Modulateurs d'enzymes

Please enquire for more information about 5-Fluoro-1-(tetrahydro-2-furyl)uracil including the price, delivery time and more detailed product information at the technical inquiry form on this page

ATP-competitive inhibitor of Met and VEGFR2

Thymidylate synthase inhibitor

Inhibitor of ADAM10 metalloprotease

Inhibits MEK1 and MEK2 kinases; targeted therapy for melanoma

During extraction of lecithin from egg yolk, peptide by-products can be isolated and purified by gel filtration. Within the by-products this has led to the discovery of biologically active value-added products. The egg yolk gel filtration (EFGF) fractions were analysed for their antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. EYGF-33 predominantly contained 3 peptides - KLSDW, YPSPV, and MPVHTDAD). KLSDW in EYGF-33 was found to have strong antioxidant activity linked to the presence of the tryptophan residue. KLSDW had nearly comparable activity to the synthetic antioxidant BHA. KLSDW did not show any notable angiotensin converting enzyme (ACE) inhibitory activity.

Rigosertib sodium is an experimental chemotherapeutic agent that is a derivative of benzyl styryl sulfone. It is synthesized chemically and functions primarily by inhibiting key signaling pathways involved in cancer cell proliferation. Specifically, Rigosertib targets the RAS signaling pathway along with the phosphatidylinositol-3-kinase/AKT and polo-like kinase 1 (Plk1) pathways, impeding the progression of the cell cycle and inducing apoptosis in malignant cells. Rigosertib sodium is under investigation for its potential application in treating hematological malignancies and solid tumors, particularly myelodysplastic syndromes (MDS) and pancreatic cancer. By targeting multiple pathways that are typically upregulated in cancer cells, Rigosertib offers a mechanism by which cancer growth may be curtailed, providing a promising strategy for therapeutic intervention. Although primarily studied in the laboratory and clinical trial settings, ongoing research aims to elucidate its efficacy and safety profile, with hopes of integrating it into standard cancer treatment regimens upon successful validation.

Histone acetyltransferase inhibitor of p300/CBP; anti-proliferative

Inhibitor of ERK1 and ERK2 serine/threonine kinases

AMARA peptide is a fragment containing the phosphorylation site for AMP activated protein kinase (AMPK) and is a substrate for all AMPK subfamily kinases. As such it is used to measure AMPK related kinase activity.

Inhibitor of dihydroorotate dehydrogenase; anti-inflammatory; immunomodulatory

Inhibitor of glutaminase; glutamine analogue

NADPH oxidase inhibitor; anti-inflammatory

Inhibitor of mutant B-rafV600E protein that results in decreased proliferation of cancer cells with this mutation. Treatment of metastatic melanoma in patients harboring the V600E mutation, had improved disease outcome. This antitumor activity is enhanced when combined with MEK inhibitor trametinib.

Nociceptin/orphanin FQ peptide receptor antagonist

Inhibitor of p38 kinase

Cyclosporin G is an immunosuppressive agent, which is derived from fungal sources with a specific mode of action that involves inhibiting calcineurin. The source of Cyclosporin G is primarily from the fermentation of the fungus *Tolypocladium inflatum*. Its mode of action involves binding to the cytosolic protein cyclophilin in T-lymphocytes, which subsequently inhibits the phosphatase activity of calcineurin. This inhibition prevents the dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT), thereby reducing the transcription of interleukin-2 and other cytokines critical for T-cell activation. The primary use of Cyclosporin G is in preventing organ transplant rejection by suppressing the immune response. It is also being explored for potential applications in treating autoimmune diseases, where dampening the immune system can be beneficial. Ongoing research is investigating its pharmacokinetics and possible advantages over similar compounds, such as Cyclosporin A, focusing on its efficacy and side effect profile. Researchers in pharmacology and transplant immunology continue to study Cyclosporin G for its clinical applications and understand its broader impacts on immune modulation.

Fludarabine triphosphate trisodium is a nucleotide analog, which is a type of chemotherapy agent derived from purine nucleosides. This compound is the active metabolite of fludarabine, sourced from synthetic chemistry designed to mimic naturally occurring nucleotides involved in DNA replication. The mode of action involves its incorporation into the DNA strand during replication, where it effectively inhibits DNA polymerase and ribonucleotide reductase. This disruption impairs DNA synthesis, leading to apoptosis or programmed cell death, particularly in rapidly dividing cancer cells. The principal use of fludarabine triphosphate trisodium is in the treatment of hematological malignancies such as chronic lymphocytic leukemia (CLL) and, in certain cases, non-Hodgkin lymphoma. Its application is especially relevant in settings where conventional therapies might be less effective or where a nucleoside analog is particularly indicated. As a chemotherapeutic agent, it requires careful management due to its immunosuppressive profile, which is a critical consideration in the comprehensive care of patients undergoing treatment. Researchers continue to investigate its use in combination therapies aimed at enhancing efficacy while minimizing adverse effects.

Cell permeable peptide which is able to activate phosphoinositide 3- kinase, for which it binds with high affinity to the p85 subunit. 740 Y-P also has mitogenic activity as it is able to induce mitosis in muscle cells, and promotes cell survival in neurones. PI 3- kinase's are a family of enzymes involved in many cellular pathways including cell proliferation, growth, differentiation, survival, motility, and intracellular trafficking. PI 3 Kinases are therefore also involved in many cancers.

Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) and its negative regulator Kelch-Like ECH-Associated Protein 1 (Keap1) provide vital protection in maintaining cellular redox. In parallel, Nrf2 also aids the resolution of inflammation and also tissue repair. In homeostatic conditions, the transcription factor Nrf2 is controlled in a cytoplasmic complex with Keap1 with ubiquitination and protein degradation. Nrf2 has been linked to numerous cancers due to mutations affecting the binding region of Nrf2 to Keap1, resulting in Nrf2 dissociating from the complex. Nrf2 constitutively accumulates in the nucleus and activation of prosurvival genes that promote cancer cell proliferation.The Neh2 region of Nrf2 interacts with Keap1, as shown by nuclear magnetic resonance spectroscopy. The 16 amino acid peptide (AFFAQLQLDEETGEFL) (69-84) flanks the conserved ETGE motif and can replicate the binding to keap1.Therapeutics targeting the Nrf2 signalling pathway and activation of Nrf2 is a keen area of research, with many cancers being linked to Nrf2, particularly pancreatic cancer. Additionally, activation of Nrf2 has become a possible target as a treatment for COVID. Nrf2 (69-84) replicating full-length Nrf2 binding has been helpful in all cases.