Catalog No.
Product Name
Application
Product Information
Citations
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DHODH Inhibitor
Lapachol is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), demonstrating significant immunosuppressive effects on lymphocytes by disrupting pyrimidine synthesis. This natural naphthoquinone exhibits antitumor properties, inhibiting DNA and RNA synthesis in neoplastic cells. Additionally, Lapachol has shown efficacy against Leishmania, suggesting its potential in parasitological research and therapeutic applications. -
DHODH Inhibitor
AG-636 is a selective and reversible inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 17 nM. This compound demonstrates significant anticancer activity, making it a valuable tool in cancer research and pharmacological studies targeting the de novo pyrimidine synthesis pathway. Its oral bioavailability further enhances its utility in preclinical and clinical studies. -
Immunomodulator/DHODH Inhibitor
Laflunimus is an immunomodulator that primarily functions as an inhibitor of dihydroorotate dehydrogenase (DHODH). This compound effectively suppresses the secretion of immunoglobulins, demonstrating IC50 values of 2.5 µM for IgM and 2 µM for IgG. Additionally, Laflunimus serves as an inhibitor of prostaglandin endoperoxide H synthases (PGHS-1 and PGHS-2), making it valuable for research applications focused on immunosuppression and inflammatory pathways. -
Potent DHODH Inhibitor
DHODH-IN-1 is a potent inhibitor of Dihydroorotate Dehydrogenase (DHODH), exhibiting an IC50 of 25 nM. By targeting the DHODH enzyme, this compound effectively disrupts the pyrimidine biosynthesis pathway, making it a valuable tool for researchers investigating cellular proliferation and metabolic regulation. Its application spans the study of autoimmune diseases, cancer research, and other conditions where modulation of pyrimidine synthesis is critical. -
DHODH Inhibitor
hDHODH-IN-5 is a potent inhibitor of human dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 0.91 μM. This compound has been demonstrated to induce differentiation in acute myeloid leukemia cells, highlighting its potential utility in cancer research. hDHODH-IN-5 serves as a valuable tool for investigating the role of DHODH in cellular differentiation and proliferation pathways. -
DHODH Inhibitor
DHODH-IN-14 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 of 0.49 μM against rat liver DHODH. This hydroxyfurazan analog of A771726 demonstrates significant potential in the treatment of rheumatoid arthritis. Its inhibitory capacity on DHODH suggests applications in modulating pyrimidine synthesis, providing a valuable tool for research in autoimmune disorders and related therapeutic development. -
DHODH Inhibitor
hDHODH-IN-4 is a selective inhibitor of human dihydroorotate dehydrogenase (DHODH), exhibiting a pIC50 of 7.8 against human recombinant DHODH. This compound effectively inhibits measles virus replication, demonstrated by a pMIC50 of 8.8. As a DHODH inhibitor, hDHODH-IN-4 is valuable for research into viral infections and the modulation of pyrimidine metabolism. -
HsDHODH Inhibitor
hDHODH-IN-3 is a potent inhibitor of human dihydroorotate dehydrogenase (HsDHODH), which plays a critical role in the de novo pyrimidine synthesis pathway. This compound has demonstrated significant antiviral activity, particularly inhibiting measles virus replication with a pMIC50 value of 8.6. hDHODH-IN-3 is particularly valuable for research in virology and metabolic diseases. -
hDHODH Inhibitor
hDHODH-IN-1 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH), an enzyme essential for de novo pyrimidine synthesis. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research in autoimmune diseases and inflammatory conditions. Its mechanism of action allows for exploration in therapeutic applications aimed at modulating immune responses and cellular proliferation. -
PfDHODH Inhibitor
PfDHODH-IN-1 is an inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH). This compound exhibits significant antimalarial activity by disrupting the pyrimidine biosynthesis pathway in the malaria parasite. PfDHODH-IN-1 serves as a valuable tool for research focused on malaria treatment and the exploration of novel therapeutic strategies against Plasmodium falciparum infections. -
Rat DHODH Inhibitor
DHODH-IN-11 is a Leflunomide derivative that functions primarily as a dihydroorotate dehydrogenase (DHODH) inhibitor. This compound demonstrates weak inhibitory activity against DHODH, an essential enzyme in the de novo pyrimidine synthesis pathway. It is particularly relevant for research in cellular metabolism and immunology, providing insights into therapeutic strategies for autoimmune disorders and certain cancers. -
Caspase-3/Caspase-7 Inhibitor
Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7, targeting the proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site. This compound is crucial for studying apoptosis and cellular signaling mechanisms by selectively modulating caspase activity. Its application extends to research areas involving cell death regulation and disease models where caspase-mediated pathways play a pivotal role. -
Tyrosinase Inhibitor
Dalbergioidin is a potent tyrosinase inhibitor that demonstrates significant activity through its ability to modulate enzymatic processes related to melanin biosynthesis. This compound has been shown to ameliorate renal fibrosis induced by doxorubicin by suppressing the TGF-β signaling pathway. Dalbergioidin's potential applications include studies focused on skin disorders and the regulation of pigmentation. -
Tyrosinase Inhibitor
AP736 is a potent inhibitor of tyrosinase, exhibiting an IC50 value of 0.9 μM, and demonstrates significant anti-melanogenesis activity in normal human melanocytes with an IC50 of 0.11 μM. By inhibiting the cAMP-PKA-CREB signaling pathway, AP736 effectively reduces the expression of tyrosinase and TRP-1/2, leading to a decrease in microphthalmia-associated transcription factor (MITF) transcripts and proteins. This compound is suitable for investigations into melanogenesis and the underlying mechanisms of hyperpigmentation. -
γ-Secretase Inhibitor
EVP-0015962 is a potent γ-secretase inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 value of 3.9 μM. By modulating the γ-secretase-mediated cleavage of amyloid precursor protein, EVP-0015962 decreases the production of Aβ42 while increasing Aβ38 levels. This compound has demonstrated efficacy in reducing amyloid aggregates, mitigating amyloid plaque formation, and lowering inflammatory markers in mouse models, thereby enhancing cognitive function. EVP-0015962 serves as a valuable tool in Alzheimer's disease research. -
γ-Secretase Modulator
AZ1136 is a selective γ-secretase modulator (GSM) that effectively reduces the levels of amyloid-beta peptides Aβ42 and Aβ40, with IC50 values of 990 nM and 1400 nM, respectively. Furthermore, AZ1136 increases levels of Aβ39 and Aβ37 while showing no effect on Aβ38. This compound is valuable for research applications investigating the pathogenesis of Alzheimer's disease and the modulation of amyloid-beta metabolism. -
γ- Secretase Modulator
BIIB042 is a selective γ-secretase modulator that effectively alters the processing of amyloid precursor protein, resulting in decreased levels of Aβ42 and increased levels of Aβ38. This compound demonstrates significant brain penetration and has shown efficacy in reducing brain Aβ42 levels in CF-1 mice and Fischer rats, while also lowering plasma Aβ42 levels in cynomolgus monkeys. Additionally, BIIB042 decreases Aβ42 levels and ameliorates Aβ plaque burden in Tg2576 mouse models. This reagent is valuable for research into Alzheimer’s disease. -
γ-secretase Modulator
(E/Z)-Sulindac sulfide is a selective γ-secretase modulator that plays a crucial role in the modulation of amyloid-beta (Aβ) peptide production. This compound notably reduces the production of Aβ42, favoring the generation of shorter Aβ species, making it a valuable tool for research into Alzheimer's disease. Its ability to influence Aβ processing makes (E/Z)-Sulindac sulfide significant for studies focusing on Alzheimer's pathogenesis and potential therapeutic strategies. -
γ-secretase Inhibitor
JNJ-40418677 is a potent orally active inhibitor of γ-secretase, capable of crossing the blood-brain barrier. It effectively inhibits the production of Aβ42 and the activity of NS2B-NS3 protease, with IC50 values of 200 nM and 3.9 μM, respectively. This compound exhibits favorable biological tolerance and is suitable for research applications related to Alzheimer's disease. -
γ-Secretase Modulator
PF-06648671 is an orally active γ-secretase modulator that effectively penetrates the blood-brain barrier. This compound demonstrates the ability to reduce levels of amyloid-beta peptides Aβ42 and Aβ40, while concurrently increasing Aβ37 and Aβ38 in vitro. PF-06648671 is valuable for research applications focused on Alzheimer’s disease and the modulation of amyloid processing pathways. -
γ-secretase Inhibitor
Sulindac sulfide is a noncompetitive inhibitor of γ-secretase, exhibiting an IC50 of 20.2 μM for γ42-secretase activity. This compound plays a crucial role in research involving Alzheimer's disease and other neurodegenerative conditions by modulating the processing of amyloid precursor protein. Its ability to inhibit γ-secretase makes it a valuable tool for studies focused on reducing amyloid-beta peptide formation and investigating related signaling pathways. -
γ-secretase Inhibitor
ELND 006 is a selective γ-secretase inhibitor that effectively reduces amyloid beta (Aβ) generation while preserving Notch signaling pathways. Developed with a focus on metabolic stability, this compound has shown significant efficacy in lowering Aβ levels both in vitro and in vivo during preclinical studies. ELND 006, alongside its structural analog ELND 007, has advanced into human clinical trials, indicating its potential therapeutic applications in Alzheimer's disease research and treatment. -
γ-secretase Modulator
RO7185876 is a selective gamma-secretase modulator that plays a crucial role in the regulation of amyloid precursor protein processing. This compound is primarily investigated for its potential in Alzheimer's disease research, where it may help reduce the production of amyloid-beta peptides. Its unique mechanism of action positions RO7185876 as a valuable tool for studying the pathophysiology of Alzheimer's and exploring therapeutic options. -
γ-secretase Modulator
GSM-1 is a potent γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1). By modulating γ-secretase activity, GSM-1 influences the processing of amyloid precursor protein (APP), making it valuable in Alzheimer's disease research. This compound can be utilized to investigate mechanisms of amyloid-beta peptide generation and potential therapeutic strategies for neurodegenerative disorders. -
gamma-Secretase Inhibitor
Gamma-secretase modulator 6 is a gamma-secretase inhibitor that effectively reduces the secretion of Aβ42 in HEK cells stably expressing amyloid precursor protein (APP), with a pIC50 value of 8.1. This compound plays a crucial role in the study of Alzheimer's disease by modulating gamma-secretase activity, thereby influencing amyloid plaque formation. It is a valuable tool for researchers exploring therapeutic strategies targeting amyloid pathology in neurodegenerative disorders. -
γ-secretase Modulator
FRM-024 is a potent γ-secretase modulator designed for central nervous system applications. It selectively alters the activity of γ-secretase, a critical enzyme involved in the pathogenesis of familial Alzheimer’s disease. This compound has demonstrated the ability to influence amyloid precursor protein processing, making it a valuable tool for research focused on Alzheimer’s therapeutics and disease mechanisms. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-2 is a selective γ-secretase inhibitor that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 226 nM. This compound demonstrates potential for research applications in Alzheimer's disease and other conditions associated with Aβ deposition. Its ability to modulate γ-secretase activity makes it a valuable tool for studying the mechanisms underlying amyloid-related pathologies. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-3 is a selective inhibitor of γ-secretase that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 148 nM. By modulating γ-secretase catalytic activity, it decreases Aβ42 production and helps mitigate the neurotoxicity associated with amyloid deposition. This compound shows potential for research applications in Alzheimer's disease (AD) studies. -
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 Modulator
(-)-FRM-024 is a potent γ-secretase modulator that effectively penetrates the central nervous system. This compound is instrumental in Alzheimer’s disease research, facilitating the study of amyloid precursor protein processing and its implications in neurodegeneration. Its ability to modulate γ-secretase activity makes it a valuable tool for exploring therapeutic interventions in Alzheimer's pathology. -
γ-Secretase Modulator
γ-Secretase modulator 4 is a potent modulator of the γ-secretase enzyme, characterized by its ability to effectively reduce Aβ42 peptide levels with IC50 values of 0.014 μM in human samples and 0.017 μM in mouse samples. This compound has significant implications in Alzheimer's research, particularly in the study of amyloid-beta production and the related pathophysiology. Its mechanism of action makes it a valuable tool for investigations into therapeutic strategies targeting Alzheimer's disease. -
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. -
Gamma-Secretase Modulator
Gamma-Secretase Modulator 1 Hydrochloride acts as a modulator of gamma-secretase, a crucial enzyme implicated in the pathogenesis of Alzheimer's disease. This compound is designed to influence the processing of amyloid precursor protein (APP), ultimately affecting the production of amyloid-beta peptide. Its potential applications include studying the modulation of amyloid-beta levels and investigating therapeutic strategies for Alzheimer's disease and related neurodegenerative disorders. -
γ-secretase Modulator
Nivegacetor is a potent γ-secretase modulator that plays a critical role in the modulation of amyloid precursor protein processing. By influencing the activity of γ-secretase, Nivegacetor is valuable for research into Alzheimer's disease and other neurodegenerative conditions. Its ability to alter the production of amyloid-beta peptides makes it a useful tool for exploring therapeutic pathways and understanding the molecular mechanisms underlying these diseases. -
γ-Secretase Modulator
Aβ42-IN-1 is a potent γ-secretase modulator (GSM) designed to target the enzymatic cleavage of amyloid precursor protein, effectively lowering amyloid-beta 42 (Aβ42) levels. With an IC50 value of 0.091 μM, Aβ42-IN-1 demonstrates significant inhibition of Aβ42 production while avoiding CYP3A4 inhibition, indicating a favorable safety profile. Its sustained pharmacokinetic properties make it a valuable tool for research into Alzheimer's disease and related neuropathologies. This compound holds promise for exploring therapeutic strategies aimed at modulating γ-secretase activity in neurodegenerative disorders. -
γ-Secretase Modulator
Aβ42-IN-1 free base is a potent γ-secretase modulator that exhibits high oral bioavailability and significant brain penetration. This compound effectively lowers Aβ42 levels with an IC50 of 0.091 μM, demonstrating substantial reduction of brain Aβ42 levels in murine models. Aβ42-IN-1 free base holds considerable potential for therapeutic applications in Alzheimer's disease research. -
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 Modulator
γ-Secretase modulator 10 is a selective modulator of the γ-secretase enzyme complex. It influences the cleavage of amyloid precursor protein (APP), thereby altering the production of amyloid β peptides associated with Alzheimer's disease pathogenesis. This compound is valuable for research applications focused on neurodegenerative diseases and therapeutic strategies aimed at modulating γ-secretase activity. -
γ-Secretase Modulator
γ-Secretase modulator 14 is a selective modulator of the γ-secretase complex, influencing the cleavage of amyloid precursor protein (APP). This compound exhibits potential in Alzheimer's disease research by altering the production of amyloid-beta peptides. Its utility extends to investigating the mechanisms underlying neurodegenerative disorders and developing novel therapeutic strategies aimed at modulating γ-secretase activity. -
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 Modulator
BPN-15606 besylate is a potent orally active γ-secretase modulator (GSM) that effectively reduces the production of Aβ42 and Aβ40 peptides in SHSY5Y neuroblastoma cells, exhibiting IC50 values of 7 nM and 17 nM, respectively. This compound has demonstrated the ability to lower Aβ42 and Aβ40 levels in the central nervous system of rodent models. Additionally, BPN-15606 besylate features favorable pharmacokinetic and pharmacodynamic properties, including good bioavailability, optimal half-life, and manageable clearance rates, making it valuable for Alzheimer's disease research and neurodegenerative studies. -
γ-secretase Modulator
BMS-932481 is a potent γ-secretase modulator that demonstrates selective reduction of β-amyloid peptides Aβ1-42 and Aβ1-40, exhibiting IC50 values of 6.6 nM and 25.3 nM, respectively. This compound is valuable for research into Alzheimer's disease and mechanisms of amyloid plaque formation, offering insights into potential therapeutic strategies targeting γ-secretase activity. -
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 Modulator
γ-Secretase modulator 12 is a selective modulator of γ-secretase, specifically designed to reduce levels of amyloid-β42 (Aβ42) with an IC50 of 0.39 µM. This compound is valuable for investigating Alzheimer's disease mechanisms and potential therapeutic interventions. Additionally, γ-secretase modulator 12 demonstrates favorable pharmacokinetics with a good brain-to-plasma ratio (Kp, brain = 0.72) in murine models, making it suitable for in vivo studies. -
γ-Secretase Modulator
γ-Secretase modulator 11 hydrochloride is a potent modulator of γ-secretase with an IC50 of 0.029 µM, demonstrating oral bioavailability. It effectively reduces brain Aβ42 levels, a critical factor in Alzheimer's disease pathology. Furthermore, this compound has shown the capability to improve cognitive deficits in Alzheimer's disease model mice, making it valuable for research into therapeutic strategies targeting Alzheimer's disease. -
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 Modulator
BMS-869780 is an orally active γ-secretase modulator that selectively regulates γ-secretase activity to modify the production profile of β-amyloid proteins. It alters the relative levels of specific β-amyloid subtypes while not inhibiting the overall production of β-amyloid proteins. Additionally, BMS-869780 demonstrates a synergistic effect when used in combination with acidic γ-secretase modulators, resulting in a reduction of total β-amyloid production in cell cultures. This compound is valuable for research into Alzheimer’s disease and related neurodegenerative disorders.
