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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
FAAH Inhibitor
N-Benzyllinolenamide is a natural macamide derived from Lepidium meyenii and acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 value of 41.8 μM. This compound is valuable for studying the modulation of endocannabinoid signaling pathways and investigating the role of FAAH in various physiological processes. Its ability to inhibit FAAH makes it a useful tool in research related to pain management, inflammation, and neuroprotection. -
HMG-CoA Reductase Inhibitor
(3R,5S)-Fluvastatin sodium is a potent competitive inhibitor of HMG-CoA reductase, displaying an IC50 value of 8 nM. This compound is effective in modulating lipid levels and exhibits protective effects on vascular smooth muscle cells by activating the Nrf2-dependent antioxidant pathway, mitigating oxidative stress. It is widely utilized in cardiovascular research and studies focusing on cholesterol metabolism and oxidative stress responses. -
HMG-CoA Reductase Inhibitor
(3R,5R)-Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 value of 11 nM. This compound is known for its ability to significantly reduce levels of low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein. Additionally, (3R,5R)-Rosuvastatin has been shown to inhibit human ether-a-go-go related gene (hERG) currents with an IC50 of 195 nM, impacting hERG protein expression and its interactions with heat shock protein 70 (Hsp70). Its pharmacological profile makes it valuable for research related to cholesterol management and cardiovascular health. -
HMG-CoA Reductase Inhibitor
(3S,5R)-Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 of 11 nM. This agent plays a significant role in reducing low-density lipoprotein (LDL) cholesterol and triglyceride levels while decreasing C-reactive protein levels. Additionally, (3S,5R)-Rosuvastatin inhibits the hERG channel with an IC50 of 195 nM and modulates the expression of the hERG protein through the disruption of its interaction with heat shock protein 70 (Hsp70). This compound is valuable in cardiovascular research and studies focused on cholesterol metabolism. -
HMG-CoA Reductase Inhibitor
(3S,5R)-Fluvastatin-d6 is a deuterium-labeled derivative of the HMG-CoA reductase inhibitor, Fluvastatin. As a competitive inhibitor with an IC50 of 8 nM, it effectively regulates cholesterol biosynthesis. This compound has been shown to protect vascular smooth muscle cells from oxidative stress via the Nrf2-dependent antioxidant pathway, making it a valuable tool in cardiovascular research and studies focused on oxidative damage and cellular stress responses. -
CYP2C9/CYP3A4 Inhibitor
Tetrahydrocurcumin-d6 is a deuterated analog of Tetrahydrocurcumin, functioning as an inhibitor of CYP2C9 and CYP3A4 enzymes. This compound exhibits significant biological activity against these cytochrome P450 isoforms, making it valuable for research into drug metabolism and pharmacokinetics. Tetrahydrocurcumin-d6 is utilized in studies aiming to elucidate the metabolic pathways and interactions of curcuminoids, as well as their potential therapeutic applications. -
HMG-CoA Reductase Inhibitor
Atorvastatin strontium is an HMG-CoA reductase inhibitor that effectively lowers cholesterol levels, impacting cardiovascular health. Its primary mechanism involves the inhibition of HMG-CoA reductase in liver tissue, which plays a crucial role in cholesterol synthesis. This compound is also utilized in research to address dyslipidemia and related metabolic disorders. -
FAAH Inhibitor
SA72 is a highly selective inhibitor of fatty acid amide hydrolase (FAAH), an enzyme crucial for the degradation of endocannabinoids. By inhibiting FAAH, SA72 modulates endocannabinoid levels, leading to potential therapeutic effects in pain management and inflammation. This compound serves as a valuable tool in research aimed at understanding the endocannabinoid system and its role in various physiological processes. -
Cathepsin G Inhibitor
Cathepsin G Inhibitor I is a potent and selective reversible competitive inhibitor of Cathepsin G, exhibiting an IC50 value of 53 nM and a Ki of 63 nM. This non-peptidic compound is primarily utilized in research investigating immune disorders, providing valuable insights into the role of Cathepsin G in various pathogenic processes. Its specificity makes it a useful tool for understanding the implications of Cathepsin G in immune system regulation. -
Cathepsin L Inhibitor
Cathepsin L-IN-2 is a selective inhibitor of Cathepsin L, exhibiting an IC50 of 15 μM. This compound irreversibly inhibits the proteolytic activity of cathepsins by covalently binding to cysteine residues in the enzyme's active site. Cathepsin L-IN-2 is primarily utilized in research focused on neurodegenerative diseases, including GRN-related frontotemporal dementia, as well as in studies investigating cancer invasion and metastasis. -
Calpain/Cathepsin Inhibitor
ALLM, also known as Calpain inhibitor II, acts as a potent inhibitor of calpain and cathepsin proteases. This compound is known to mitigate neuronal cell death, thereby enhancing chronic neurological function following spinal cord injury (SCI). Its utility in research extends to studies investigating protease activity and the mechanisms underlying neuroprotection in trauma-related conditions. -
Cathepsin X Inhibitor
Cathepsin X-IN-1 is a potent inhibitor of Cathepsin X, exhibiting an IC50 of 7.13 µM. This compound effectively reduces PC-3 cell migration while demonstrating low cytotoxicity. It serves as a valuable tool in cancer research, particularly in studies focused on metastatic processes and the modulation of proteolytic enzymes. -
Cysteine Cathepsin Inhibitor
JPM-OEt is a potent cysteine cathepsin inhibitor that binds covalently to the active site, irreversibly inhibiting the cysteine cathepsin family. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate cysteine cathepsins expands its potential applications in studying various pathophysiological processes and therapeutic interventions. -
Cathepsin Inhibitor
Aurantiamide acetate is a selective and orally active inhibitor of cathepsins, derived from the plant Portulaca oleracea L. This compound exhibits significant anti-inflammatory properties, making it valuable for investigating the mechanisms underlying inflammatory diseases. Researchers can utilize aurantiamide acetate to explore therapeutic strategies aimed at modulating cathepsin activity in various pathological conditions. -
Cathepsin L Inhibitor
KGP94 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 189 nM. This compound effectively inhibits the migration and invasion of metastatic carcinoma while demonstrating low cytotoxicity with a GI50 of 26.9 µM across various human cell lines. KGP94 is suitable for research applications focused on cancer biology and the modulation of proteolytic enzyme activity.
