Modulateurs d'enzymes

Specific inhibitor of the ubiquitin specific protease-7 (USP7), which is a validated deubiquitinase of the E3 ubiquitin-protein ligase MDM2. The compound inhibits the USP7 deubiquitinase activity by binding to acidic amino acid residues important for the interaction with ubiquitin. Induces tumor cell death and enhances cytotoxicity of chemotherapeutic agents.

TDZD 8 is a selective, non-ATP competitive inhibitor of the glycogen synthase kinase GSK3β. TDZD 8 inhibits GSK3β with IC50 of 2 μM and was reported to not significantly affect Cdk-1/cyclin B, casein kinase CK-II, protein kinase A and C (PKA, PKC) activities. TDZD 8 was also identified as an inhibitor of the main protease in coronaviruses. In an in vitro study, TDZD 8 was characterised as an aggregate-based inhibitor as the presence of Triton-X decreased the inhibitory potency to Mpro protease of the SARS-CoV-2 virus (IC50 without Triton-X: 2.15 μM).

Cilastatin is a renal dehydropeptidase inhibitor drug that is used to prevent degradation of imipenem. It is used to treat a variety of infections in combination with imipenem. This drug blocks the mechanism of imipenem which is hydrolyzed by dehydropeptidase-I. Cilastatin sodium 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.

Crizotinib is a drug that belongs to the group of tyrosine kinase inhibitors. It is used in the treatment of cancers, including non-small cell lung cancer, small cell lung cancer, and other types of solid tumours. Crizotinib inhibits the activity of the tyrosine kinase ALK or anaplastic lymphoma kinase, which is involved in many signalling pathways and biological processes. The inhibition of this enzyme leads to decreased energy metabolism, reduced mitochondrial membrane potential and increased susceptibility to apoptosis. Crizotinib 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.

Potent inhibitor of phosphodiesterase type 9 (PDE9), tested in human and murine in vitro assays (IC50 values: 55 nM and 100 nM, respectively). BAY 73-6691 induces long-term potentiation and improves memory in rodents. BAY 73-6691 has been studied as a potential therapy for Alzheimer’s disease.

Inhibitor of proteaseγ‐secretase, which allows to modulate of the activity of γ‐secretase substrates Notch, E-cadherin, ErbB4, and amyloid precursor protein (APP). The compound can inhibit the growth of tongue carcinoma cells by arresting cell cycle in G0-G1 phase, modulate the activity of Notch1 receptor and Caspase-3 protease and induce apoptosis. It was also demonstrated that this inhibitor reduces the levels of β-amyloid peptide in the brain of mice model for Alzheimer’s disease. This compound also enhances the neuronal differentiation embryonic cells.

Potent inhibitor of β5i subunit of immunoproteasomes (IC50 = 6.6 nM), selective over β5c subunit (IC50 = 287 nM). The β5i subunit of immunoproteasomes (iCPs) is the chymotrypsin-like active sites that have implications on anti-cancer affects. On the other hand, β5c subunits are found in constitutive proteasomes (cCPs).

Aminopterin is an antineoplastic agent and antifolate, which is a synthetic derivative of pteroylglutamic acid. It functions as a chemotherapeutic agent by inhibiting dihydrofolate reductase, an enzyme crucial in the folic acid pathway, thereby preventing the conversion of dihydrofolate to tetrahydrofolate. This disruption leads to impaired synthesis of purine nucleotides and thymidylate, which are essential for DNA synthesis and cell division. Aminopterin is primarily used in cancer research and treatment due to its ability to halt the proliferation of rapidly dividing cells. It has historical significance as one of the initial antifolates developed and was utilized in the treatment of leukemia and other malignancies. However, due to its toxic side effects and the development of safer folate antagonists like methotrexate, its clinical use has been limited. Today, aminopterin's role is more focused within research settings, contributing to the understanding of cell biology and cancer pathways.

Olaparib is a small molecule inhibitor of DNA polymerase and topoisomerase, which are enzymes that maintain the integrity of DNA. Olaparib inhibits the proliferation of cancer cells by preventing the synthesis of DNA, RNA, and proteins. Olaparib has been shown to be effective against breast cancer tissues in mouse models. It also has minimal toxicity in humans and has been shown to inhibit the growth of diseased cells with significant cytotoxicity. Olaparib 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.

Iproniazid is an irreversible monoamine oxidase inhibitor of the hydrazine class. It was initially used for the treatment of tuberculosis however now it is used for the treatment of depression. Iproniazid inhibits the activity of monoamine oxidases (MAOs) by itself and through an active metabolite, isopropylhydrazine. Additionally, it prevents the enzymatic breakdown of norepinephrine. Iproniazid 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.

A cell permeable inhibitor of oligosaccharyltransferase that interferes with the transfer of mature glycan precursors to recipient proteins. Causes reduced proliferation, G1 arrest and senescence in EGFR- and FGFR-dependent non-small-cell lung carcinoma (NSCLC) cells.

SD 0006 is a small-molecule inhibitor, which is synthesized through specialized chemical processes. It functions by selectively inhibiting the cyclooxygenase-2 (COX-2) enzyme, which plays a significant role in the inflammatory pathway. This inhibition reduces the production of pro-inflammatory prostaglandins, ultimately leading to a decrease in inflammation. In scientific research, SD 0006 is primarily utilized in the study of inflammation-related diseases. It serves as a valuable tool in elucidating the pathways and physiological mechanisms involved in diseases such as rheumatoid arthritis, osteoarthritis, and other inflammatory conditions. By targeting COX-2, SD 0006 helps to understand the differential effects of COX inhibition and the balance between therapeutic efficacy and potential side effects. Its applications extend to in vitro cellular assays as well as in vivo animal models, providing insights into the development of new anti-inflammatory therapeutics. The specificity and mode of action of SD 0006 make it an essential component in both pharmacological studies and the broader field of biomedical research.

Potent inhibitor of γ-secretase. LY 411575 inhibited production of amyloid β (Aβ) peptides with IC50 of 0.078 nM in vitro as well as decreased levels of Aβ40 and Aβ42 amyloids in brain of a mouse model for Alzheimer’s disease. In vitro studies confirmed that LY 411575 inhibited cleavage of Notch receptor at S3 site with IC50 of 0.39 nM, which blocked Notch activation and downstream signalling, leading to apoptosis in primary and immortalized Kaposi's sarcoma cells.

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.

Inhibitor of MEK kinase

H+/K+ ATPase inhibitor

Inhibitor of Factor Xa; anti-thrombotic

Baricitinib is a Janus kinase inhibitor (JAK) currently used as monotherapy in the treatment of rheumatoid arthritis. Barictinib is also recommened for the treatment of atopic dermatitis and systemic lupus erythematosus. In mice interestingly, the administration of baricitinib reduced the inflammatory effects induced by a high-sugar diet on the metabolism.

Cilastatin is a renal dehydropeptidase inhibitor, which is a compound sourced from synthetic processes designed to augment the pharmacokinetic profile of certain beta-lactam antibiotics. Its primary mode of action is to inhibit the enzyme dehydropeptidase I (DHP-I), located in the renal brush border. This enzyme typically degrades antibiotics, like imipenem, within the renal tubules. By inhibiting DHP-I, cilastatin prevents the inactivation of these antibiotics, thereby prolonging their active presence in the body and enhancing their antimicrobial efficacy. The key application of Cilastatin is in combination with the antibiotic imipenem, forming a synergistic therapeutic approach to treat severe bacterial infections. The pair, imipenem-cilastatin, is particularly effective against a wide range of Gram-positive and Gram-negative bacteria, including multidrug-resistant strains. Importantly, Cilastatin itself has no inherent antibacterial activity; its value lies solely in its ability to protect imipenem from renal degradation, ensuring optimal therapeutic concentrations are maintained during the treatment of complex infections.

Inhibitor of GSK3 kinase; activator of Wnt signalling