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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PDE4 Inhibitor
GPD-1116 is a potent inhibitor of Phosphodiesterase (PDE) 4 and PDE1, demonstrating oral bioactivity. This compound effectively reduces smoke-induced apoptosis in lung cells, making it relevant for respiratory research. GPD-1116 shows promise in various animal disease models, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma, and pulmonary hypertension, supporting its potential therapeutic applications in pulmonary disorders. -
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. -
IDO/Tubulin Inhibitor
HI5 is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO) and tubulin, demonstrating an IC50 of 70 nM in HeLa cells. It effectively reduces kynurenine production, thereby promoting T cell activation and proliferation. Additionally, HI5 interferes with tubulin polymerization and migration, induces G2/M phase cell cycle arrest, and triggers apoptosis through a mitochondrial-dependent pathway, leading to increased reactive oxidative stress. HI5 is suitable for research in anticancer applications. -
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. -
MAO-B/Acetylcholinesterase Inhibitor
MAO-B-IN-26 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase, demonstrating neuroprotective properties against β-amyloid (Aβ) induced cytotoxicity in SH-SY5Y cells. This compound effectively mitigates morphological alterations, reactive oxygen species (ROS) generation, and membrane damage associated with neurodegeneration. Additionally, MAO-B-IN-26 suppresses Aβ-induced autophagy and apoptosis, making it a valuable tool for research focused on therapeutic strategies for Alzheimer's disease. -
TrxR Inhibitor
TrxR-IN-6 is an inhibitor of thioredoxin reductase (TrxR), a key enzyme in maintaining the cellular redox balance. This compound induces the accumulation of reactive oxygen species (ROS), leading to mitochondrial dysfunction, endoplasmic reticulum (ER) stress, and DNA damage. TrxR-IN-6 effectively promotes oxidative stress, resulting in apoptosis, making it a valuable tool for cancer research and studies focusing on oxidative stress mechanisms. -
PARP1/NAMPT Inhibitor
PARP1/NAMPT-IN-1 is a potent dual inhibitor of PARP1 and NAMPT, exhibiting IC50 values of 1.2 nM and 6.7 nM, respectively. This compound disrupts the homologous recombination repair pathway, leading to the accumulation of DNA double-strand breaks, which induces cell cycle arrest and apoptosis. Additionally, PARP1/NAMPT-IN-1 demonstrates antimigratory effects and has shown significant antitumor activity in a breast cancer xenograft model. It is a valuable tool for research on triple-negative breast cancer (TNBC). -
MAO-B Inhibitor
MAO-B-IN-49 is a selective and reversible inhibitor of monoamine oxidase B (MAO-B), with an impressive IC50 of 1 nM for human MAO-B and minimal activity against MAO-A (IC50 = 633.9 μM). This compound effectively reduces reactive oxygen species (ROS) production in HT22 cells, demonstrating substantial neuroprotective effects. In preclinical models of Parkinson's disease, MAO-B-IN-49 significantly mitigates motor dysfunction in MPTP-induced mice, making it a valuable reagent for studying neurodegenerative disorders and their underlying mechanisms. -
α-Amylase Inhibitor
α-Amylase-IN-14 is a selective inhibitor of α-amylase, demonstrating robust interactions with the enzyme (-5.55 kcal/mol). This compound serves as a dual anti-inflammatory and anti-hyperglycemic agent, exhibiting significant radical scavenging activity against DPPH and ABTS radicals. α-Amylase-IN-14 is valuable for research focused on diabetes and related metabolic disorders. -
MAO-B Inhibitor
Multi-target kinase-IN-10 is a selective and reversible inhibitor of monoamine oxidase B (MAO-B), exhibiting an IC50 of 0.0053 μM. This compound effectively penetrates the blood-brain barrier and competitively binds to the active site of MAO-B, disrupting substrate interactions. By chelating Cu2+ ions, it inhibits copper-induced reactive oxygen species (ROS) production and decreases the release of pro-inflammatory cytokines such as NO, TNF-α, and IL-1β. Multi-target kinase-IN-10 holds potential for therapeutic applications in the treatment of Parkinson's disease. -
PPARγ Inhibitor, heme oxygenase-1 Activator, Nrf2 Activator
PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders. -
Reactive Oxygen Species Inhibitor
Heme Oxygenase-1-IN-2 is a selective inhibitor of heme oxygenase-1, exhibiting an IC50 of 0.95 μM. This compound demonstrates significant antiproliferative activity in vitro, making it a valuable tool in the study of reactive oxygen species and their roles in cellular processes. Its application extends to research involving oxidative stress and potential therapeutic interventions in various diseases related to dysregulated oxidative pathways. -
HO Inhibitor
N'-Isonicotinoylisonicotinohydrazide is a competitive inhibitor of heme oxygenase (HO), demonstrating an IC50 range of 5-30 μM. This compound significantly impedes iron release, thereby disrupting iron acquisition in bacteria. It exhibits selective inhibitory effects on HO enzymes from Pseudomonas aeruginosa and Neisseria meningitidis, making it a valuable tool for investigating multidrug-resistant Gram-negative bacterial infections. -
Pancreatic Lipase/Acetylcholinesterase/Glutamic-oxaloacetic Transaminase 1/Alpha-glucosidase Inhibitor
Aspulvinone H is a potent inhibitor targeting pancreatic lipase, acetylcholinesterase, glutamic-oxaloacetic transaminase 1 (GOT1), and α-glucosidase, with IC50 values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It demonstrates key biological activities including inhibition of cancer cell proliferation, disruption of glutamine metabolism, and induction of apoptosis in cancer cells. Additionally, Aspulvinone H lowers postprandial blood glucose levels in mice and exhibits antibacterial properties against Staphylococcus aureus. This compound is suitable for research into pancreatic ductal adenocarcinoma, diabetes management, and infectious diseases caused by Staphylococcus aureus. -
HO-1 Inhibitor
Dehydrocurdione, a sesquiterpene derived from zedoary, acts as a heme oxygenase-1 (HO-1) inhibitor. It is known to induce the expression of HO-1 in RAW 264.7 macrophages through interaction with Keap1, leading to the translocation of Nrf2 and activation of the HO-1 E2 enhancer. Additionally, Dehydrocurdione demonstrates anti-inflammatory properties by suppressing lipopolysaccharide-induced nitric oxide release, marking its potential application in research related to inflammation and oxidative stress. -
HO-1/HO-2 Inhibitor
Azalanstat is an imidazole-dioxolane derivative that functions as a specific inhibitor of heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2), with IC50 values of 5.5 µM and 24.5 µM, respectively. This compound is valuable for studying the roles of HO-1 and HO-2 in various biological processes, including inflammation and oxidative stress. Its inhibition properties make Azalanstat a useful tool in research focused on diseases where the modulation of heme oxygenase activity is relevant. -
FXR Inhibitor
Gly-β-MCA is a potent farnesoid X receptor (FXR) inhibitor, selectively acting within the intestine. This stable bile acid demonstrates significant biological activity, making it a promising candidate for research focused on metabolic disorders. Its oral bioavailability enhances its potential for therapeutic application and further investigation in related studies. -
Foxo1 Inhibitor
AS1708727 is an orally active inhibitor of Foxo1, exhibiting EC50 values of 0.33 μM for glucose-6-phosphatase (G6Pase) and 0.59 μM for phosphoenolpyruvate carboxykinase (PEPCK). This compound plays a significant role in modulating metabolic pathways and is valuable for research into glucose homeostasis and metabolic disorders. AS1708727 can be utilized in studies investigating the therapeutic potential of targeting Foxo1 in various diseases, including diabetes and cancer. -
HMG-CoA Reductase Inhibitor
Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor that effectively reduces blood lipid levels. This compound demonstrates the ability to inhibit human smooth muscle cell proliferation and invasion, with IC50 values of 0.39 μM and 2.39 μM, respectively. Its capacity to modulate lipid metabolism makes it significant for research in cardiovascular diseases and metabolic disorders. -
FAAH Inhibitor
Macamide B is a selective inhibitor of fatty acid amide hydrolase (FAAH), derived from the plant Lepidium meyenii. This compound has been shown to enhance levels of endocannabinoids by inhibiting their degradation, thereby playing a crucial role in modulating pain and inflammation. Macamide B is primarily utilized in research focused on pain management, neuroprotection, and the therapeutic potential of endocannabinoids in various physiological processes. -
12R-LOX Inhibitor
12R-LOX-IN-2 is a potent inhibitor of 12R-lipoxygenase (12R-LOX), demonstrating significant biological activity in the modulation of keratinocyte proliferation. This compound effectively inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and suppresses colony formation. Additionally, 12R-LOX-IN-2 decreases protein levels of Ki67 and mRNA expression of IL-17A in IMQ-treated cells, making it a valuable reagent for research on psoriasis and related skin inflammatory conditions.
