Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
PAI-1 inhibitor
Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling. -
ACE inhibitor
Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase. -
hCA II inhibitor
EMAC10101d is a potent and selective inhibitor of Carbonic Anhydrase Isoform toward hCA II with an inhibitory activity in the low nanomolar range. Ki of 8.1 nM -
PDE4 inhibitor
Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM. -
ACLY inhibitor
NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. -
CRM1-selective inhibitor
Selinexor trans-isomer is a trans-isomer of Selinexor or KPT-330, which is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells. -
Potassium Channel inhibitor
Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. -
α-glucosidase inhibitor
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. -
sEH inhibitor
1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. -
α-glucosidase inhibitory activities
Tangshenoside I, isolated from the roots of Codonopsis lanceolata, exhibits weak α-glucosidase inhibitory activities in vitro with an IC50 of 1.4 mM. -
5-LO Inhibitor
EP6 is a selective 5-Lipoxygenase (5-LO) inhibitor that exhibits potent anti-tumor activity. It effectively reduces the viability of various tumor cell lines while demonstrating a lack of mutagenic properties. This compound is valuable for research applications focused on cancer therapy and the modulation of inflammatory pathways. -
IDH1 Inhibitor
GSK321 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), showing IC50 values of 2.9, 3.8, 4.6, and 46 nM for the R132G, R132C, R132H, and wild-type IDH1 variants, respectively, with over 100-fold selectivity for IDH2. This compound effectively reduces intracellular levels of α-Hydroxyglutaric acid (2-HG), disrupts the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. GSK321 is valuable for research on acute myeloid leukemia (AML) and various other malignancies. -
SIRT Inhibitor
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
Topoisomerase IV Inhibitor
Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology. -
Phospholipase C Inhibitor, Angiogenesis Modulator
Neomycin sulfate is a phospholipase C inhibitor that modulates angiogenesis through its influence on calcium signaling pathways. This aminoglycoside antibiotic disrupts bacterial protein synthesis by binding irreversibly to the 30S ribosomal subunit. In addition to its antibacterial properties, neomycin sulfate effectively inhibits angiogenin-mediated nuclear translocation, cell proliferation, and angiogenesis. It also disrupts inositol trisphosphate (IP3)-mediated calcium release and electrical excitation-evoked calcium transients in skeletal muscle. Neomycin sulfate is utilized in cancer research and studies related to calcium signaling and angiogenesis. -
Carbonic Anhydrase Inhibitor
Methazolamide is an orally active inhibitor of carbonic anhydrase, demonstrating a Ki of 14 nM for human carbonic anhydrase II. This compound effectively reduces intraocular pressure and exhibits neuroprotective properties, including the ability to inhibit neuronal apoptosis. Methazolamide is applicable in research concerning ophthalmic diseases, such as glaucoma, and cerebrovascular conditions, including subarachnoid hemorrhage. -
COX2 Inhibitor
Iminostilbene is a well-characterized inhibitor of COX2 (Cyclooxygenase-2) with additional activity against PKM2 (Pyruvate Kinase M2). This compound effectively reduces the expression of COX2 and iNOS, as well as the release of pro-inflammatory cytokines such as IL-1β, IL-6, TNF-α, and MCP-1 in macrophages. Its ability to mitigate macrophage-mediated inflammatory responses makes iminostilbene a valuable reagent for investigating mechanisms of inflammation regulation, cardiovascular disease, including myocardial ischemia/reperfusion injury, and immune-related disorders. -
GARFT Inhibitor
Lometrexol, a potent GARFT inhibitor, effectively blocks glycinamide ribonucleotide formyltransferase activity, thereby disrupting de novo purine synthesis. This inhibition leads to abnormal cell proliferation, apoptosis, and potential cell cycle arrest, demonstrating its anticancer properties. Additionally, Lometrexol acts as an inhibitor of human serine hydroxymethyltransferase 1 and 2 (hSHMT1/2), further influencing metabolic processes in cancer research applications. -
HSP90 Inhibitor
Kongensin A is a covalent inhibitor of the heat shock protein 90 (HSP90), isolated from the plant Croton kongensis. This natural product effectively inhibits RIP3-dependent necroptosis while also inducing apoptosis. Kongensin A demonstrates significant potential in research applications focused on necroptosis and inflammation, making it a valuable tool for investigating cellular death pathways and therapeutic strategies. -
Nampt Inhibitor
OT-82 is a selective, orally active inhibitor of Nicotinamide Adenine Dinucleotide Phosphate (NAMPT). It exhibits potent cytotoxicity specifically towards hematopoietic cells and induces cell death in a NAD+ dependent manner. Due to these properties, OT-82 shows potential as an innovative antineoplastic agent for investigating hematological malignancies. -
Cathepsin B Inhibitor
(Rac)-Z-FA-FMK is a potent inhibitor of cathepsin B, exhibiting a Ki value of 1.5 μM. This compound also inhibits multiple caspases, specifically caspases 2, 3, 6, 7, and 9, with IC50 values ranging from 6.147 to 110.7 μM. Additionally, (Rac)-Z-FA-FMK demonstrates antiviral activity by inhibiting the main protease involved in SARS-CoV-2 replication with an IC50 of 11.39 μM. It further attenuates the increase in IL-1β levels induced by LPS and represses NF-κB transactivation in macrophages, making it useful for research in inflammation and viral pathogenesis. -
Hsp90 Inhibitor
GUT-70 is a tricyclic coumarin that functions as a potent Hsp90 inhibitor. It activates caspases 2, 3, 8, and 9, leading to apoptosis in leukemic cells. Additionally, GUT-70 effectively inhibits HIV-1 replication in chronically infected cells by targeting the NF-κB signaling pathway. This compound is suitable for research applications involving leukemia, mantle cell lymphoma (MCL), and HIV-1 infection studies. -
PFKFB4 Inhibitor
PFKFB4-IN-1 is a selective ATP-competitive inhibitor of PFKFB4, demonstrating an IC50 of 4.50 μM and over 12-fold selectivity against PFKFB1/4 and PFKFB3/4. This compound effectively reduces intracellular PFKFB4 protein levels and exhibits significant anti-cancer activities, including the inhibition of cell proliferation, induction of apoptosis, and suppression of cell migration. PFKFB4-IN-1 has shown efficacy in vivo, effectively inhibiting tumor growth in the MDA-MB-231 xenograft mouse model, making it a valuable tool for research in breast, lung, and liver cancer. -
PCSK9 Inhibitor
Inclisiran is a double-stranded small interfering RNA (siRNA) that specifically targets and inhibits the transcription of proprotein convertase subtilisin/kexin type 9 (PCSK9). By reducing PCSK9 levels, Inclisiran effectively modulates lipid metabolism and demonstrates anti-inflammatory properties, including the inhibition of pyroptosis and a decrease in NLRP3, cleaved caspase-1, IL-1β, and IL-18. This reagent is valuable for research applications focused on hyperlipidemia and cardiovascular diseases (CVD), as it supports studies aimed at understanding lipid regulation and atherosclerosis. -
15-lipoxygenase Inhibitor
4-MMPB is a selective inhibitor of 15-lipoxygenase, exhibiting an IC50 of 18 μM. It demonstrates competitive inhibition with IC50 values of 19.5 μM for soybean 15-lipoxygenase and 19.1 μM for human 15-lipoxygenase-1. This compound may hold promise for research applications focused on prostate cancer, providing insights into the role of 15-lipoxygenase in tumor biology. -
HMG-CoA Reductase Inhibitor
Pitavastatin sodium is a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase, significantly reducing cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. This compound serves as an effective inducer of low-density lipoprotein-cholesterol (LDL-C) receptors in hepatocytes. In addition to its primary role in cholesterol regulation, pitavastatin sodium exhibits various biological activities, including anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective, and reno-protective effects, making it valuable for diverse research applications in lipid metabolism and disease. -
IDO1/TrxR1 Inhibitor
ZC0109 is a potent dual inhibitor targeting indoleamine 2,3-dioxygenase 1 (IDO1) and thioredoxin reductase 1 (TrxR1), exhibiting IC50 values of 50 nM and 3.0 μM, respectively. This compound is effective in inducing reactive oxygen species (ROS) accumulation and causing cell cycle arrest at the G1/S phase, ultimately leading to apoptosis in cancer cells. ZC0109 is a valuable reagent for research applications focused on cancer therapy and the modulation of immune response through IDO1 and TrxR1 inhibition. -
5-Lipoxygenase Inhibitor
CNB-001 is a potent inhibitor of 5-lipoxygenase (5-LOX), demonstrating strong oral bioavailability. This compound effectively reduces 5-LOX expression and enhances proteasome activity, leading to the inhibition of soluble Amyloid-β accumulation and ubiquitinated protein aggregates. It also exhibits neuroprotective properties by inhibiting apoptosis and reactive oxygen species (ROS) production while stabilizing mitochondrial membrane potential. Additionally, CNB-001 addresses insulin resistance and enhances glucose uptake, making it valuable for research into inflammation, neurological disorders, and metabolic diseases such as Alzheimer's disease, stroke, and diabetes. -
CypA Inhibitor
HL001 is an oral small molecule inhibitor targeting Cyclophilin A (CypA) and acting as a receptor antagonist for Lysophosphatidic acid 1 (LPA1). This compound induces cell cycle arrest and apoptosis in tumor cells via p53 stabilization, achieved by down-regulating G3BP1 and promoting reactive oxygen species production and DNA damage. HL001 disrupts the MDM2-p53-72R interaction in a CypA-dependent manner, demonstrating significant antitumor activity. Additionally, HL001 serves as a valuable tool in the investigation of pulmonary fibrosis. -
Cathepsin Inhibitor
TS-24 is a selective inhibitor of cathepsin S, demonstrating an IC50 value of 4.3 μM. This compound has been shown to exhibit radiosensitizing effects in wild-type BRCA1 and triple-negative breast cancer (TNBC) xenograft models, primarily by inducing apoptotic pathways. TS-24 is suitable for research applications focused on cancer therapeutic development and understanding cathepsin-mediated biological processes. -
α-Glucosidase Inhibitor
Malabaricone B is a naturally occurring phenolic compound that functions as an α-glucosidase inhibitor, exhibiting an IC50 of 63.7 µM. This compound demonstrates significant biological activities, including anticancer, antimicrobial, antioxidant, and antidiabetic effects. It is suitable for research applications focused on metabolic regulation and the investigation of glycemic control. -
Phospholipase A2 Inhibitor
(2E)-OBAA is a selective inhibitor of phospholipase A2 (PLA2) with an IC50 value of 70 nM. This compound effectively induces apoptosis in human umbilical vein endothelial cells (HUVECs) and demonstrates its capacity to inhibit melittin-induced Ca2+ influx in Trypanosoma brucei, exhibiting an IC50 of 0.4 μM. (2E)-OBAA is valuable for research focused on cell signaling, apoptosis, and parasitology. -
Phospholipase D Inhibitor
PLD-IN-1 is a selective inhibitor of phospholipase D, exhibiting an IC50 of 1.97 μM. This compound reduces the expression of immune evasion markers such as CD24, CD47, and PD-L1 while promoting calreticulin, thereby enhancing phagocytosis of lung cancer cells by macrophages. PLD-IN-1 demonstrates significant cytotoxic effects on various lung cancer cell lines, including A549, HCC44, H460, and HCC15, with IC50 values ranging from 18.44 to 24.85 μM. Additionally, it induces apoptosis, inhibits cell migration, enhances M1 macrophage polarization, and exhibits antitumor efficacy in mouse models, making it a valuable tool for cancer research. -
IDO-1/NS2B-NS3 Inhibitor
Palmatine is a selective, irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1), exhibiting IC50 values of 3 μM against HEK 293-hIDO-1 and 157 μM against rhIDO-1. Additionally, Palmatine effectively inhibits the West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. This compound demonstrates diverse biological activities including anti-cancer, anti-oxidation, anti-inflammatory, neuroprotective, antibacterial, and antiviral effects, making it a valuable tool for research in cancer biology, inflammation, and infectious diseases. -
Enpp/Carbonic Anhydrase Inhibitor
Enpp/Carbonic Anhydrase-IN-1 is a potent inhibitor of ecto-nucleotide triphosphate diphosphohydrolase (ENPP) and carbonic anhydrase, exhibiting IC50 values of 1.36 μM for NPP1, 1.35 μM for NPP2, 3.00 μM for NPP3, 0.88 μM for CA-II, and 1.02 μM for CA-IX. This compound demonstrates significant antiproliferative effects on cancer cells while displaying low cytotoxicity to normal cells. Additionally, Enpp/Carbonic Anhydrase-IN-1 has been shown to induce apoptosis, making it a valuable tool for cancer research and therapeutic investigations. -
Carbonic Anhydrase Inhibitor
Zonisamide sodium is a potent carbonic anhydrase inhibitor, effectively targeting hCA II and hCA V with Kis of 35.2 nM and 20.6 nM, respectively. This compound exhibits neuroprotective properties by promoting anti-apoptotic mechanisms and enhancing the expression of manganese superoxide dismutase (MnSOD). Additionally, Zonisamide sodium has been shown to upregulate Hrd1, contributing to improved cardiac function in animal models of cardiac hypertrophy. Its diverse biological activities make it suitable for investigations related to seizures, Parkinson's disease, and cardiovascular research. -
HSP90/mTOR Inhibitor
HSP90/mTOR-IN-1 is a potent inhibitor targeting both Hsp90 and mTOR, exhibiting IC50 values of 69 nM and 29 nM, respectively. This compound effectively suppresses the proliferation of SW780 cells by over-activating the PI3K/AKT/mTOR signaling pathway. In addition to inducing apoptosis and autophagy through selective inhibition, HSP90/mTOR-IN-1 demonstrates significant in vivo anti-tumor activity. It serves as a valuable reagent for research applications focused on bladder cancer. -
PAI-1 Inhibitor
TM5441 sodium is a potent inhibitor of plasminogen activator inhibitor-1 (PAI-1), demonstrating IC50 values ranging from 13.9 to 51.1 μM. It has been shown to induce intrinsic apoptosis in various human cancer cell lines, making it a valuable tool in cancer research. Additionally, TM5441 sodium mitigates cardiac hypertension and vascular senescence induced by Nω-nitro-l-arginine methyl ester, suggesting potential therapeutic applications in cardiovascular studies. -
Carbonic Anhydrase Inhibitor
hCAIX/XII-IN-5 is a selective inhibitor of carbonic anhydrases IX and XII, demonstrating Ki values of 93.9 nM and 85.7 nM, respectively. This compound exhibits notable anti-proliferative effects on cancer cells, leading to cell cycle delay and the induction of apoptosis. hCAIX/XII-IN-5 is a valuable tool for elucidating the roles of carbonic anhydrases in cancer biology and for developing targeted therapeutic strategies. -
NAMPT Inhibitor
(E/Z)-Daporinad hydrochloride is a potent inhibitor of nicotinamide phosphoribose transferase (NAMPT). By specifically targeting NAMPT, this compound induces apoptosis through the gradual depletion of intracellular NAD+. (E/Z)-Daporinad hydrochloride is utilized in research to explore mechanisms in cancer biology and inflammatory diseases. -
IDO/Tubulin Inhibitor
IDO/Tubulin-IN-2 is a potent inhibitor targeting both indoleamine 2,3-dioxygenase (IDO) and tubulin. This compound exhibits significant anticancer activity, demonstrated by its effect on various cell lines, including U87, HepG2, A549, HCT-116, and LO2, with IC50 values of 0.43, 0.036, 0.041, 0.095, and 1.04 μM, respectively. IDO/Tubulin-IN-2 is valuable for research applications in cancer biology, particularly in elucidating mechanisms of tumorigenesis and therapeutic resistance. -
PDE1 Inhibitor
PDE1-IN-6 is a selective phosphodiesterase 1 (PDE1) inhibitor with an IC50 of 7.5 nM. It effectively inhibits cell proliferation and induces apoptosis in acute myelogenous leukemia (AML) cells. This compound serves as a valuable tool in cancer research, particularly in studies focused on signaling pathways involved in leukemia progression and treatment.
