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Catalog No.
Product Name
Application
Product Information
Citations
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PDE Inhibitor
Quazodine is a potent phosphodiesterase (PDE) inhibitor that modulates intracellular cAMP and cGMP levels. Its primary activity involves vasodilatory effects, making it a valuable tool in studies related to vascular smooth muscle function. Quazodine is suitable for research applications exploring cardiovascular diseases and smooth muscle physiology. -
Phosphodiesterase (PDE) Inhibitor
K-252d is an indolocarbazole alkaloid that acts primarily as a phosphodiesterase (PDE) inhibitor. It demonstrates significant inhibitory activity against calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart, with an IC50 of 46.2 μM, and is also recognized for its role as a protein kinase C (PKC) inhibitor, exhibiting an IC50 of 350 nM against PKC isolated from rat brain. This compound is valuable for studies related to signal transduction pathways and therapeutic interventions targeting PDE-related disorders. -
PDE4 Inhibitor
Cipamfylline is a potent inhibitor of phosphodiesterase 4 (PDE4), specifically facilitating the accumulation of PDE4A4 within distinct cellular regions via its interaction with the ubiquitin scaffolding protein p62. This compound plays a critical role in research focused on atopic dermatitis, contributing to the understanding of inflammatory pathways and potential therapeutic interventions in this condition. -
PDE4 Inhibitor
ONO-6126 is a selective phosphodiesterase 4 (PDE4) inhibitor with potential therapeutic applications in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). By inhibiting PDE4, it increases intracellular cAMP levels, which can help reduce inflammation and bronchoconstriction. This compound is valuable for research focused on understanding the molecular mechanisms of respiratory conditions and testing novel therapeutic strategies. -
PDE4 Inhibitor
Braylin is a potent phosphodiesterase-4 (PDE4) inhibitor that plays a significant role in anti-inflammatory and immunomodulatory processes. It is particularly relevant in the exploration of immunoinflammatory diseases, making it a valuable tool for researchers studying these conditions. Its ability to modulate inflammatory responses positions it as a potential therapeutic target in related research applications. -
PDE4 Inhibitor
RS-25344 is a selective inhibitor of phosphodiesterase type IV (PDE4), which plays a crucial role in the degradation of cyclic adenosine monophosphate (cAMP). By inhibiting PDE4 activity, RS-25344 promotes increased intracellular cAMP levels, contributing to an array of biological responses. This compound is valuable for research in inflammation, immune disorders, neurodegenerative diseases, and cardiovascular conditions. Its ability to modulate cAMP signaling makes it a significant tool for exploring therapeutic strategies in these areas. -
PDE5 Inhibitor
Desmethyl thiosildenafil is a selective phosphodiesterase type 5 (PDE5) inhibitor. This compound exhibits significant biological activity by promoting vasodilation through the inhibition of PDE5, thereby enhancing nitric oxide signaling. It is commonly used in research applications focused on cardiovascular function and erectile dysfunction, providing insights into the therapeutic potential for related disorders. -
PDE5 Inhibitor
JNJ-10258859 is a highly selective phosphodiesterase type 5 (PDE5) inhibitor, exhibiting a Ki value of 0.23 nM. This compound effectively elevates cyclic GMP levels, which is crucial for promoting smooth muscle relaxation and improving erectile function. JNJ-10258859 is primarily utilized in research focused on erectile dysfunction and related cardiovascular studies. -
PDE1 Inhibitor
MMPX is a potent phosphodiesterase type 1 (PDE1) inhibitor that modulates intracellular signaling pathways by increasing cyclic nucleotide levels. This compound exhibits significant biological activity in various cellular processes, making it a valuable tool for studying the physiological roles of PDE1 in neurological and cardiovascular research. Its application extends to exploring therapeutic strategies for diseases associated with dysregulated cyclic nucleotide signaling. -
PDE5 Inhibitor
BMS-341400 mesylate is a selective phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 value of 0.3 nM. This compound attenuates the degradation of cyclic guanosine monophosphate (cGMP), thereby facilitating nitric oxide (NO)-induced relaxation of corpus cavernosum smooth muscle and enhancing erectile function. BMS-341400 mesylate serves as a valuable tool for investigating mechanisms underlying erectile dysfunction. -
KRAS-PDEδ Inhibitor
NHTD is a selective inhibitor of KRAS-PDEδ, targeting the prenyl-binding pocket of PDEδ and modulating the cellular localization of KRAS. This action effectively inhibits the proliferation of KRAS-mutant cancer cells and promotes apoptosis. NHTD is a valuable tool for investigations into KRAS-driven non-small cell lung cancer (NSCLC) and related oncology research. -
Phosphodiesterase (PDE) Inhibitor
Saterinone is a phosphodiesterase III (PDE III) inhibitor that enhances intracellular cAMP levels, leading to increased vasodilation and improved cardiac function. This compound is significant in cardiovascular research, particularly in studies focused on heart failure and angina. Its role in modulating cAMP signaling pathways makes it an important tool for exploring therapeutic strategies in cardiovascular diseases. -
Phosphodiesterase (PDE) Inhibitor
PDE IV-IN-1 is a selective inhibitor of phosphodiesterase IV (PDE4), an enzyme involved in the degradation of cyclic AMP. This compound exhibits anti-inflammatory properties, making it valuable for the research of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD), as well as other inflammatory diseases. Its ability to modulate cAMP levels positions PDE IV-IN-1 as a significant tool in the study of inflammatory signaling pathways. -
Phosphodiesterase (PDE) Inhibitor
L791943 is a selective phosphodiesterase-4 (PDE4) inhibitor, demonstrating a potent inhibitory effect with an IC50 value of 4.2 nM. This compound is primarily utilized in research aimed at understanding the role of PDE4 in various inflammatory and neurological disorders. Its efficacy in modulating cyclic nucleotide levels makes it a valuable tool for studying signal transduction pathways and therapeutic interventions. -
Phosphodiesterase (PDE) Inhibitor
Sch59498 is a potent inhibitor of phosphodiesterase 1C (PDE1C), a phosphodiesterase enzyme involved in cellular signal transduction through the hydrolysis of cyclic nucleotides. This compound demonstrates significant effects on intracellular cAMP and cGMP levels, thereby influencing various physiological processes. Sch59498 is primarily utilized in research applications focused on cardiovascular diseases, neuroprotection, and cancer biology, providing insights into the modulation of signaling pathways associated with these conditions. -
Phosphodiesterase (PDE) Inhibitor
Win-62005 is a potent inhibitor of cyclic AMP phosphodiesterase III (PDE III), exhibiting Ki values of 25 nM for rat heart and 26 nM for canine aorta. This compound is primarily utilized in cardiovascular research to explore its effects on cAMP signaling pathways and its potential therapeutic applications in heart conditions. Through the inhibition of PDE III, Win-62005 enhances intracellular cAMP levels, thereby influencing myocardial contractility and vascular tone. -
PKCα Inhibitor
Leucosceptoside A is a phenylethanoid glycoside that functions as a selective inhibitor of Protein Kinase C alpha (PKCα). This compound demonstrates significant anti-hyperglycemic and anti-hypertensive effects and exhibits inhibitory activity against α-glucosidase, with an IC50 value of 19.0 μM. Leucosceptoside A is relevant for research into metabolic disorders and cardiovascular diseases, providing insights into therapeutic approaches targeting PKCα. -
ALOX12-ACC1 interaction inhibitor
IMA-1 is an inhibitor of the interaction between arachidonic acid 12-lipoxygenase (ALOX12) and acetyl-CoA carboxylase 1 (ACC1). This compound has demonstrated significant efficacy in blocking the progression of diet-induced non-alcoholic steatohepatitis (NASH) in male mice and crab-eating monkeys, while not inducing hyperlipidemia. IMA-1 serves as a valuable tool for investigating the underlying mechanisms and potential treatments for NASH. -
DHFR Inhibitor
4'-DTMP is a potent inhibitor of dihydrofolate reductase (DHFR), exhibiting Ki values of 5.1 nM for wild-type DHFR and 34.3 nM for the L28R variant. This compound features a polar modification that enhances local interactions with the enzyme, particularly affecting the hairpin structure of the M20 loop, which is crucial for internal communication within DHFR. Due to its inhibitory effects, 4'-DTMP may also have potential applications in targeting E. coli. -
DHFR Inhibitor
1954U89 is a potent, lipid-soluble inhibitor of dihydrofolate reductase (DHFR) with oral bioavailability. This compound demonstrates significant anticancer activity, making it a valuable tool in cancer research. Its ability to inhibit DHFR provides insights into folate metabolism and therapeutic strategies targeting rapidly proliferating cells. -
DHFR Inhibitor
WR99210 hydrochloride is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 of less than 0.075 nM. This compound exhibits significant antiparasitic activity, demonstrating efficacy against Plasmodium falciparum strains and Toxoplasma gondii. WR99210 hydrochloride serves as a valuable tool in research focused on parasitic infections and the development of new therapeutic strategies targeting DHFR. -
DHFR Inhibitor
Piritrexim is a potent dihydrofolate reductase (DHFR) inhibitor that demonstrates strong efficacy against Pneumocystis carinii and Toxoplasma gondii, with IC50 values of 0.038 and 0.011 μM, respectively. It has significant applications in AIDS research due to its ability to inhibit folate metabolism in pathogenic organisms. Additionally, Piritrexim exhibits anticancer properties, making it valuable for oncology research. -
DHFR Inhibitor
Fluorofolin is a potent dihydrofolate reductase (DHFR) inhibitor, demonstrating an IC50 of 2.5 nM. This compound exhibits significant antimicrobial activity against Pseudomonas aeruginosa, making it a valuable reagent for research in antibacterial drug development and mechanisms of resistance. Fluorofolin is suitable for studies involving folate metabolism and has potential applications in exploring therapeutic strategies targeting DHFR-related pathways. -
DHFR Inhibitor
Phomarin is a specific inhibitor of dihydrofolate reductase (DHFR), an enzyme critical for folate metabolism. It demonstrates potential antimalarial activity, making it a valuable tool for research in malaria treatment and prevention. Its mechanism of action supports further investigations into antifolate strategies and their implications for drug development. -
DHFR Inhibitor
DHFR-IN-5 is a highly potent and orally bioavailable inhibitor of dihydrofolate reductase (DHFR), exhibiting a Ki value of 0.54 nM against the quadruple mutant strain of Plasmodium falciparum DHFR. This compound demonstrates significant anti-malarial activity, making it a valuable tool for research into malaria therapeutics and the study of resistance mechanisms in Plasmodium species. -
DHFR Inhibitor
Epiroprim is a selective inhibitor of dihydrofolate reductase (DHFR), a key enzyme in folate metabolism. It exhibits potent antibacterial activity against various Gram-positive bacterial strains, including staphylococci, enterococci, pneumococci, and streptococci. Epiroprim is commonly utilized in research applications focused on antimicrobial resistance and drug development strategies targeting bacterial infections. -
DHFR Inhibitor
Methotrexate diethyl ester is a potent inhibitor of dihydrofolate reductase (DHFR). This compound demonstrates significant biological activity in the context of T. cruzi infection and leukemia research, making it valuable for investigating therapeutic strategies in these disease areas. Its ability to inhibit DHFR underscores its potential applications in studies focusing on cancer and parasitic infections. -
DHFR Inhibitor
DHFR-IN-9 is a potent inhibitor of dihydrofolate reductase (DHFR), critically involved in purine and thymidylate biosynthesis, playing a significant role in cellular proliferation and growth. This compound demonstrates robust antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 with an IC50 of 0.25 μg/mL, as well as notable anti-infective effects in mouse models of systemic and thigh infections. Additionally, DHFR-IN-9 exhibits superior anticancer efficacy compared to paclitaxel in a mouse breast cancer model, administered at 2.5 mg/kg every three days. -
DHFR Inhibitor
DHFR-IN-8 is a potent dihydrofolate reductase (DHFR) inhibitor that disrupts purine and thymidylate biosynthesis, thereby impeding cell proliferation and growth. This compound exhibits significant antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300, with an IC50 value of 15.6 ng/mL. DHFR-IN-8 is applicable in research focused on tackling systemic infections and thigh infections in murine models. -
DHFR Inhibitor
DHFR-IN-22 is a potent inhibitor of Dihydrofolate Reductase (DHFR), classified as a 2,4-diaminopyrimidine compound. It demonstrates remarkable inhibitory activity against purified DHFR and key non-tuberculous mycobacterial species, including Mycobacterium avium and Mycobacterium abscessus, with IC50 values of 1.1 nM and 6.3 nM, respectively, and MIC values of 1.5 μg/mL and 0.1 μg/mL, respectively. In contrast, it exhibits a significantly higher IC50 of 2100 nM against human DHFR. DHFR-IN-22 is valuable for investigating therapeutic strategies to address NTM infections. -
DHFR Inhibitor
10-Deazaaminopterin is a potent inhibitor of dihydrofolate reductase (DHFR), an essential enzyme involved in folate metabolism. This compound has demonstrated significant anti-tumor activity and is primarily utilized in cancer research to investigate its effects on cellular proliferation and metabolism. Its application is particularly relevant in studies focusing on advanced cancer therapies and folate-dependent biochemical pathways. -
DHFR Inhibitor
DHFR-IN-24 is a dihydrofolate reductase (DHFR) inhibitor with a benzothiazole structure. This compound exhibits intrinsic antibacterial activity against Gram-positive and Gram-negative bacteria. Additionally, it demonstrates a synergistic effect when combined with photodynamic therapy (PDT), enhancing antibacterial efficacy against multidrug-resistant pathogens. Research applications include studying bacterial resistance mechanisms and developing novel antibacterial therapies. -
DHFR Inhibitor
DHFR-IN-5 hydrochloride is a potent inhibitor of dihydrofolate reductase (DHFR), exhibiting a Ki value of 0.54 nM against quadruple mutant Plasmodium falciparum DHFR. This compound demonstrates significant anti-malarial activity, making it a valuable tool for research in malaria treatment and drug development targeting DHFR pathways. -
DHFR Inhibitor
DHFR-IN-19 is a selective inhibitor of dihydrofolate reductase (DHFR) specifically targeting Trypanosoma brucei. With a Ki value of 9 nM, DHFR-IN-19 demonstrates significant antiparasitic activity, exhibiting an EC50 of 14.5 μM. This compound serves as a valuable tool for research into treatments for diseases caused by Trypanosoma brucei, particularly in the context of potential therapeutic applications against African sleeping sickness. -
DHFR Inhibitor
DDPO is a potent inhibitor of dihydrofolate reductase (DHFR) with an IC50 of 0.035 µM. This compound demonstrates significant anticancer activity by inhibiting the growth of L1210 and WI-L2 cell lines, with IC50 values of 5 µM and 0.28 µM, respectively. DDPO is primarily used in research applications focusing on cancer therapeutics and DHFR-related pathways. -
DHFR/TS Inhibitor
CB 3705 is a potent inhibitor of dihydrofolate reductase (DHFR) and thymidylate synthetase (TS). This compound demonstrates significant anti-cancer activity, exhibiting ID50 values of 4.77 μM against L1210 cells and 408 μM against the mutant L1210:C15 cell line. Its inhibition of key enzymes involved in nucleotide synthesis makes CB 3705 a valuable tool for cancer research and drug development. -
GSK3β Inhibitor
GSK3β-IN-3 is an ATP-competitive inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 0.90 μM. It effectively lowers the phosphorylation levels of tau protein in the BR5706 strain and reduces the accumulation of amyloid-beta (Aβ) aggregates in the CL2006 strain. This compound is essential for research applications focused on Alzheimer's disease (AD), aiding in the understanding of neurodegenerative mechanisms and potential therapeutic strategies. -
DHFR Inhibitor
Lysine-methotrexate is a dihydrofolate reductase (DHFR) inhibitor, structurally related to Methotrexate. This compound exhibits potent biological activity by inhibiting folate metabolism, making it useful in studying cellular processes that rely on nucleotide synthesis. Lysine-methotrexate is applicable in cancer research and other therapeutic contexts where modulation of DHFR activity is of interest. -
MtDHFR Inhibitor
DHFR-IN-2 is a potent uncompetitive inhibitor of MtDHFR (dihydrofolate reductase from Mycobacterium tuberculosis), demonstrating an IC50 value of 7 μM. This compound serves as a valuable tool for tuberculosis research, aiding in the study of pathogenic processes and potential therapeutic strategies against TB. -
DHFR Inhibitor
Denopterin is a dihydrofolate reductase (DHFR) inhibitor and an established antifolate agent. This compound functions as an antimetabolite, exhibiting cytotoxic effects on rapidly dividing cells, making it relevant for cancer research. Its ability to inhibit DHFR provides a valuable tool for investigating folate metabolism and developing therapeutic strategies against various malignancies. -
DHFR Inhibitor
TNP-351 is a dihydrofolate reductase (DHFR) inhibitor known for its potent antitumor activity. This antifolate compound exhibits efficacy against both leukemia and solid tumor cells in vitro and in vivo, making it a valuable tool in cancer research. Its mechanism of action involves the disruption of folate metabolism, ultimately hindering DNA synthesis and cell proliferation. -
SCDKI Pathway Inhibitor
SNX7 is a selective inhibitor of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. This compound plays a crucial role in studying cellular senescence and various CDKI-related diseases. By targeting the CDKI pathway, SNX7 serves as a valuable tool in cancer research and other conditions where cell cycle regulation is disrupted. -
Cathepsin L Inhibitor
Gallinamide A is a potent inhibitor of cathepsin L, demonstrating an IC50 value of 17.6 pM. This compound plays a crucial role in research applications focused on investigating the functions of cathepsin L in various biological processes, including protein degradation and immune response regulation. Its inhibitory activity makes Gallinamide A a valuable tool for studying the implications of cathepsin L in pathophysiological conditions. -
α-Glucosidase Inhibitor
DNJ-20 is an α-glucosidase inhibitor with an IC50 of 55.3 μg/mL, demonstrating significant broad-spectrum activity against SARS-CoV-2. It disrupts the endoplasmic reticulum-associated glycoprotein folding process, inhibiting proper processing of viral glycoproteins and consequently blocking viral particle formation and infection. DNJ-20 exhibits IC50 values as low as 1.49 μM against various SARS-CoV-2 variants, as well as HCoV-229E and HCoV-OC43. This inhibitor is suited for pan-coronavirus research applications. -
CYP2C1/CYP2C19 Inhibitor
CYP2C1/CYP2C19-IN-2 is a potent inhibitor of the CYP2C1 and CYP2C19 enzymes. This compound exhibits minimal hepatotoxicity and lacks Ames toxicity, making it a safer choice for research applications. CYP2C1/CYP2C19-IN-2 is particularly useful in studies investigating antiviral mechanisms against Zika virus (ZIKV). -
CYP2C9/CYP2C19 Inhibitor
CYP2C9/CYP2C19-IN-1 is a potent inhibitor of the cytochrome P450 enzymes CYP2C9 and CYP2C19. This compound exhibits key biological activity by effectively modulating drug metabolism pathways without hepatotoxic effects or Ames toxicity. It serves as a valuable tool for research applications, including studies on anti-Zika virus (ZIKV) therapeutics. -
MAO-A/B Inhibitor
Tedizolid phosphate sodium is a selective inhibitor of monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). This compound exhibits significant activity against Gram-positive bacteria, making it valuable in the study of antimicrobial resistance and the development of new therapeutic agents. Its mechanisms of action and inhibition properties facilitate research into neurological disorders and other conditions associated with monoamine dysregulation. -
α-glucosidase Inhibitor
1-Deoxynojirimycin hydrochloride is a potent α-glucosidase inhibitor, primarily utilized for modulating postprandial blood glucose levels. This compound demonstrates notable antihyperglycemic and anti-obesity effects, making it valuable in diabetes mellitus research. Additionally, 1-Deoxynojirimycin hydrochloride exhibits antiviral properties, contributing to its diverse applicability in metabolic and infectious disease studies. -
HMG-CoA Synthase Inhibitor
Hymeglusin is a fungal β-lactone antibiotic that functions as a potent inhibitor of HMG-CoA synthase, exhibiting an IC50 of 0.12 μM. This compound covalently modifies the active cysteine residue at position 129 of the enzyme, thereby disrupting its activity. Hymeglusin is primarily utilized in research applications focused on lipid metabolism and studying the modulation of cholesterol biosynthesis pathways. -
Phospholipase C Inhibitor, Angiogenesis Modulator
Neomycin is an aminoglycoside antibiotic known for its role as a phospholipase C (PLC) inhibitor and angiogenesis modulator. It effectively inhibits the nuclear translocation of angiogenin, resulting in reduced cell proliferation and angiogenesis. Additionally, Neomycin interferes with IP3-mediated calcium release and MgATP-dependent calcium uptake, influencing skeletal muscle calcium transients. Its ability to modulate crucial biological pathways makes Neomycin a valuable tool for cancer research and understanding microbial impact on health. Prolonged exposure may lead to adverse effects such as hearing impairment and kidney damage.
