Catalog No.
Product Name
Application
Product Information
Citations
-
Aldose Reductase Inhibitor
WJ-39 is a potent orally active inhibitor of aldose reductase (AR), demonstrating significant therapeutic potential. This compound has been shown to mitigate tubular damage in diabetic nephropathy models by activating the PINK1/Parkin signaling pathway, thereby promoting mitophagy and reducing apoptosis. WJ-39 serves as a valuable tool for studying diabetic complications and the underlying mechanisms of kidney injury. -
Granzyme B/Caspase-8 Inhibitor
Ac-IETD-CHO is a potent, reversible inhibitor of granzyme B and caspase-8. By blocking these proteases, Ac-IETD-CHO effectively inhibits Fas-mediated apoptotic cell death, as well as preventing hemorrhage and liver failure. This compound is valuable for research in apoptosis, immune response, and the modulation of cytotoxic T lymphocyte-induced cell death. -
Proteasome Inhibitor
Ub4ix is a potent proteasome inhibitor that selectively protects K48-linked ubiquitin chains from deubiquitinating enzymes (DUBs), thereby preventing the degradation of ubiquitin-tagged proteins. This compound has demonstrated significant biological activity, including the reduction of cell viability and induction of apoptosis in HeLa cells, with an IC50 value of 1.6 μM. Ub4ix is a valuable tool for research applications focused on understanding protein homeostasis and the role of the proteasome in cellular processes. -
uPA Inhibitor
UCD38B hydrochloride is a competitive inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 value of 7 μM. This compound exhibits cell permeability and specifically targets intracellular uPA, leading to its mistrafficking into perinuclear mitochondria. This mistrafficking results in a reduction of mitochondrial membrane potential and ultimately promotes the release of apoptotic inducible factor (AIF), thereby inducing apoptosis. UCD38B hydrochloride is useful in research applications focused on cancer biology and therapeutic strategies targeting apoptosis. -
Proteasome Inhibitor
Baceridin is a proteasome inhibitor characterized as a cyclic hexapeptide. Isolated from the culture medium of Epiphytic Bacillus, it disrupts proteasome function, leading to inhibition of cell cycle progression and induction of apoptosis in tumor cells via a p53-independent mechanism. This compound is valuable for cancer research applications, particularly in studies exploring proteasome inhibition and its effects on tumor biology. -
Tubulin/MMP Inhibitor
Tubulin/MMP-IN-2 is a dual inhibitor targeting both tubulin and matrix metalloproteinases (MMPs). It effectively inhibits tubulin polymerization, leading to induced apoptosis in cancer cells. Additionally, Tubulin/MMP-IN-2 demonstrates inhibitory activity against MMP-2, MMP-3, and MMP-9, with IC50 values of 24.95 μM, 31.60 μM, and 22.37 μM, respectively. This compound is valuable for research focused on cancer biology and therapeutic development. -
γ-secretase Inhibitor
Nirogacestat dihydrobromide is a selective, noncompetitive inhibitor of γ-secretase, with a reported IC50 of 6.2 nM. This compound effectively inhibits Notch signaling, making it a valuable tool for studying Notch receptor-dependent cancers while minimizing gastrointestinal toxicity. It is particularly useful in research focused on the role of γ-secretase in cancer biology and therapeutic development. -
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. -
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
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 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.
