Modulatori enzimatici

<p>Ligand of plasminogen; used for bleeding control</p>

<p>Selective inhibitor histone methyltransferases SUV420H1 and SUV420H2 (IC50 values = 25 nM and 144 nM, respectively). Reduces histone H4K20me2 and H4K20me3 expression whilst increasing H4K20me1 global expression. Inhibits formation of p53-binding protein 1 (53BP1) foci upon ionizing radiation and reduces NHEJ-mediated DNA-break repair.</p>

<p>5-HT6 serotonin receptor antagonist; anti-convulsant</p>

Inhibitor of NPM-ALK kinase

Inhibits Akt translocation by targeting the pleckstrin homology (PH) domain. Inhibits hepatitis C virus NS5B RNA-dependent RNA polymerase (IC50 = 79 µM). Attenuates cannabinoid agonist-mediated proliferation of neural stem/precursor cells.

Angiotensin-converting enzyme inhibitor; antioxidant

MG 132 is a modified tripeptide that acts as proteasomal inhibitor. In 2006, MG 132 has been experimentally tested in in vitro cell-based and in vivo models for to assess its use in the medical treatment of Parkinson's disease.

<p>SU 3327, originally introduced as a thiadiazole JNK inhibitor (De et al. 2009) has recently been identified as having antibiotic activity against a broad range of bacteria including drug-resistant gram positive and negative strains (Strokes et al. 2020). This molecule has been given the fictional name ‘Halicin’ inspired by the AI approach used to discover its novel biological activity.</p>

Sumoylation inhibitor; reported to inhibit histone acetylation transferase

<p>1-NM-PP1, also known as 1NM-PP1, is an inhibitor of the Src kinase. Studies have shown that 1-NM-PP1 inhibits analog-sensitive kinases (as-kinases) characterised by a small amino acid as gatekeeper of the ATP binding site. Tested to prevent parasitic infections, 1-NM-PP1 inhibited the Toxoplasma gondii life cycle when used at a higher concentration than 500 nM.</p>

<p>Binds to FK506 binding proteins (FKBPs) to form a complex that inhibits mammalian targets of rapamycin (mTOR). Blocks p70 S6 kinase activation by interleukin-2 and thereby inhibits proliferation of T cells. Induces differentiation of human pluripotent stem cells (hPSCs) to mesendoderm and blood progenitor cells.</p>

Small molecule antagonist of heparan sulfate that binds to glycosaminoglycans electrostatically. Surfen neutralised anti-coagulant activity of unfractionated and low molecular weight heparins, inhibited enzymatic sulfation and degradation reactions. Surfen also blocked signalling and cell adhesion to fibronectin that was triggered by heparan sulphate.

<p>Potent and specific inhibitor of checkpoint kinase CHK2 with IC50 of 3 nM. CCT 241533 binds to the ATP pocket of CHK2 and shows minimal cross-reactivity against related kinases. CCT 241533 blocked the activity of CHK2 and impaired DNA repair in response to DNA damage in human tumoral cell lines. The compound did not potentiate genotoxicity of several genotoxic compounds but it did potentiate the cytotoxicity of a PARP inhibitor olaparib.</p>

Tyrosine kinase inhibitor; affects EGFR receptor; pancreatic cancer treatment

Simvastatin Na is the salt form of Simvastatin. It acts as HMG-CoA reductase inhibitor and suppresses TNF-mediated NF-kappaB activation.

<p>Inhibitor of HMG-CoA reductase</p>

<p>Inhibitor of FLT3 kinase and acid sphingomyelinase</p>

<p>Tolcapone is a catechol-O-methyltransferase (COMT) inhibitor that is used as adjunct therapy to manage symptoms of Parkinson’s disease. Although its precise mechanism is unknown, it is thought to be an inhibitor of COMT and allows for a greater reduction in the symptoms of Parkinson’s.</p>

<p>Inhibitor of ADAM10 metalloprotease</p>

<p>Tegafur is an antineoplastic agent that is used for the treatment of gastric and colorectal cancers in combination with other medications. This drug is a prodrug of 5-fluorouracil and has anticancer properties by inhibiting thymidylate synthase during DNA synthesis. Additionally, Tegafur causes disruptions of RNA functions.<br><br>Tegafur 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>