Enzyme Modulators

Inhibitor of chymotrypsin

A novel non-covalent inhibitor of the PLpro protease from SARS-CoV-2 and SARS-CoV viruses. GRL 0617 inhibits the proteolytic processing of the viral polypeptide. As PLpro also acts as a protease in pathways involved in innate immunity, there are indications that it can promote immunity against the virus.

Inhibits MET, VEGFR1-3, Tie and Ron tyrosine kinases; antineoplastic

MK 886 is a leukotriene antagonist that has been studied for use in treating atherosclerosis. This drug inhibits the 5-lipoxygenase activating protein thus inhibiting 5-lipoxygenase.

Inhibitor of ERK1 and ERK2 serine/threonine kinases

Inhibitor of activin receptor-like kinases (ALK4, ALK5 and ALK7), members of TGFβ type I receptor family. Blocks activin- and TGFβ-mediated signaling and phosphorylation of Smad2 downstream. Suppresses tumor-promoting and tumor-suppressing effects of TGFβ. Promotes differentiation of human embryonic stem cells (hESCs), whilst sustaining mouse ESCs in the undifferentiated state.

Selective inhibitor of the Src kinase family with subnanomolar IC50 values and good selectivity over c-Abl, PDGFRα and c-Kit kinases. The compound is effective in inhibiting growth in drug resistant cancer cell lines. In a recent study, it inhibited the growth of HER2-positive breast cancer cell lines which were resistant to pan-HER family kinase inhibitors such as lapatinib.

RET receptor tyroine kinase inhibitor

Rigosertib sodium is an experimental chemotherapeutic agent that is a derivative of benzyl styryl sulfone. It is synthesized chemically and functions primarily by inhibiting key signaling pathways involved in cancer cell proliferation. Specifically, Rigosertib targets the RAS signaling pathway along with the phosphatidylinositol-3-kinase/AKT and polo-like kinase 1 (Plk1) pathways, impeding the progression of the cell cycle and inducing apoptosis in malignant cells.

Inhibitor of cyclin-dependent kinases CDK4 and CDK6

Inhibitor of FLT3 and AXL tyrosine kinases

Sulindac is a non-steroidal anti-inflammatory drug that has anti-inflammatory and analgesic properties. It is used to relieve the pain of osteoarthritis and rheumatoid arthritis by reducing inflammation and inhibiting the production of prostaglandins, which are chemicals that cause inflammation.

Acetylcholinesterase inhibitor; therapy for Alzheimer's disease

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.

Inhibitor of carbonic anhydrase; muscle relaxant

Lovastatin is an HMG-CoA reductase inhibitor that is used to lower LDL cholesterol levels and to aid in the management of cardiovascular diseases. Animal studies have demonstrated that this drug has vasculoprotective properties.

Linagliptin is a dipeptidyl peptidase-4 inhibitor drug that is used to manage hyperglycaemia in patients with type 2 diabetes. This drug works by inhibiting the enzyme dipeptidyl peptidase-4 and allows for the breakdown of GLP-1 and glucose dependent insulinotropic polypeptide. As a result of this, breakdown of glycogen is reduced and release of insulin is increased. Linagliptin 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 factor Xa