effectively disrupts aerobic glycolysis in PLC/PRF/5 cells, promoting apoptotic cell death. Galloflavin potassium is valuable for research applications related to cancer biology, particularly in studies focused on metabolic reprogramming and the Warburg effect. -
IDO1 Inhibitor
LW106 is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an IC50 of 1.57 μM. It preferentially targets IDO1 without affecting IDO2 or tryptophan 2,3-dioxygenase (TDO). LW106 demonstrates antitumor activity by disrupting stroma-immune interactions and reducing the enrichment of cancer stem cells (CSCs) within the tumor microenvironment, leading to decreased tumor cell proliferation and increased apoptosis. This compound is suitable for research applications in lung cancer and melanoma. -
CYP51 Inhibitor
Antifungal agent 136 is an irreversible inhibitor of fungal lanosterol 14α-demethylase (CYP51). It demonstrates potent antifungal activity against drug-resistant strains of Candida albicans and effectively downregulates IL-6 expression. This compound holds potential for research applications in the fields of fungal infection and inflammatory diseases. -
PKM2 Inhibitor
PKM2 modulator 2 (compound C599) is a potent inhibitor of pyruvate kinase M2 (PKM2), a key regulator of cellular metabolism. This compound exhibits significant antiproliferative activity and induces apoptosis in various cancer cell lines. PKM2 modulator 2 is a valuable tool for research on glioblastoma and other malignancies where PKM2 plays a critical role in tumorigenesis. -
RARγ Inhibitor
ZSH-512 is a potent inhibitor of retinoic acid receptor gamma (RARγ). It demonstrates significant antiproliferative effects by inducing apoptosis in cancer cells, while concurrently downregulating key stemness markers such as CD133, NANOG, SOX2, and EPCAM. With its strong anticancer activity, ZSH-512 is a valuable tool for investigating therapeutic strategies in colorectal cancer research. -
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. -
PDE5 Inhibitor
PDE5-IN-3 is a potent phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 of 1.57 nM. In addition to its primary mechanism, PDE5-IN-3 demonstrates moderate inhibition of epidermal growth factor receptor (EGFR) with an IC50 of 5.827 µM and significantly affects the Wnt/β-catenin signaling pathway with an IC50 of 1286.96 ng/mL. This compound has been shown to induce the intrinsic apoptotic mitochondrial pathway in HepG2 cells and displays strong antitumor activity, making it valuable for cancer research applications. -
Ser/Thr Protease Inhibitor
ONO-3403 is an orally active serine/threonine protease inhibitor that targets key proteolytic processes. This compound has been shown to inhibit lipopolysaccharide (LPS)-induced production of tumor necrosis factor-alpha (TNF-α) and nitric oxide, demonstrating anti-inflammatory properties. Additionally, ONO-3403 exhibits cytotoxic effects by inhibiting cell growth and inducing apoptosis, making it a valuable tool in antitumor research. -
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. -
IDH1 Inhibitor
ZD-2767P is a reversible and competitive inhibitor of isocitrate dehydrogenase 1 (IDH1), with an IC50 value of 410 nM. This compound has been shown to effectively modulate IDH1 activity, making it a valuable tool for investigating metabolic pathways and oncogenic processes associated with IDH1 mutations. ZD-2767P is suitable for research applications focused on cancer biology and metabolic regulation. -
PDE5/HDAC Inhibitor
PDE5/HDAC-IN-1 is a dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) with IC50 values of 46.3 nM and 14.5 nM, respectively. This compound has demonstrated the capability to induce cell apoptosis and exhibits significant anticancer activities. PDE5/HDAC-IN-1 is a valuable tool for research in cancer therapeutics and epigenetic modulation. -
Mutant IDH1/NAMPT Inhibitor
Mutant IDH1/NAMPT-IN-1 is a dual inhibitor targeting mutant isocitrate dehydrogenase 1 (mutant IDH1) and nicotinamide phosphoribosyltransferase (NAMPT), with IC50 values of 14.93 nM and 12.56 nM, respectively. This compound effectively induces apoptosis, making it a valuable tool for research into cancer mechanisms and treatment strategies. Additionally, Mutant IDH1/NAMPT-IN-1 demonstrates the capability to cross the blood-brain barrier, enhancing its potential for applications in neurological studies and therapies. -
PDEIII Inhibitor
Anagrelide hydrochloride monohydrate is a selective inhibitor of phosphodiesterase type III (PDE3), with an IC50 value of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and reduces bone marrow megakaryocytopoiesis. Additionally, Anagrelide hydrochloride monohydrate demonstrates the capability to decrease cell proliferation and induce apoptosis in gastrointestinal stromal tumor (GIST) cells in vitro, making it relevant for research in hematology and oncology. Its platelet-lowering properties contribute to its antithrombopoietic effects. -
NAMPT Inhibitor
Nampt-IN-16 is a potent NAMPT inhibitor exhibiting an IC50 value of 0.15 μM. This compound effectively reduces intracellular levels of NAD+ and ATP, leading to the inhibition of proliferation, migration, and invasion in gastric cancer cells. Additionally, Nampt-IN-16 induces cell cycle arrest and apoptosis while altering cellular metabolism. It is a valuable tool for research focused on tumors, particularly gastric cancer. -
TrxR Inhibitor
TrxR Inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR) with an EC50 of 2.8 nM. This compound effectively inhibits tumor proliferation in both in vitro and in vivo studies, making it a valuable tool for cancer research. Its ability to modulate TrxR activity supports investigations into redox biology and therapeutic strategies targeting oxidative stress in cancer cells.
