Modulateurs d'enzymes

<p>Inhibitor of ErbB2 (IC50 = 3 nM) and EGFR kinase (IC50 = 6.4 nM) with anti-proliferative effects. It inhibits ErbB2 receptor autophosphorylation and induces G1 cell cycle block. The CP 724714 treatment induces reduction of downstream ErbB2 receptor tyrosine kinase signalling, tumor cell apoptosis, release of caspase 3 and regression of tumors in in vivo and in vitro models.</p>

<p>Rensocatib is a reversible inhibitor of DPP-1, also known as cathepsin C, which is a peptidase involved in the activation of neutrophil, an elastase-like serine protease in lung tissue. Brensocatib is an oral drug used to treat infections of the airways (lungs) that are characterised by a permanent enlargement and presenting symptoms such as, coughing and greater mucus production (bronchiectasis). Alternative names of brensocatib are INS-1007 and AZD7986.</p>

<p>Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) used to reduce inflammation, relieve pain and reduce fever. The mechanism of action of ibuprofen has not been fully elucidated, but it may be due to inhibiting the enzyme cyclooxygenase and thus decreasing the synthesis of prostaglandins allowing a reduction of pain and inflammation.</p>

<p>Inhibitor of S-adenosylhomocysteine hydrolase that disrupts histone methylation by EZH2. Anti-proliferative in some breast cancer and invasive prostate cancer cell lines. One of four key molecules required for inducing chemical reprogramming of somatic cells into induced pluripotent stem cells (iPSC).</p>

<p>A cytidine analogue and inhibitor of DNA methyl transferases (DNMTs) with anti-cancer activity. This stable, hydrophilic compound forms covalent complexes between DNMT and zebularine-substrate DNA. It causes DNA lesions that block replication and cause replication fork collapse, leading to the formation of DNA double-strand breaks. It was also shown that zebularine-induced DNA methylation decrease in the IL-1β promoter region and disrupts molecular mechanisms of neuroinflammation. Moreover, this molecule down-regulates the DNA-methylation profile in the pluripotency genes’ promoters, which leads to improved development of somatic cell nuclear transfer (SCNT) embryos.</p>

<p>Inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2 and FGFR3). Demonstrated anti-tumor effects in pre-clinical models of FGFR-driven tumors. AZD 4547 resulted in tumor progression when applied on a patient-derived model of FGFR1-amplified squamous cell lung disease. Antineoplastic effects also observed in FGFR2-amplified gastric cancer.</p>

<p>Moclobemide is a monoamine oxidase inhibitor that is used to treat major depressive disorder and dipolar disorder. This drug’s mechanism of action involves the reversible inhibition of the enzyme MAO-A. The inhibition of this enzyme results in a decreased metabolism and destruction of neurotransmitters thus relieving the symptoms of depression and bipolar disorder.</p>

<p>Orally available prodrug of gemcitabine</p>

<p>Inhibitor of dopamine-?-hydroxylase</p>

<p>COX-2 enzyme inhibitor; anti-inflammatory</p>

<p>VEGFR tyrosine kinase inhibitor</p>

<p>Azathioprine belongs to the group of immunosuppressant drugs that suppress the immune system by inhibiting the production of white blood cells (leukocytes). It is used to treat inflammatory diseases, such as rheumatoid arthritis, lupus, and Crohn's disease. Azathioprine is metabolized in the liver. Additionally, this drug inhibits DNA synthesis by binding to nuclear DNA, preventing RNA transcription and protein synthesis in susceptible cells.</p>

<p>Imatinib is a tyrosine kinase inhibitor drug that is used for the treatment of various leukaemias, gastrointestinal stromal tumours and myeloproliferative disease. This drug inhibits the BCR-ABL tyrosine kinase and thus prevents the downstream phosphorylation of target proteins. This drug also inhibits PDGF, SCF and c-kit.</p>

<p>N-ω-Propyl-L-arginine is a selective inhibitor of neuronal nitric oxide synthase (nNOS). This enzyme is involved in the production of nitric oxide, which plays important roles in various physiological and pathological processes in the body. N-ω-Propyl-L-arginine selectively inhibits nNOS, preventing the conversion of L-arginine to nitric oxide. This makes it a useful tool for studying the role of nNOS in various Life Sciences fields, such as neuroscience and cardiovascular research. It can also be used as an enzyme modulator or ligand in drug discovery studies targeting nNOS.<br>N-ω-Propyl-L-arginine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Inhibitor of HIF-prolyl hydroxylase isozymes PHD1, PHD2 and PHD3 with Ki in nanomolar range. The compound mimics the binding of N-oxalylglycine, chelates catalytic iron and prevents substrate entry into catalytic site. Inhibition of PHD enzymes leads to stabilization of hypoxia-induced factors HIF1α and HIF2α, followed by the production of erythropoietin (EPO).</p>

<p>TAS 6417 hydrochloride is a small-molecule inhibitor, which is synthesized via chemical processes in pharmaceutical research. It functions primarily as a potent and selective inhibitor of specific mutant forms of the epidermal growth factor receptor (EGFR). By targeting these EGFR mutations, TAS 6417 hydrochloride disrupts the signaling pathways that are crucial for the proliferation and survival of cancer cells.</p>

<p>PI3K enzyme inhibitor; antineoplastic</p>

<p>Inhibitor of CDK4/6 serine/threonine kinases; antineoplastic</p>

<p>Inhibitor of prolyl 4-hydroxylase PHD</p>

<p>Inhibitor of FGFR kinase</p>