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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Cysteine Protease inhibitor
Leupeptin hemisulfate is a reversible inhibitor of trypsin-like and cysteine proteases such as calpain. -
HIV-1 attachment inhibitor
BMS-626529 is a potent HIV-1 attachment inhibitor. BMS-663068 is also the phosphonooxymethyl prodrug of BMS-626529 that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells. -
Proteasome inhibitor
ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies. -
Neutrophil elastase inhibitor
Sivelestat is a cell-permeable sulfanilide compound that acts as a potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase). -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
metalloendopeptidase inhibitor
Phosphoramidon Disodium Salt is a metalloendopeptidase inhibitor. -
Calpain inhibitor
PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 uM for μ-Calpain, about 20-fold selectivity over m-calpain. -
HIV protease inhibitor
Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM. -
aspartic protease inhibitor
Pepstatin A is a potent aspartic protease inhibitor, and also inhibits HIV replication. -
phosphatase inhibitor
(-)-p-Bromotetramisole Oxalate is a potent and non-specific alkaline phosphatase inhibitor. -
protein phosphatase inhibitor
Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1. -
PTP/PTEN Inhibitor
bpV(phen) is a potent inhibitor of protein tyrosine phosphatases (PTPs) and PTEN, exhibiting IC50 values of 38 nM, 343 nM, and 920 nM for PTEN, PTP-β, and PTP-1B, respectively. This compound demonstrates significant anti-proliferative effects on the protozoan parasite Leishmania in vitro. Additionally, bpV(phen) enhances the secretion of various chemokines and pro-inflammatory cytokines while promoting a Th1-type immune response characterized by IL-12 and IFNγ production. It also induces apoptosis and exhibits anti-angiogenic and anti-tumor properties, making it valuable for research in cancer and inflammation biology. -
Thrombin Inhibitor
Hirudin is a potent thrombin inhibitor known for its anticoagulant properties. It exhibits significant anti-thrombotic activity and is implicated in therapeutic applications such as wound repair, anti-fibrosis, and anti-tumor responses. Additionally, Hirudin has been explored for its effects on diabetic complications and cerebral hemorrhage, making it a valuable reagent in various research contexts. -
Calpain Inhibitor
Z-LLY-FMK is a potent calpain inhibitor that exhibits significant effects on apoptosis across various cell systems. By inhibiting calpain activity, Z-LLY-FMK has been shown to mitigate intestinal apoptosis following common bile duct ligation and reduce parasite burden in mouse models challenged with Taenia crassiceps cysts. This reagent serves as a valuable tool for research into cysticercosis and the role of calpain in cellular processes. -
Tyrosinase Inhibitor
Aloesin is a potent tyrosinase inhibitor known for its diverse biological activities, including anti-inflammatory effects and ultraviolet protection. Additionally, it exhibits antibacterial properties and has been shown to induce apoptosis in various cancer cell lines, making it a valuable compound for research in ovarian cancer and related studies. Its multifunctional profile provides a broad spectrum of applications in both dermatological and oncology research. -
LonP1/ CT-L proteasome inhibitor
BT317 is a selective inhibitor of mitochondrial Lon peptidase I (LonP1) and the caspase-like (CT-L) activity of the proteasome. This compound has been shown to increase the production of reactive oxygen species (ROS), leading to apoptosis in astrocytoma cells. BT317 exhibits significant antitumor activity, making it a valuable reagent for research in cancer biology and therapeutic applications targeting gliomas. -
Proteasome Inhibitor
YSY01A is a potent proteasome inhibitor that promotes apoptosis in cancer cells, demonstrating IC50 values of 51.0 nM in HEK293T, 9.2 nM in A549, 5.2 nM in MCF-7, 8.9 nM in MGC-803, and 35.4 nM in PC-3M cell lines. This compound effectively disrupts constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A serves as a valuable tool for research in cancer therapy and apoptosis mechanisms. -
PTPN2/1 Dual Inhibitor
PTPN2/1-IN-4 is a potent dual inhibitor of PTPN1 and PTPN2, exhibiting IC50 values of 12.8 nM and 5.8 nM, respectively. This compound effectively modulates the IFNγ-JAK-STAT signaling pathway, resulting in enhanced CD8+ T-cell infiltration into tumors. PTPN2/1-IN-4 demonstrates significant anticancer activity, inhibiting tumor growth both as a standalone treatment and in combination with anti-PD-1 antibodies in B16-OVA syngeneic mouse models, making it a valuable tool for cancer research. -
DHODH Inhibitor
JNJ-74856665 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 of 0.396 nM for human DHODH. This compound disrupts pyrimidine synthesis, making it a valuable tool for studying the role of DHODH in various biological processes, including cell proliferation and immune response modulation. JNJ-74856665 has potential applications in research related to autoimmune diseases and cancer therapeutic strategies. -
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 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 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. -
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/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.
