Catalog No.
Product Name
Application
Product Information
Citations
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γ secretase Modulator
PF-06442609 is an orally active γ secretase modulator that effectively inhibits amyloid-beta (Aβ42) production with an IC50 of 6 nM. This compound demonstrates excellent brain penetration, making it suitable for research in neurodegenerative disease models, particularly Alzheimer's disease. Its modulatory effects on γ secretase activity provide valuable insights into the mechanistic understanding of amyloid plaque formation and associated pathologies. -
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
LY-411575 (isomer 1) is a potent γ-secretase inhibitor that selectively modulates the enzyme's activity. This compound is primarily utilized in the investigation of Alzheimer’s disease pathogenesis by reducing the production of harmful amyloid-beta peptides. Its mechanism of action allows for a deeper understanding of γ-secretase's role in cellular signaling and pathology, making it a valuable tool in neurological research. -
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. -
Tyrosinase-Resistant Mimetic
3,5-Difluoro-L-tyrosine is a functional mimetic of tyrosine that exhibits resistance to tyrosinase. This compound is utilized to investigate the substrate specificity of protein tyrosine phosphatases (PTPs), making it valuable for research into tyrosine phosphorylation pathways and their regulatory mechanisms. -
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. -
Calcium Supplement
Calcium glucoheptonate is a highly soluble calcium supplement that primarily targets calcium deficiency. It enhances the proliferation rate and calcium uptake in MG-63 osteoblast-like cells and increases the activity of alkaline phosphatase (ALP). Additionally, it upregulates the expression of osteogenic markers such as collagen-1 and osteocalcin. This compound is valuable for research applications focused on osteoporosis and hypocalcemia. -
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. -
DPPH Scavenger
2,4,7-Trihydroxy-9,10-dihydrophenanthrene is a dihydrophenanthrene derivative primarily targeting DPPH radicals. It exhibits significant antioxidant activity, with an IC50 value of 16.2 μM in DPPH radical-scavenging assays. This compound is useful in research applications focused on antioxidant mechanisms and the study of natural products derived from Pholidota chinensis Lindl. -
DPP4 Inhibitor
Evogliptin tartrate is an orally active DPP4 inhibitor that exhibits significant and sustained hypoglycemic effects in murine models. It not only lowers blood glucose levels but also attenuates the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. This compound is suitable for research applications related to type 2 diabetes, osteoporosis, renal impairment, and chronic liver inflammation. -
DHODH Inhibitor
DHODH-IN-8 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH) in both human and Plasmodium falciparum, exhibiting IC50 values of 0.13 μM and 47.4 μM, respectively. Additionally, it demonstrates Kis of 0.016 μM for human DHODH and 5.6 μM for the parasite's enzyme. This compound shows significant antimalarial activity, making it a valuable tool for research into malaria treatment and the inhibition of the pyrimidine biosynthesis pathway. -
DHODH Inhibitor
DHODH-IN-20 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), an iron-containing flavin-dependent enzyme located in the inner mitochondrial membrane of human cells. By inhibiting DHODH, this compound exhibits significant anti-tumor activity, making it a valuable tool in the study of cancer biology. DHODH-IN-20 is particularly relevant for research focused on acute myelogenous leukemia, offering insights into potential therapeutic strategies. -
HsDHODH Inhibitor
DHODH-IN-3 is a selective inhibitor of Human Dihydroorotate Dehydrogenase (HsDHODH), demonstrating a potent inhibitory effect with an IC50 value of 261 nM. By targeting the ubiquinone binding sites within the enzyme, DHODH-IN-3 exhibits a competitive inhibition profile, characterized by a Kiapp of 32 nM. This compound shows promise for therapeutic applications in malaria research, potentially contributing to the development of novel treatments. -
DHODH Inhibitor
DHODH-IN-12 is a derivative of Leflunomide that functions as a dihydroorotate dehydrogenase (DHODH) inhibitor. This compound displays weak inhibitory activity against DHODH, making it a valuable tool for studying the modulation of pyrimidine metabolism. Its applications include investigations into immunological diseases and the development of therapeutics targeting nucleotide synthesis pathways. The pKa of 5.07 further informs its solubility and stability characteristics in biological systems. -
hDHODH Inhibitor
hDHODH-IN-2 is a selective inhibitor of human dihydroorotate dehydrogenase (hDHODH), functioning as an analogue of Leflunomide's active metabolite. This compound exhibits anti-inflammatory properties, making it relevant for research into autoimmune diseases and other inflammatory conditions. Its mechanism of action targets pyrimidine synthesis, effectively reducing the production of lymphocytes involved in inflammatory responses. -
DHODH Inhibitor
DHODH-IN-13 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), displaying an IC50 of 4.3 μM for rat liver DHODH. This hydroxyfurazan analog of A771726 demonstrates significant biological activity in modulating pyrimidine metabolism. DHODH-IN-13 is primarily utilized in research related to rheumatoid arthritis and other autoimmune conditions, making it a valuable tool for exploring therapeutic strategies in these areas. -
hDHODH Inhibitor
hDHODH-IN-14 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH), exhibiting an IC50 value of 0.469 μM. This compound is utilized primarily in research focused on modulating the de novo pyrimidine biosynthesis pathway. Its inhibitory effects make hDHODH-IN-14 a valuable reagent for studying metabolic processes and potential therapeutic strategies in various diseases, including autoimmune disorders and cancer. -
DHODH Inhibitor
DHODH-IN-19 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), an essential enzyme located in the inner membrane of human mitochondria that is critical for pyrimidine biosynthesis. This compound demonstrates significant anticancer activity by inhibiting tumor growth, making it a valuable tool for research in cancer and inflammatory diseases. Its mechanism of action offers potential insights into the metabolic pathways involved in these conditions. -
DHODH Inhibitor
hDHODH-IN-7 is a selective inhibitor of human dihydroorotate dehydrogenase (DHODH). It exhibits antiviral activity with a reported pMIC50 of 7.4, indicating its potential efficacy in reducing viral replication. This compound is suitable for research applications involving the study of viral infections and the regulation of pyrimidine biosynthesis. -
DHODH Inhibitor
DHODH-IN-15 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor, exhibiting an IC50 of 11 μM in rat liver DHODH assays. This hydroxyfurazan analog of A771726 demonstrates significant biological activity, making it a valuable tool for investigating the role of DHODH in various metabolic pathways. Its application extends to research on rheumatoid arthritis, contributing to the understanding of therapeutic strategies for inflammatory diseases. -
DHODH Inhibitor
DHODH-IN-25 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 value of 5.4 nM for human DHODH. This compound demonstrates significant biological activity and is particularly relevant for research applications involving acute myeloid leukemia (AML). DHODH-IN-25 provides valuable insights into the therapeutic potential of targeting pyrimidine biosynthesis in cancer treatment. -
DHODH Inhibitor
DHODH-IN-4 is a dihydroorotate dehydrogenase (DHODH) inhibitor targeting both human and Plasmodium falciparum DHODH. With IC50 values of 4 μM for PfDHODH and 0.18 μM for HsDHODH, this compound demonstrates significant potential as an antimalarial agent. It is suitable for research applications focused on understanding malaria pathology and developing effective treatments against Plasmodium infections. -
DHODH Inhibitor
DHODH-IN-24 is a potent inhibitor of human dihydroorotate dehydrogenase (DHODH) with an IC50 value of 91 nM. This compound effectively impairs the proliferation of rapidly dividing cells by hindering pyrimidine synthesis. DHODH-IN-24 is an important tool for investigating the role of DHODH in various biological processes and may have applications in the research of autoimmune diseases and cancer therapy. -
DHODH Inhibitor
P1788 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), a key enzyme in the de novo pyrimidine synthesis pathway. By inhibiting DHODH, P1788 induces DNA damage and has demonstrated potential in various cancer research applications. Its effects on pyrimidine metabolism make it a valuable tool for studying cellular proliferation and apoptosis. -
RORγ/DHODH Inhibitor
RORγ/DHODH-IN-1 is a dual inhibitor targeting RORγ and dihydroorotate dehydrogenase (DHODH) with IC50 values of 9.7 nM and 100 nM, respectively. This compound effectively inhibits the replication of SARS-CoV-2, human cytomegalovirus (HCMV), and adenovirus type 5 (HAdV5), making it a valuable tool in viral research. Its dual mechanism of action allows for potential applications in understanding viral-pathogen interactions and developing therapeutic strategies against viral infections. -
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. -
Tyrosinase inhibitor
Aloin (Barbaloin) is a yellow crystalline substance obtained from aloe and is reported to be a potent inhibitors of tyrosinase. -
Tyrosinase inhibitor
Arbutin is a glycosylated hydroquinone used in traditional Chinese medicine (TCM). Arbutin inhibits melanin formation due to its tyrosinase inhibitory activity.
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HIV Protease inhibitor
Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). -
HIV Protease inhibitor
Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). -
Thrombin inhibitor
BIBR-1048 (Dabigatran etexilate) is an anticoagulant from the class of the direct thrombin inhibitors. -
Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
Aminopeptidase inhibitor
CHR-2797 (Tosedostat) is a novel metalloenzyme inhibitor that exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity. -
Proteasome Inhibitor
Ixazomib Citrate (MLN9708) Analogue is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.
- Pimecrolimus is a natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase).
- Doxycycline Hydrochloride is a synthetic tetracycline derivative with similar antimicrobial activity.
- Racecadotril is a potent enkephalinase inhibitor which exhibits selective antisecretory activity.
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HIV Protease inhibitor
Ritonavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease.Ritonavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. -
DDP-4 inhibitor
Sitagliptin phosphate is an anti-diabetic (antihyperglycemic) drug of the dipeptidyl peptidase-4 (DPP-4) class. Inhibition of the enzyme DPP-4 is thought to increase Glucagon-like peptide-1 (GLP-1) which inhibits glucagon release , stimulates the insulin release and lowers blood glucose. -
protein tyrosine phosphatases inhibitor
Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue. -
reversible Protease inhibitor
Ubenimex, also known as NK 421 and Bestatin, is a CD13 inhibitor. Ubenimex attenuates acquired sorafenib resistance in renal cell carcinoma by inhibiting Akt signaling in a lipophagy associated mechanism. Ubenimex synergistically enhances the effects of anticancer drugs in hepatocellular carcinoma. Ubenimex inhibits cell proliferation, migration and invasion by inhibiting the expression of APN and inducing autophagic cell death in prostate cancer cells.
