Modulatori enzimatici

COX-2 enzyme inhibitor; anti-inflammatory

<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>A potent and selective covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4). This receptor tyrosine kinase activates an oncogenic driver in hepatocellular carcinoma, the fibroblast growth factor 19 (FGF19). The FGFR4 inhibitor is therefore a promising candidate for the treatment of advanced liver cancer.</p>

<p>Inhibitor of metalloendopeptidase neprilysin</p>

<p>Tipifarnib is a farnesyltransferase inhibitor, which is a synthetic compound designed for experimental cancer treatment. It functions by targeting farnesyltransferase, an enzyme involved in the post-translational modification of proteins through the attachment of a farnesyl group to the protein's cysteine residue. This modification is crucial for the activity of several proteins, including those in the Ras signaling pathway, which is often dysregulated in cancer.</p>

<p>Inhibits c-MET tyrosine kinases</p>

<p>A selective inhibitor of PI3Kα. Inhibits cancer cell proliferation by blocking the G0/G1 phase of the cell cycle. Anti-tumor effect of BYL 719 has been demonstrated in models of tumors with PI3KCA mutation and amplification in vivo. BYL 719 also suppresses tumor growth in pre-clinical models of osteosarcoma.</p>

<p>Dual IGF-1R and InsR kinase inhibitor; antineoplastic</p>

Letrozole is an aromatase inhibitor drug that is used in the treatment of breast cancer in postmenopausal women. It is a non-steroidal type II inhibitor that blocks the active site and thus blocking the electron transfer chain of CYP19A1. As a result of this, the conversion of androgen to estrogen is inhibited.

<p>A potent non ATP-competitive inhibitor of MAP/ERK kinase (MEK). Has anti-tumor activity in melanoma and papillary thyroid cancer cells with B-Raf mutations. Enhances generation and survival of induced pluripotent stem cells (iPSCs).</p>

Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties.

<p>Caspase Modulator I, 1541 is a chemical compound designed to modulate the activity of caspases, a family of cysteine proteases critical in the regulation of apoptosis and inflammation. This product is synthesized through advanced chemical processes to ensure high specificity and potency. Its mode of action involves the selective inhibition and modulation of caspase activity, thereby influencing apoptotic pathways and immune responses.</p>

<p>Potent inhibitor of dual specificity tyrosine-phosphorylation-regulated kinase 3 (DYRK3) with IC50 value of 0.7 nM. Elevates hemoglobin and platelet levels in anemic mice.</p>