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Catalog No.
Product Name
Application
Product Information
Citations
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γ-secretase Inhibitor
ELN318463 is a selective inhibitor of γ-secretase, targeting the amyloid precursor protein (APP). It demonstrates differential inhibition of presenilin 1 (PS1) and presenilin 2 (PS2) γ-secretase complexes, with EC50 values of 12 nM and 656 nM, respectively, showcasing a 51-fold greater selectivity for PS1. This compound is primarily utilized in research focused on Alzheimer's disease and related neurodegenerative disorders, making it a valuable tool for studies investigating APP processing and amyloid plaque formation. -
γ-secretase Inhibitor
(9R)-RO7185876 is a selective inhibitor of γ-secretase, targeting the cleavage of amyloid precursor protein. This compound significantly reduces the secretion of Aβ42 peptides, making it a valuable tool for research on Alzheimer's disease and related disorders, such as cerebral amyloid angiopathy and multi-infarct dementia. Additionally, (9R)-RO7185876 may be utilized to investigate conditions associated with amyloid deposition, including dementia pugilistica and Down syndrome. -
γ-secretase Inhibitor
MK-0752 sodium is a potent, orally bioavailable inhibitor of γ-secretase, exhibiting a dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. This compound effectively crosses the blood-brain barrier and demonstrates the ability to decrease newly generated central nervous system Aβ levels in vivo. MK-0752 sodium is primarily utilized in research on Alzheimer’s disease and other neurodegenerative disorders linked to amyloid-beta pathology. -
γ-secretase Inhibitor
γ-Secretase modulator 11 functions as a potent γ-secretase inhibitor, effectively reducing levels of amyloid beta 42 in vitro and demonstrating significant brain penetration. This compound exhibits minimal inhibition of cytochrome P450 enzymes, highlighting its selective profile. Additionally, γ-secretase modulator 11 has shown considerable efficacy in alleviating cognitive deficits in Alzheimer's disease model mice, making it a valuable tool for research in neurodegenerative disorders. -
γ-Secretase Inhibitor
GSI-18 is a potent γ-secretase inhibitor that disrupts Notch signaling, contributing to its anticancer properties. This compound effectively inhibits the attachment-free growth of pancreatic cancer cells, making it valuable for research into cancer biology and therapeutic interventions. Its mechanism of action offers insights into the regulation of cell proliferation and differentiation in oncogenic contexts. -
γ-secretase Inhibitor
ELND 007 is a selective γ-secretase inhibitor that primarily targets the reduction of amyloid beta (Aβ) generation while minimizing inhibition of Notch signaling. It demonstrates significant biological activity in both in vitro and in vivo settings, effectively decreasing Aβ levels. This compound has shown potential therapeutic benefits for Alzheimer’s disease, particularly as evidenced by reductions in Aβ levels observed in cerebrospinal fluid during human clinical trials, following a strategic emphasis on metabolic stability and chirality in its development. -
γ-secretase Inhibitor
γ-Secretase-IN-2 is a potent inhibitor of γ-secretase, demonstrating an IC50 of 0.06 nM. This compound is instrumental in researching Alzheimer's disease, providing insights into the enzymatic processes involved in neurodegeneration. Its high efficacy makes it a valuable tool for studying the pathophysiology of Alzheimer's and exploring potential therapeutic strategies. -
γ-secretase Inhibitor
LY3056480 is a potent γ-secretase inhibitor that targets Notch signaling pathways. This compound has demonstrated efficacy in enhancing recovery from mild to moderate sensorineural hearing loss, while exhibiting a favorable safety profile. Additionally, intratympanic administration of LY3056480 has been shown to promote hair cell regeneration and contribute to partial auditory recovery in mammalian models, making it a valuable tool for research in hearing restoration and neurodegenerative studies. -
γ-secretase Inhibitor
III-31-C is a hydroxyethyl urea-based inhibitor of γ-secretase. It demonstrates potent inhibition of amyloid-beta (Aβ) production, with an IC50 value of 10 nM in a cell-free γ-secretase assay and 200 nM in APP-transfected cells. This compound is relevant for research focused on Alzheimer's disease and offers valuable insights into the modulation of Aβ metabolism. -
γ-secretase Inhibitor
LY-411575 (isomer 2) is a potent inhibitor of γ-secretase, an enzyme involved in the cleavage of amyloid precursor protein and a key player in the pathogenesis of Alzheimer's disease. This compound has been shown to effectively reduce the production of amyloid-beta peptides, making it valuable for research into therapeutic strategies for neurodegenerative disorders. Its selective inhibition of γ-secretase also facilitates the study of its role in cellular signaling and development. -
γ-secretase Inhibitor
GSI-136 is a potent inhibitor of γ-secretase, exhibiting an IC50 of 3 nM. This compound effectively reduces Aβ40 levels in diethylamine-extracted brain homogenates from C57BL/6 mice in a dose-dependent manner. GSI-136 serves as a valuable tool in medicinal chemistry and Alzheimer’s disease research, aiding in the exploration of therapeutic strategies targeting amyloid-beta production. -
γ-secretase Inhibitor
LY-411575 (isomer 3) is a potent inhibitor of γ-secretase, an enzyme complex involved in the proteolytic processing of various transmembrane proteins, including amyloid precursor protein (APP). This compound is utilized in research studying Alzheimer's disease and other conditions associated with aberrant Notch signaling. Its ability to modulate γ-secretase activity makes it a valuable tool for investigating the therapeutic potential of targeting this pathway. -
γ-secretase Inhibitor
ELN318463 racemate is a selective γ-secretase inhibitor targeting the amyloid precursor protein (APP). It demonstrates differential inhibition of presenilin (PS1) and PS2-comprised γ-secretase, with EC50 values of 12 nM for PS1 and 656 nM for PS2, indicating a 51-fold selectivity for PS1. This compound is useful in research applications focused on Alzheimer's disease and the modulation of amyloid beta peptide production. -
PTPN1/PTPN2 Inhibitor
Osunprotafib hydrochloride is a selective inhibitor of protein tyrosine phosphatases PTPN1 and PTPN2, exhibiting IC50 values of 2.5 nM and 1.8 nM, respectively. This compound demonstrates significantly reduced activity against PTPN9 and no activity on SHP-1 or SHP-2. Osunprotafib hydrochloride enhances the sensitivity of human cancer cell lines to interferon-gamma (IFNγ) and promotes robust anti-tumor immunity through the activation of JAK-STAT signaling pathways while mitigating T cell dysfunction. This makes it a valuable reagent for research into cancer immunotherapy and signaling modulation. -
Thrombin Inhibitor
Isorhamnetin 3-O-galactoside is a flavonoid glycoside that acts as a thrombin inhibitor, isolated from Oenanthe javanica. It exhibits significant antithrombotic and profibrinolytic properties by inhibiting thrombin and factor Xa activity, thereby reducing the maximum rate of thrombin-catalyzed fibrin polymerization. Additionally, Isorhamnetin 3-O-galactoside suppresses TNF-α-induced PAI-1 secretion and decreases the PAI-1/tissue-type plasminogen activator (t-PA) ratio, making it instrumental in research on liver injury and thrombotic vascular diseases. -
Proteasome Inhibitor
CEP1612 is a dipeptidyl proteasome inhibitor that exhibits an IC50 of 60 nM. This compound induces the expression of cell cycle regulators p21(WAF1) and p27(KIP1), leading to enhanced apoptotic activity in cancer cells. Due to its ability to disrupt proteasomal degradation, CEP1612 demonstrates significant anticancer efficacy in vivo, making it a valuable tool for research into cancer therapeutics. -
Aldose Reductase Inhibitor
APPA is an aldose reductase inhibitor that functions by disrupting the polyol pathway, thereby preventing apoptosis associated with diabetic conditions. In preclinical studies, APPA has demonstrated efficacy in alleviating symptoms related to Streptozotocin-induced diabetes in rat models. This compound shows promise for research applications in diabetic nephropathy (DN), offering insights into potential therapeutic strategies. -
γ-secretase Inhibitor
MRK 003 is a selective and orally bioavailable inhibitor of γ-secretase. It demonstrates significant reduction of Aβ peptide production in the brain in vivo, making it a valuable tool for Alzheimer's disease research. Additionally, MRK 003 induces caspase-dependent apoptosis and inhibits tumor cell proliferation both in vitro and in vivo, supporting its potential applications in cancer research. -
Proteasome Inhibitor
NIC-0102 is an orally active proteasome inhibitor that specifically targets NLRP3 inflammatory vesicle activation, exhibiting a pIC50 of 7.55. This compound demonstrates significant anti-inflammatory effects in models of dextran sulfate sodium (DSS)-induced ulcerative colitis. Additionally, NIC-0102 is effective in inhibiting the production of pro-IL-1β, making it a valuable tool for research in inflammation and related pathways. -
Proteasome Inhibitor
UR238 is a potent proteasome inhibitor that decreases the levels of the immunomodulatory protein HE4. Additionally, UR238 effectively reduces PDL1 expression on various cell types. Its anticancer properties make it a valuable reagent for research focusing on epithelial ovarian cancer. -
DHODH Inhibitor
Vidofludimus hemicalcium is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH) and a novel modulator of the farnesoid X receptor (FXR). This compound exhibits immunomodulatory properties, making it a valuable tool for investigating autoimmune disorders, including inflammatory bowel disease (IBD). Additionally, Vidofludimus hemicalcium is relevant for research in hepatic lipid metabolism and fatty liver disease due to its targeting of FXR. -
DHODH Inhibitor
DHODH-IN-17 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), with an IC50 value of 0.40 μM. This compound is pivotal for studying the metabolic pathways involved in acute myeloid leukemia (AML) and may aid in the development of targeted therapies for this condition. Its ability to inhibit DHODH highlights its potential use in cancer research, particularly in understanding tumor metabolism and proliferation. -
DHODH Inhibitor
DHODH-IN-23 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), a key enzyme in the de novo pyrimidine synthesis pathway. This compound exhibits significant biological activity in cancer research, facilitating the exploration of metabolic pathways and their implications in tumorigenesis. DHODH-IN-23 serves as a valuable tool for studies aiming to elucidate the role of pyrimidine metabolism in cancer cell proliferation and survival. -
hDHODH Inhibitor
hDHODH-IN-13 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH), with an IC50 value of 173.4 nM. This compound demonstrates significant potential in the investigation of inflammatory bowel disease (IBD) by modulating pyrimidine biosynthesis. hDHODH-IN-13 is a valuable tool for exploring therapeutic strategies targeting hDHODH in various disease models. -
DHODH Inhibitor
(E/Z)-Ginkgolic acid C17:2 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), a key enzyme in the de novo pyrimidine biosynthesis pathway. This compound, derived from Ginkgo biloba, demonstrates the ability to bind tightly to the target enzyme, mediating its biological activity. Its inhibitory effect on DHODH makes it a valuable reagent for studying cellular proliferation, autoimmune diseases, and potential anti-cancer strategies. -
hDHODH Inhibitor
hDHODH-IN-8 is a selective inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibiting an IC50 value of 16 nM. This compound demonstrates significant antiproliferative effects and possesses excellent solubility in aqueous solutions. hDHODH-IN-8 is particularly relevant for research exploring tumorigenesis, with potential implications in lymphoma studies. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-1 is a dual inhibitor targeting retinoic acid receptor-related orphan receptor gamma t (RORγt) and dihydroorotate dehydrogenase (DHODH). With IC50 values of 0.083 μM for RORγt and 0.172 μM for DHODH, this compound demonstrates significant potency. RORγt/DHODH-IN-1 has been shown to possess notable in vivo anti-inflammatory activity, making it a valuable tool for research in immunology and inflammation-related studies. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-3 is a dual inhibitor targeting both RORγt and dihydroorotate dehydrogenase (DHODH), exhibiting IC50 values of 0.098 μM for RORγt and 0.432 μM for DHODH. This compound demonstrates significant in vivo anti-inflammatory activity, making it a valuable tool for researchers investigating autoimmune diseases and other inflammatory conditions. Its dual mechanism of action positions it as a promising candidate for therapeutic development in these areas. -
hDHODH Inhibitor
hDHODH-IN-11 is a selective inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibiting an IC50 value of 7.2 nM. This compound demonstrates low cytotoxicity, making it suitable for in vitro studies. hDHODH-IN-11 is primarily utilized in research focused on acute myeloid leukemia (AML), contributing to the understanding of therapeutic targets within this malignancy. -
hDHODH Inhibitor
hDHODH-IN-10 is a selective and potent inhibitor of human dihydroorotate dehydrogenase (hDHODH), demonstrating an IC50 value of 10.9 nM. This compound exerts its biological activity through hydrogen bonding interactions with key residues, including Arg136 and Gln47. hDHODH-IN-10 effectively inhibits the proliferation of cancer cells and is useful for research applications related to various malignancies, such as acute myeloid leukemia (AML) and colorectal cancer. -
RORγt/DHODH Inhibitor
RORγt/DHODH-IN-2 is a potent dual inhibitor of RORγt and DHODH, targeting key pathways involved in immune regulation and inflammation. This compound exhibits significant biological activity that can be leveraged in the investigation of inflammatory bowel disease (IBD) and related immune disorders. Its dual action provides a valuable tool for research into therapeutic strategies aimed at modulating RORγt and DHODH activity in inflammatory contexts. -
DHODH Inhibitor
DHODH-IN-18 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), with an IC50 value of 0.2 nM. This compound effectively modulates the de novo pyrimidine biosynthesis pathway, making it a valuable tool in studies of cell proliferation and differentiation. DHODH-IN-18 is suitable for research applications in cancer biology and autoimmune disorders, where DHODH plays a critical role. -
DHODH Inhibitor
DHODH-IN-21 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor, exhibiting an IC50 value of 1.1 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for research into acute myeloid leukemia (AML). Its high potency and specificity for DHODH facilitate investigations into the mechanistic roles of this enzyme in cancer biology. -
DHODH Inhibitor
DHODH-IN-22 is a highly selective and orally bioavailable inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 0.3 nM. This compound demonstrates significant potential in the research of acute myelogenous leukemia (AML) by modulating pyrimidine synthesis and impacting cell proliferation. Its properties make DHODH-IN-22 a valuable tool for studying the biochemical pathways involved in AML and evaluating novel therapeutic strategies. -
DHODH Inhibitor
Indoluidin E is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), an enzyme involved in the de novo pyrimidine biosynthesis pathway. This compound has demonstrated notable inhibitory effects on cancer cell proliferation, making it a valuable tool for cancer research. Its mechanistic action allows for potential applications in studying metabolic pathways and developing therapeutic strategies targeting DHODH in various malignancies. -
hDHODH Inhibitor
hDHODH-IN-9 is a specific inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 value of 0.34 μM. This compound exhibits significant cytotoxic activity against MCF-7 and A375 cancer cell lines, showcasing its potential for selective targeting in cancer research. hDHODH-IN-9 serves as a valuable tool for studies investigating the role of hDHODH in tumorigenesis and cancer therapy. -
DHODH Inhibitor
DHODH-IN-34 is a selective inhibitor of human dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 13 nM. This compound is particularly valuable for researching RNA viruses, including measles virus and chikungunya virus, due to its ability to disrupt nucleotide synthesis pathways critical for viral replication. Researchers can leverage DHODH-IN-34 to investigate therapeutic strategies against these viral infections. -
Tyrosinase Inhibitor
Cepharadione B is a natural tyrosinase inhibitor derived from the leaves of Piper sanctum, exhibiting an IC50 value of 170 μM. This compound demonstrates significant inhibitory effects on cell growth in various cancer cell lines, including A-549, SK-OV-3, SK-MEL-2, XF-498, and HCT-15. Cepharadione B is valuable for research exploring pigmentation processes, melanoma, and potential therapeutic interventions against cancer. -
Thrombin/ Factor Xa Inhibitor
Ciraparantag is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants. This compound effectively neutralizes the effects of low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. Its unique mechanism makes Ciraparantag a valuable tool for research focused on anticoagulation reversal and hemostasis. -
Thrombin/Factor Xa Inhibitor
Ciraparantag acetate is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants, including low molecular weight heparins, unfractionated heparins, and certain direct oral anticoagulants, excluding vitamin K antagonists (VKAs). Its primary mechanism targets the coagulation pathway, facilitating the restoration of normal hemostasis in clinical situations where anticoagulation reversal is necessary. Ciraparantag acetate is valuable in research applications focused on anticoagulation management and hemostatic balance in cardiovascular studies. -
Thrombin Inhibitor
Edoxaban impurity 4 is a structural impurity related to Edoxaban, a selective and potent thrombin inhibitor. It demonstrates significant biological activity and is primarily utilized in research applications focusing on anticoagulation strategies. Edoxaban itself serves as an effective anticoagulant, with its mechanistic role in inhibiting factor Xa contributing to therapeutic approaches for stroke prevention and other thromboembolic disorders. -
Thrombin/Factor Xa Inhibitor
Ciraparantag TFA is a potent thrombin and factor Xa inhibitor utilized as a broad-spectrum reversal agent for anticoagulants. It effectively antagonizes the effects of various anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and specific direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. This compound is significant for research applications focused on enhancing hemostatic management in patients receiving anticoagulant therapy. -
Thrombin/Factor Xa/Trypsin/Papain Inhibitor
Bacithrocin D is a potent inhibitor of key proteases, specifically targeting thrombin, factor Xa, trypsin, and papain. It effectively prolongs clotting time, making it valuable in studies related to coagulation and hemostasis. Bacithrocin D demonstrates IC50 values of 124 μM for thrombin, 9 μM for factor Xa, 0.85 μM for trypsin, and a remarkable 0.01 μM for papain, showcasing its high potency against these proteases. This reagent is useful for investigating protease-related pathways and developing therapeutic strategies in anticoagulation research. -
Thrombin Inhibitor
Bacithrocin A is a potent thrombin inhibitor that also targets factor Xa, trypsin, and papain, demonstrating IC50 values of 48 μM, 13 μM, 0.65 μM, and 0.02 μM, respectively. This compound is of particular interest in the study of coagulation processes and the development of anticoagulant therapies. Its broad-spectrum inhibitory activity makes it a valuable reagent for biological research focused on protease activity modulation and hemostasis. -
Thrombin Inhibitor
Bacithrocin C is a potent thrombin inhibitor that effectively targets thrombin, factor Xa, trypsin, and papain, exhibiting IC50 values of 80 μM, 15 μM, 1.3 μM, and 0.02 μM, respectively. This compound demonstrates significant inhibitory activity, making it a valuable tool for research in coagulation pathways and protease-related studies. It is suitable for applications focused on understanding thrombotic processes and developing antithrombotic strategies. -
Thrombin Inhibitor
Bacithrocin B is a potent thrombin inhibitor that also targets factor Xa, trypsin, and papain. It exhibits inhibitory activity with IC50 values of 84 μM for thrombin, 17 μM for factor Xa, 1.7 μM for trypsin, and 0.02 μM for papain. This compound is valuable for research applications aiming to study coagulation processes and enzyme dynamics in various biological systems. -
Glutamine Synthetase Inhibitor; Convulsant
L-Methionine-DL-sulfoximine is a highly specific and irreversible inhibitor of glutamine synthetase, which significantly affects astroglial metabolism and morphology. This compound also demonstrates potent convulsant properties. L-Methionine-DL-sulfoximine has been utilized in research to inhibit glutamine-dependent neuronal toxicity in vitro and to study the mechanisms underlying convulsive seizures. Additionally, it enhances the rate of fixed nitrogen release in cyanobacteria, making it a valuable tool for applications in biofertilizer research. -
μ-Calpain Inhibitor
Calpain Inhibitor-2 is a peptide inhibitor targeting μ-calpain, with a Ki value of 9 nM. This compound demonstrates significant antiproliferative activity against melanoma cell lines, specifically A-375 and B-16F1, as well as PC-3 prostate cancer cells in vitro. It is a valuable tool for research applications focused on exploring calpain-mediated pathways in cancer biology. -
Aminopeptidase P2 Inhibitor
ST-115 is a potent inhibitor of aminopeptidase P2, a target involved in the regulation of various physiological processes. Its high specificity makes it an invaluable tool for studying the role of aminopeptidase P2 in ischemic stroke and related conditions. Researchers may utilize ST-115 to explore its potential therapeutic implications in neuroprotection and recovery following cerebral ischemia. -
Aminopeptidase A Inhibitor
Firibastat is a potent inhibitor of aminopeptidase A (APA), exhibiting a Ki value of 200 nM. This first-in-class compound effectively inhibits the conversion of brain angiotensin-II to angiotensin-III, resulting in reduced blood pressure in hypertensive models. Firibastat is particularly valuable in exploring the role of APA in neurophysiological processes and hypertension research.
