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Catalog No.
Product Name
Application
Product Information
Citations
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PDE3 inhibitor
Olprinone is a selective phosphodiesterase 3 (PDE3) inhibitor. -
DHFR inhibitor
Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. -
FAAH inhibitor
PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen. -
Hsp90 inhibitor
Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9. -
Human cathepsin L inhibitor
SID 26681509 is a reversible and potent human cathepsin L inhibitor. SID 26681509 displays no inhibitory activity of cathepsin G. -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
PAK4/NAMPT Inhibitor
KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. -
LXRα inhibitor
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects. -
HDAC/ACE inhibitor
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. -
DHFR inhibitor
Methotrexate is a cytotoxic agent that inhibits thymidylate synthetase and de novo purine synthesis. -
Dehydrogenase inhibitor
Mono-ammonium glycyrrhizinate(AMGZ) is a unique product derived from Licorice root and has an extremely sweet taste. -
Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
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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. -
Monoamine Oxidase Inhibitor
Harmol is a β-carboline alkaloid functioning as a monoamine oxidase inhibitor and TFEB activator. It has been shown to induce cell mitosis, autophagy, and apoptosis, promoting the degradation of α-synuclein through the autophagy-lysosomal pathway. Harmol exhibits notable anti-tumor, anti-depressant, and anti-aging properties and demonstrates efficacy in improving motor impairments in models of Parkinson's disease. This compound holds significant potential for research in neurodegenerative diseases and cellular autophagy mechanisms. -
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. -
IDO Inhibitor
(Rac)-Indoximod is an indoleamine 2,3-dioxygenase (IDO) inhibitor that modulates immune responses. This compound synergizes with interferon-gamma (IFN-γ) to significantly decrease the activity of human cardiac myofibroblasts, characterized by α-SMA expression, and promotes apoptosis by upregulating the genes IRF-1, Fas, and FasL. Its applications include studying immune regulation and apoptosis in cardiac tissue and investigating therapeutic strategies for fibrotic diseases. -
ACE Inhibitor
Benazepril is an orally active angiotensin-converting enzyme (ACE) inhibitor that reduces the production of angiotensin II. This compound exhibits protective effects against oxidative stress and apoptosis through modulation of the PI3K/Akt signaling pathway. Benazepril is commonly utilized in research focusing on hypertension, heart failure, and diabetic nephropathy, demonstrating efficacy in improving diabetic nephropathy and reducing proteinuria. -
PKM2 Inhibitor
PKM2-IN-6 is a potent inhibitor of pyruvate kinase M2 (PKM2), exhibiting an IC50 value of 23 nM. This compound induces apoptosis and facilitates cell cycle arrest at the G2 phase, demonstrating significant anticancer activity. PKM2-IN-6 also decreases the mRNA levels of both PKM1 and PKM2, indicating its effect on metabolic regulation. This reagent is particularly relevant for research applications focused on triple-negative breast cancer. -
PCSK9 Inhibitor
Pinostrobin is a flavonoid that acts as a potent inhibitor of PCSK9, targeting its catalytic activity. This compound demonstrates significant anti-cancer, antioxidant, antiviral, and neuroprotective properties. Pinostrobin is suitable for research applications in diverse areas, including viral infections, cancer therapeutics, cardiovascular and cerebrovascular disorders, cirrhosis, inflammatory diseases, and neurological conditions. -
GLUT4 Inhibitor
GLUT4-IN-2 is a selective inhibitor of the glucose transporter GLUT4, exhibiting IC50 values of 6.8 µM for GLUT4 and 11.4 µM for GLUT1. This compound has been shown to induce cell apoptosis and arrest the cell cycle at the G0/G1 phase, highlighting its potential as an anticancer agent. GLUT4-IN-2 is suitable for research applications aimed at understanding glucose metabolism and evaluating therapeutic strategies in cancer biology. -
Phospholipase A2 Inhibitor
OBAA is a potent inhibitor of phospholipase A2 (PLA2), exhibiting an IC50 of 70 nM. This compound effectively blocks Melittin-induced calcium influx in Trypanosoma brucei, demonstrating an IC50 of 0.4 μM. OBAA is valuable for research applications aimed at understanding the role of PLA2 in various biological processes and cellular responses. -
IDO-1/NS2B-NS3 Inhibitor
Palmatine hydroxide is an irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1) with IC50 values of 3 μM and 157 μM against HEK 293-hIDO-1 and rhIDO-1, respectively. This compound also exhibits uncompetitive inhibition of the West Nile virus NS2B-NS3 protease with an IC50 of 96 μM. Palmatine hydroxide demonstrates a wide range of biological activities, including anti-cancer, anti-oxidation, anti-inflammatory, neuroprotective, antibacterial, and antiviral effects, making it a valuable tool for research in cancer therapy, viral infections, and oxidative stress-related studies. -
PAI-1 Inhibitor
MDI-2268 is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), a crucial regulator of coagulation and fibrinolysis. By enhancing fibrinolytic activity, MDI-2268 exhibits significant antithrombotic properties, making it a valuable tool for studying blood coagulation dynamics. This compound is particularly relevant in research related to conditions such as deep vein thrombosis and other thromboembolic disorders. -
Fatty Acid Synthase (FASN) Inhibitor
trans-Chalcone is an effective inhibitor of fatty acid synthase (FASN) and α-amylase, offering significant potential in metabolic research. Isolated from the skin of Aronia melanocarpa, this biphenolic compound induces cell cycle arrest and apoptosis in the MCF-7 breast cancer cell line, demonstrating its utility in cancer studies. Additionally, trans-Chalcone exhibits antifungal properties, making it applicable in studies of both cancer and microbial pathogenicity. -
ALDH Inhibitor
KS106 is a selective inhibitor of aldehyde dehydrogenase (ALDH), demonstrating IC50 values of 334 nM for ALDH1A1, 2137 nM for ALDH2, and 360 nM for ALDH3A1. This compound exhibits significant antiproliferative and anticancer properties while maintaining low toxicity. KS106 effectively increases reactive oxygen species (ROS) levels, enhances lipid peroxidation, and leads to the accumulation of toxic aldehydes. Furthermore, it promotes apoptosis and induces cell cycle arrest at the G2/M phase, making it a valuable tool for cancer research and therapeutic studies. -
hCE1 Inhibitor
Nevadensin is a selective inhibitor of human carboxylesterase 1 (hCE1), exhibiting an IC50 value of 2.64 μM, while demonstrating significantly lower selectivity for hCE2 (IC50 of 132.8 μM). This natural flavonoid has been shown to induce apoptosis and DNA damage in cancer cells, indicating its potential for therapeutic applications in oncology. Additionally, Nevadensin displays a range of bioactivities, including anti-inflammatory, anti-tumor, anti-hypertensive, anti-tubercular, antitussive, antioxidant, and anti-microbial effects, making it a valuable agent for various research investigations. -
ALDH Inhibitor
KS100 is a potent inhibitor of aldehyde dehydrogenase (ALDH), demonstrating IC50 values of 230 nM for ALDH1A1, 1542 nM for ALDH2, and 193 nM for ALDH3A1. This compound exhibits significant antiproliferative and anticancer effects with minimal toxicity. KS100's mechanism includes the induction of reactive oxygen species (ROS), lipid peroxidation, and accumulation of toxic aldehydes. Additionally, it triggers apoptosis and causes cell cycle arrest at the G2/M phase, making it a valuable tool for cancer research. -
SCD Inhibitor
CVT-11127 is a potent inhibitor of stearoyl-CoA desaturase (SCD), which plays a crucial role in lipid metabolism. This compound induces apoptosis and causes cell cycle arrest at the G1/S phase, which may impact cellular proliferation. CVT-11127 is primarily utilized in research related to lung cancer, providing valuable insights into therapeutic strategies targeting SCD pathways. -
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. -
PKM2 Inhibitor
Vitamin K5 hydrochloride is a specific inhibitor of pyruvate kinase M2 (PKM2), with reported IC50 values of 28, 191, and 120 μM for PKM2, PKM1, and PKL, respectively. This compound exhibits significant biological activity by inducing apoptosis in colon 26 cancer cells, making it relevant for cancer research. Additionally, Vitamin K5 hydrochloride serves as a photosensitizer and antimicrobial agent, and it is applicable in the study of infections as well as a potential preservative in pharmaceuticals, foods, and beverages. -
PPARγ Inhibitor
Soyasaponin Ab is a potent PPARγ inhibitor with oral bioavailability. It effectively suppresses PPARγ transcriptional activity and induces apoptosis at elevated concentrations. This compound exhibits a range of biological activities, including anti-obesity, anti-oxidation, anti-inflammation, and anti-aging effects. Additionally, Soyasaponin Ab has been shown to mitigate memory impairment induced by Scopolamine, making it a valuable reagent for research in metabolic and neuroprotective applications. -
PDEIII Inhibitor
Anagrelide is a potent phosphodiesterase type III (PDE3) inhibitor with an IC50 of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and attenuates megakaryocytopoiesis in the bone marrow. Additionally, Anagrelide demonstrates the capacity to reduce proliferation and promote apoptosis in gastrointestinal stromal tumor (GIST) cells in vitro. Its primary application includes functioning as a platelet-lowering agent with significant antithrombopoietic properties. -
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. -
MitoNEET Agonist /MAO-B Inhibitor
TT01001 is a selective and orally active mitoNEET agonist and monoamine oxidase B (MAO-B) inhibitor, with an IC50 of 8.84 μM. It functions by preventing mitoNEET-mediated mitochondrial dysfunction, thus attenuating oxidative stress and neuronal apoptosis. TT01001 has demonstrated potential in improving type II diabetes and enhancing mitochondrial function in murine models. This compound is suitable for research focused on type II diabetes and neurological disorders. -
Cathepsin L/JAK Inhibitor
Dual Cathepsin L/JAK-IN-1 is a dual inhibitor targeting Cathepsin L (CTSL) and Janus kinases (JAK), exhibiting IC50 values of 0.68 μM for CTSL, 337.1 nM for JAK1, 5.251 nM for JAK2, 27.29 nM for JAK3, and 172.6 nM for TYK2. This compound effectively inhibits the activation of key signaling pathways, including MAPK, NF-κB, and JAK/STAT, thereby providing substantial anti-inflammatory effects. Dual Cathepsin L/JAK-IN-1 is useful for investigating mechanisms underlying acute lung injury (ALI) and other inflammatory conditions. -
FGFR/CYP Inhibitor
FGFR-IN-10 is an orally bioactive inhibitor targeting fibroblast growth factor receptors (FGFR) and various cytochrome P450 enzymes (CYPs). It demonstrates significant potency against both wild type and V564F mutant FGFR2, with IC50 values of 104.1 nM and 43.6 nM, respectively. Additionally, FGFR-IN-10 inhibits CYP enzymes, including CYP2C9 (IC50: 3.33 µM), CYP2C19 (IC50: 18.75 µM), CYP2D6 (IC50: 4.34 µM), and CYP3A4 (IC50: 0.69 µM). This compound is valuable for researching FGFR-related signaling pathways and the pharmacokinetics of drug metabolism. -
HSP Synthesis Inhibitor
KNK423 is a specific inhibitor of heat shock protein (HSP) synthesis, targeting HSP70. This compound enhances the efficacy of Amphotericin B against resistant strains of Aspergillus terreus by disrupting HSP expression. KNK423 is valuable for research in cancer therapy and bacterial infection mechanisms. -
FKBP51-Hsp90 Interaction Inhibitor
FKBP51-Hsp90-IN-1 is a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, exhibiting an IC50 value of 0.1 μM against FKBP51. This compound is valuable for research into stress-related diseases, Alzheimer's disease, and various metabolic disorders, owing to its ability to modulate protein interactions critical for cellular stress responses and stability. Its specificity makes it a potent tool for elucidating the role of FKBP51 in disease mechanisms. -
HSP90 Inhibitor
HSP90-IN-20 is a potent inhibitor of Heat Shock Protein 90 (HSP90) with an IC50 of ≤10 μM. This compound plays a significant role in cancer research by impeding the function of HSP90, which is critical for the stability and activity of several oncogenic proteins. HSP90-IN-20 can be utilized to investigate the therapeutic potential of HSP90 inhibition in various cancer models. -
HSP90 Inhibitor
Hsp90-IN-17 is a selective inhibitor of Heat Shock Protein 90 (HSP90) that interferes with its chaperone activity. This compound demonstrates significant potential in addressing various proliferative conditions, including cancer and neurodegenerative disorders. Hsp90-IN-17 serves as a valuable tool for research focused on the molecular mechanisms of HSP90 and its role in disease progression and treatment responses. -
HSP90 Inhibitor
Aminohexylgeldanamycin hydrochloride is a potent inhibitor of Heat Shock Protein 90 (HSP90). This Geldanamycin derivative demonstrates significant antiangiogenic and antitumor activities, making it valuable for cancer research. Its ability to modulate HSP90 function provides insights into the molecular mechanisms of tumorigenesis and offers potential therapeutic applications in oncology. -
SIRT2/Hsp70 Inhibitor
YM-08 is a selective inhibitor of SIRT2 and Hsp70, exhibiting an IC50 of 19.9 μM for SIRT2. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases and cellular stress responses. Its dual inhibitory activity allows for investigation into SIRT2 and Hsp70's roles in various biological processes and potential therapeutic applications. -
HSP70 Inhibitor
DMT003096 is a selective inhibitor of HSP70, a heat shock protein that plays a critical role in cellular stress responses. Its upregulation has been associated with various cancers, including breast, lung, colon, and cervical cancer. This compound is valuable for research applications targeting cancer therapies and investigating the role of HSP70 in tumor progression and survival mechanisms.
