Modulateurs d'enzymes

BCR-ABL1 tyrosine kinase inhibitor

Nicotinamide phosphoribosyl transferase (NAMPT) competitive inhibitor with IC50 = 3.1 nM. A major consequence of NAMPT inhibition is the attenuation of glycolysis at the GADPH step because this enzyme requires NAD+ for activity. The compound exhibits broad spectrum anti-cancer activity and significant tumor regression was observed in vitro. Although retinal and haematological toxicity has been associated with NAMPT inhibitors, LSN 3154567 does not lead to retinopathy in rats and can be mitigated with co-administration of nicotinic acid.

Inhibitor of dihydroorotate dehydrogenase; broad spectrum antiviral

Antagonist of Aurora A serine/threonine protein kinase; antineoplastic

novel tricyclic indole; promising new treatment for a variety of diseases

Inhibitor of protein kinase PKC

Inhibitor of VEGF receptor tyrosine kinases and non-receptor tyrosine kinases

A small molecule inhibitor with high selectivity for CDK8 over CDK19. Increases IL-10 production in stimulated human and murine macrophages and dendritic cells. Modulatory action on inflammatory responses has therapeutic potential.

Afatinib is a small molecule that inhibits the activity of cellular kinases that are involved in the progression of cancer. It is an Irreversible inhibitor of three members of the ErbB family. This molecule binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling which inhibits cellular growth and promotes apoptosis. It has been researched for the treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer and colorectal cancer. Afatinib 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 dopamine-?-hydroxylase

Inhibitor of IGF1 receptor

A selective inhibitor of MEK1/2 kinase. Anti-proliferative and pro-apoptotic in multiple myeloma (MM) cells via G0/G1 cell cycle arrest and caspase 3 and PARP cleavage, respectively. Synergistic with other anti-MM therapies. Has anti-tumor effects in some solid tumors, such as in K-ras mutated colorectal cancer.

LY-404039 is a potent metabotropic glutamate receptor agonist with nanomolar affinity for group II receptors mGluR2 (Ki = 149 nM) and mGluR3 (Ki = 92 nM). It modulates glutamatergic activity in limbic and forebrain areas and has antipsychotic properties in animal studies. LY-404039 represents a potential new therapy for neurophysiatric disorders including schizophrenia, psychosis and anxiety.

Human epidermal growth factor receptor 2 (HER-2)/epidermal growth factor receptor-2 (ErbB-2), is a key receptor linked to metastasis in tumours. The oncogenic ErbB-2 receptor has intrinsic receptor tyrosine kinase (RTK) activity. The receptor is activated by ligand binding which induces receptor dimerization. These RTK complexes can activate mitogen-activated protein kinase (MAPK) and phosphoinositol 3'-kinase (PI3K)/Akt pathways. This peptide has been identified as a substrate for HER-2/ErbB-2 as it is phosphorylated upon receptor activation and therefore acts as a marker for receptor activation in kinases assays.

Milrinone has an application for use in the treatment of heart failure. It has been shown to increase cardiac output and decrease left ventricular end diastolic pressure (LVEDP). Milrinone also increases the amount of oxygen delivered to the tissues by increasing cardiac contractility.  Milrinone 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 Bruton's tyrosine kinase (BTK)

Inhibitor of sodium/potassium ATP-ase; anti-arrhythmic

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

Pravastatin is an HMG-CoA reductase inhibitor that is used to lower lipid levels and manage cardiovascular events such as strokes and myocardial infarction. This drug inhibits HMG-CoA reductase allowing for a reduction in the level of cholesterol. Pravastatin sodium salt 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.

Diclofenac is a non-steroidal anti-inflammatory drug that is used to treat the signs and symptoms of arthritis and osteoarthritis. This drug inhibits COX-1 and COX-2 enzymes. As a result, it reduces pain and inflammation in joints. Diclofenac is usually used as a first line therapy for acute and chronic pain. Diclofenac sodium salt 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.