Modulateurs d'enzymes

Lisinopril is a drug that belongs to the group of angiotensin converting enzyme (ACE) inhibitors. It is used to treat hypertension, heart failure and myocardial infarction. Lisinopril binds to the active site of the ACE enzyme, preventing it from converting angiotensin I into angiotensin II. (S)-Lisinopril 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&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.

Sitagliptin is a drug that can be used to treat type 2 diabetes. This drug increases the production of an incretin hormone called glucagon-like peptide-1 (GLP-1) by stimulating the GLP-1 receptor. Sitagliptin is used in combination with metformin or a thiazolidinedione to improve glycemic control in patients with type 2 diabetes mellitus. Sitagliptin has been shown to improve postprandial blood glucose levels and reduce the risk of cardiovascular events. It also reduces the incidence of myocardial infarction and congestive heart failure in patients with type 2 diabetes who are already at high risk for these conditions. Sitagliptin phosphate monohydrate 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&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.

Seratrodast is a thromboxane receptor antagonist that is used to treat asthma. However, this drug does not affect thrombus formation as other thromboxane synthase inhibitors do such as ozagrel. Seratrodast 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&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.

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is negative regulator of hepatic low-density lipoprotein (LDL) receptors by promoting their degradation. This leads to an increase in plasma levels of cholesterol-LDL (LDL-c). PCSK9 binds to the LDL receptor at the epidermal growth factor precursor homology domain A (EGF-A) which leads the receptor to be targeted for degradation. Natural loss of function mutations in PCSK9 have been linked to improved coronary health and lower cholesterol levels with reduced risk of coronary heart disease. This has led to further study to find inhibitors of PCSK9 with the hope that they may be clinically relevant in the future.As discussed, PCSK9 binds to EGF-A on the LDL receptor. A peptide named pep 2-8 is a mimic of EGF-A and binds PCSK9 in the same manner observed with the LDL receptor. Pep 2-8 is a potent selective competitive inhibitor of PCSK9. Pep 2-8 restores LDL receptor function and LDL uptake of PCSK9-treated HepG2 cells. This is still an active area of research to optimise inhibition of PCSK9 for cholesterol regulation.Pep 2-8 has also been utilised as an anchor peptide in phage-display experiments to bind an extension peptide library to the groove site.Peptide Ac-TVFTSWEEYLDWV-NH2 is a Research Peptide with significant interest within the field academic and medical research. This peptide is available for purchase at Cymit Quimica in multiple sizes and with a specification of your choice. Recent citations using Ac-TVFTSWEEYLDWV-NH2 include the following: LDL-R promoting activity of peptides derived from human PCSK9 catalytic domain (153-421): design, synthesis and biochemical evaluation RH Alghamdi, P O'Reilly, C Lu, J Gomes - European journal of , 2015 - Elsevierhttps://www.sciencedirect.com/science/article/pii/S0223523415000422 Biological characterization of computationally designed analogs of peptide TVFTSWEEYLDWV (Pep2-8) with increased PCSK9 antagonistic activity C Lammi, J Sgrignani , A Arnoldi , G Grazioso - Scientific reports, 2019 - nature.comhttps://www.nature.com/articles/s41598-018-35819-0 Computational design and biological evaluation of analogs of lupin peptide p5 endowed with dual pcsk9/hmg-coar inhibiting activity C Lammi, EMA Fassi, J Li , M Bartolomei, G Benigno - Pharmaceutics, 2022 - mdpi.comhttps://www.mdpi.com/1999-4923/14/3/665 Molecular dynamics insights on the role beta-augmentation of the peptide N-terminus with binding site beta-hairpin of proprotein convertase subtilisin/kexin 9 B Pasam, KM Medicherla , RS Rathore - Chemical Biology & , 2019 - Wiley Online Libraryhttps://onlinelibrary.wiley.com/doi/abs/10.1111/cbdd.13612

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

Gastric proton pump inhibitor

Pemetrexed is a chemotherapy drug that belongs to the class of drugs called folate antimetabolites. It is used for the treatment of various cancers such as non-small cell lung cancer and pleural mesothelioma. Pemetrexed targets the enzymes thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. The drug works by inhibiting those enzymes so that the formation of DNA and RNA is prevented. Pemetrexed 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&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.

Aurora kinase inhibitor; antineoplastic

This peptide is phosphorylated by Janus kinase 1 (JAK1) and is an ideal substrate for use in kinase assays. The JAK family of kinases is essential for the signalling of a host of immune modulators in tumour, stromal, and immune cells where they are highly expressed. JAK family proteins mediate the signalling of the interferon (IFN), IL-6, and IL-2 families of cytokines.JAK kinases are associated with cytokine receptors. Cytokine binding to these receptors results in activation of JAK kinases and receptor phosphorylation. Phosphorylated cytokine receptors recruit STAT proteins, which are then phosphorylated by the activated JAK kinases. Phosphorylated STAT proteins form homo- and hetero-dimers that translocate into the nucleus and function as transcription factors.This JAK1 substrate peptide contains an N-terminal glycine-residue.

Sphingosine is a sphingolipid that can be found in human cells and plays an important role in signal transduction. Sphingosine is synthesized by the enzyme sphingosine kinase from sphinganine, which is a product of the breakdown of phospholipids. It also has a basic structure that can be used to inhibit the activity of protein kinases, such as PKC and Src, and tumor necrosis factor alpha. Sphingosine 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&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.

Inhibitor of caspases; broad spectrum

Inhibits interaction between small GTPase Rab27a and its effector JFC1 (synaptotagmin-like protein1, Slp1). These proteins regulate neutrophil exocytosis, decrease neutrophil infiltration in liver and kidneys and reduce extracellular ROS production by NAPDH oxidase. Thus, nexinhibib20 suppresses systemic inflammation.

Pentoxifylline is a methylxanthine derivative that is used to treat intermittent claudication that is caused by chronic occlusive arterial disease of the limbs. This drug also has antioxidant and anti-inflammatory properties. Pentoxifylline is a phosphodiesterase inhibitor aiding to increase levels of cAMP. Pentoxifylline 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&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.

PD 168393 is a potent and selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It is synthesized through advanced chemical processes, designed to specifically target and covalently modify the ATP-binding site of EGFR. The mode of action involves the irreversible binding to the cysteine residue in the ATP-binding pocket, leading to the inhibition of EGFR autophosphorylation and subsequent downstream signaling pathways. PD 168393 is primarily utilized in cancer research to investigate the role of EGFR in tumor development and progression. By effectively inhibiting EGFR activity, it serves as a valuable tool in studying the biological processes regulated by EGFR, as well as in the development of therapeutic strategies targeting EGFR-driven malignancies. Researchers apply PD 168393 in both in vitro and in vivo models to elucidate the mechanisms of action, resistance, and potential combination therapies in oncology.

Potent and specific inhibitor of the tyrosine protein kinase Mer precursor (MERTK) with 38-fold selectivity over the FMS-like protein kinase FLT3. UNC 4203 inhibits MERTK with an IC50 value of 2.4 nM and shows favourable pharmacokinetic properties. In vivo experiments in mice showed that UNC 4203 dramatically decreased the phosphorylation of MERTK in bone marrow leukemia cells.

Arbutin or alpha-arbutin is a natural product. It is a hydroquinone glucoside with antioxidant properties. It is widely used in cosmetics as depigmenting agent, acting as an inhibitor of tyrosinase in melanocytes. Arbutin acts by supressing the enzymes that stimulate these melanocytes without killing or fully inhibiting them. As a consequence, melanin production is decreased to avoid hyperpigmentation that might be caused by an excess of UV radiation or a higher activity of tyrosinases.

Inhibitor of HIF prolyl hydroxylase

An inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase that reduces total cholesterol and low-density lipoprotein (LDL). Cerivastatin is cardioprotective and anti-atherosclerotic. Cerivastatin inhibits the expression of the atherosclerotic genes monocyte chemoattractant protein-1 (MCP-1) and C-C chemokine receptor type 2 (CCR2), whilst inducing the expression of Kruppel-like factor 2 (KLF2).

Pamidronic acid is a bisphosphate used in the treatment of Paget’s disease, osteolytic bone lesions and in the treatment of hypercalcemia of malignancy. This drug inhibits farnesyl diphosphate and induces apoptosis of hematopoietic tumor cells. Pamidronic acid sodium salt hydrate 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&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.

Inhibitor of CKD1, CDK2, and CDK4 serine/threonine kinases