Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
Calpain Inhibitor
Calpain Inhibitor V (Mu-Val-HPh-FMK) is an irreversible inhibitor of calpain, designed for effective cellular penetration. This compound exhibits notable anti-chlamydial activity and is utilized in research exploring calpain-mediated pathways and their implications in various diseases. Its application extends to studies focused on cellular signaling processes and the therapeutic potential of calpain modulation. -
Dopamine receptor Agonist, 20S proteasome Activator
Apomorphine hydrochloride is a potent dopamine receptor agonist and a known activator of the 20S proteasome. It enhances proteasomal and insulin-degrading enzyme activities, facilitating the degradation of intracellular amyloid-beta (Aβ), phosphorylated tau (p-tau), and p53, thereby reducing their levels in neuronal cells. This compound is particularly relevant for research focused on neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions including schizophrenia. -
Tyrosinase Inhibitor
2-Hydroxy-4-methoxybenzaldehyde is a potent inhibitor of the enzyme tyrosinase, which is crucial in melanin biosynthesis. This compound plays a significant role in research pertaining to pigmentation disorders and skin-related applications. Additionally, it can be utilized as a precursor for the synthesis of Urolithin M7, expanding its utility in biochemical studies. -
Aminopeptidase Inhibitor
Amastatin hydrochloride is a potent competitive inhibitor of aminopeptidases, exhibiting slow, tight binding kinetics. It demonstrates Ki values of 0.26 nM, 30 nM, and 52 nM against Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, and microsomal aminopeptidase, respectively. This compound is valuable for research applications focusing on protein metabolism and post-translational modifications, as well as in studies exploring the role of aminopeptidases in various physiological and pathological processes. -
Cell-penetrating Peptide/Proteasome Inhibitor
Octaarginine is a cell-penetrating peptide and potent proteasome inhibitor. It exhibits mixed-type inhibition against the chymotrypsin-like, caspase-like, and trypsin-like activities of the 20S proteasome while displaying reduced efficacy against the 26S proteasome. This compound facilitates the accumulation of ubiquitin-conjugated proteins and promotes HSPG-dependent cellular internalization through macropinocytosis, thereby enhancing the uptake of liposomal cargo and gene delivery. Octaarginine is valuable for research related to cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections. -
Aminopeptidase B Inhibitor
Arphamenine B hemisulfate is a selective inhibitor of aminopeptidase B, a Zn2+-dependent exopeptidase that primarily cleaves arginine and lysine residues from the N-terminus of peptide substrates. This compound is derived from bacterial sources and has been shown to enhance immune responses. Arphamenine B hemisulfate is utilized in research for characterizing novel proteases and investigating their biological roles. -
Proteasome Inhibitor
PR-39 is a natural proline- and arginine-rich antibacterial peptide that functions as a noncompetitive, reversible allosteric inhibitor of the proteasome. By binding to the α7 subunit of the proteasome, PR-39 effectively blocks the degradation of NF-κB inhibitor IκBα through the ubiquitin-proteasome pathway. This compound demonstrates key biological activities such as stimulating angiogenesis and inhibiting inflammatory responses, making it a valuable tool for research on myocardial infarction and inflammatory diseases. -
NEP/APN Inhibitor
Sialorphin targets neprilysin (NEP) and aminopeptidase N (APN) as a potent inhibitor, effectively preventing the degradation of key neuropeptides like Substance P and methionine enkephalin. This compound demonstrates significant biological activity, including analgesic effects, modulation of sexual behavior in male rats, and the alleviation of colitis. Additionally, Sialorphin exhibits low toxicity against specific tumor cells, making it a valuable tool for research into pain management, inflammatory bowel disease, and oncology. -
Proteasome Inhibitor
Antitrypanosomal agent 15 is a selective proteasome inhibitor targeting Trypanosoma cruzi, with an impressive pIC50 of 7.4 for the T. cruzi proteasome and minimal activity (pIC50 < 4) against human proteasomes. This orally active compound demonstrates excellent brain penetration and favorable ADME properties, making it suitable for research focused on Chagas disease and related therapeutic interventions. Its selectivity and efficacy highlight its potential for advancing studies in trypanosomiasis. -
PfDHODH Inhibitor
PfDHODH-IN-3 is a potent inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 47 nM. This compound exhibits strong antimalarial activity, effectively inhibiting the growth of Plasmodium in animal models. PfDHODH-IN-3 is valuable for research focused on antimalarial drug development and understanding the mechanisms of Plasmodium resistance. -
20S Proteasome Inhibitor
20S Proteasome-IN-4 is a selective inhibitor of the 20S proteasome, exhibiting an IC50 of 6.3 nM against Trypanosoma brucei brucei. This brain-penetrant compound is orally active and demonstrates potential for research into human African trypanosomiasis (HAT). Its specificity for the parasite makes it a valuable tool for studying proteasomal functions in this significant infectious disease. -
Proteasome Inhibitor
LXE408 fumarate is a non-competitive proteasome inhibitor selectively targeting kinetoplastids. It exhibits potent inhibitory activity with an IC50 of 0.04 μM against the L. donovani proteasome, demonstrating an EC50 of 0.04 μM for L. donovani itself. With limited ability to penetrate the blood-brain barrier, LXE408 fumarate is primarily suitable for research in visceral leishmaniasis (VL). -
Proteasome Inhibitor
Carmaphycin-17 is a selective 20S proteasome inhibitor, with an EC50 value of 217 nM. This compound exhibits strong antimicrobial activity against Trichomonas vaginalis, effectively overcoming Metronidazole resistance. It significantly reduces parasite burden in a topical treatment model without noted adverse effects. Carmaphycin-17 is a valuable tool for research on sexually transmitted diseases, specifically trichomoniasis. -
PfDHODH Inhibitor
DSM267 is a triazolopyrimidine compound that preferentially inhibits Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 38 nM, demonstrating significant selectivity over human DHODH with an IC50 exceeding 100,000 nM. This reagent is valuable for in vitro systematic screening and characterizing the pathways of resistance evolution in Plasmodium falciparum against DHODH inhibitors. Its use supports research into antimalarial resistance mechanisms and facilitates the development of novel therapeutic strategies. -
Pf Proteasome Inhibitor
Proteasome-IN-8 is a specific inhibitor of the proteasome in Plasmodium falciparum. This compound demonstrates notable antiparasitic activity against the P. falciparum 3D7 strain. It is a valuable tool for research into the mechanisms of malaria pathogenesis and the development of therapeutic strategies targeting parasitic proteasomes. -
DHODH Inhibitor
Genz-669178 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), demonstrating an IC50 range of 0.015-0.05 μM against Plasmodium species. It effectively inhibits P. berghei and P. falciparum strains 3D7 and Dd2, with respective IC50 values of 0.068, 0.008, and 0.01 μM. In vivo studies indicate that Genz-669178 exhibits significant anti-malarial efficacy in P. berghei-infected mice, with an ED50 of 13-21 mg/kg/day, alongside favorable pharmacokinetic properties. This compound serves as a valuable tool for malaria research and drug development. -
PfDHODH/PbDHODH Inhibitor
DSM74 is a potent inhibitor of dihydroorate dehydrogenase (DHODH) in both Plasmodium falciparum (PfDHODH) and Plasmodium berghei (PbDHODH), with IC50 values of 0.28 μM and 0.38 μM, respectively. This orally active compound exhibits significant antimalarial activity, effectively inhibiting the growth of Plasmodium species in animal models. It is a valuable tool for researchers investigating the mechanisms of malaria and developing novel therapeutic strategies. -
PfDHODH Inhibitor
BRD7539 is a potent inhibitor of PfDHODH, exhibiting an IC50 value of 0.033 μM. This compound demonstrates significant efficacy against multidrug-resistant asexual blood-stage Plasmodium falciparum (Dd2 strain) with an EC50 of 0.010 μM, as well as against liver-stage Plasmodium berghei, with an EC50 of 0.015 μM. BRD7539 serves as a valuable tool for research targeting malaria drug development and resistance mechanisms. -
Aminopeptidase B Inhibitor
Arphamenine B is a selective inhibitor of aminopeptidase B, a Zn2+-dependent exopeptidase that cleaves arginine and lysine residues from the amino terminus of peptide substrates. This compound enhances immune responses and serves as a valuable tool for the characterization of novel proteases in biochemical research. Its unique mechanism provides insights into protein metabolism and potential therapeutic applications. -
RORγ/DHODH Inhibitor
Izumerogant (IMU-935) is an orally active dual inhibitor of RORγ and DHODH, with IC50 values of 10 nM and 98 nM, respectively. This compound effectively disrupts the replication of various viruses, including SARS-CoV-2, HCMV, and HAdV5, demonstrated by EC50 values ranging from 3.6 to 17 nM. Izumerogant serves as a valuable tool for investigating antiviral mechanisms and therapeutic strategies against viral infections. -
NS2B-NS3/thrombin Inhibitor
5-((1H-Indol-3-yl)methylene)imidazolidine-2,4-dione is a potent inhibitor of the dengue virus NS2B-NS3 protease and thrombin. This compound is valuable for studying the mechanisms of viral replication and coagulation processes, making it an essential tool in research focused on infectious diseases and related therapeutic interventions. Its dual activity highlights its potential for investigating the dynamics of viral pathology and thrombotic complications. -
MMP/TACE/ADAM Inhibitor
(R)-TAPI-2 is a potent inhibitor targeting matrix metalloproteinases (MMPs), tumor necrosis factor alpha-converting enzyme (TACE), and a disintegrin and metalloproteinase (ADAM), exhibiting an IC50 value of 20 μM for MMP activity. This compound is utilized in research focused on inflammation, cancer progression, and cell signaling due to its ability to modulate proteolytic processes. Additionally, (R)-TAPI-2 has demonstrated efficacy in preventing viral entry, specifically in the context of SARS-CoV infections, making it valuable for virology studies. -
RORγ/DHODH Inhibitor
RORγ/DHODH-IN-2 is a potent dual inhibitor of RORγ and DHODH, exhibiting IC50 values of 11.9 nM and 90 nM, respectively. This compound demonstrates significant antiviral activity against multiple viruses, including SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC50 values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively. RORγ/DHODH-IN-2 is ideal for research applications targeting immune signaling pathways and viral infections. -
Aminopeptidase N/Leukotriene A4 Hydrolase Inhibitor
Bestatin trifluoroacetate is a potent inhibitor of CD13 (Aminopeptidase N) and leukotriene A4 hydrolase. It plays a significant role in cancer research by modulating enzymatic activity associated with tumor progression and inflammation. With its capability to interfere with amino acid metabolism, Bestatin trifluoroacetate is valuable for studying the biological processes linked to these targets.
