Modulateurs d'enzymes

Inhibitor of Rho-kinases

Anti-rheumatic; immunosuppressant; neuroprotective; neuroregenerative

Inhibitor of FLT3 receptor tyrosine kinases; anti-neoplastic

Inhibitor of aurora kinases

Potent and selective MAP/ERK kinase 1/2 inhibitor. Reduces growth of tumor cells with B-Raf and Ras mutations. Tumor regression observed after chronic treatment in in vivo xenograft models. Enhances anti-tumor effect in combination with irinotecan or docetaxel.

Inhibitor of fibroblast growth factor receptors (FGFR1, FGFR2 and FGFR3). Demonstrated anti-tumor effects in pre-clinical models of FGFR-driven tumors. AZD 4547 resulted in tumor progression when applied on a patient-derived model of FGFR1-amplified squamous cell lung disease. Antineoplastic effects also observed in FGFR2-amplified gastric cancer.

(S)-Mephenytoin is a substrate of cytochrome P450 enzyme CYP2C19 (a hydroxylase). It is an effective anticonvulsant that improves control of seizures in patients. According to studies, the drug exhibits a genetic polymorphism in CYP2C19 that results in reduced metabolism in some individuals.  (S)-Mephenytoin 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.

O6-Benzylguanine is a guanine analog that is an antineoplastic agent. It works by acting as a suicide inhibitor of the enzyme O6-alkylguanine-DNA alkyltransferase. This results to an interruption of DNA repair so that damage can occur to local tumor targets. O6-Benzylguanine 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.

Dorzolamide is a carbonic anhydrase inhibitor agent that is used to treat eye disorders such as glaucoma and ocular hypertension. Dorzolamide decreases intraocular pressure by blocking the activity of aqueous humor outflow. Dorzolamide HCl 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.

Inhibits proto-oncogene Pim kinases (Pim-1, Pim-2 and Pim-3); antineoplastic

Omeprazole is a proton pump inhibitor (PPI) that inhibits the production of gastric acid in the stomach. This is due to Omeprazole binding through a stable disulphide bond to the H+/K+ ATPase enzyme found on parietal cells, and preventing hydrogen ion transport. Consequently, gastric acid secretion is supressed. As a PPI, Omerprazole can be used to treat disorders where gastric acid is over-secreted. Examples of these disorders are gastroesophageal reflux disease (GERD) and peptic ulcer disease. Omeprazole 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.

Specific inhibitor of 8-oxoguanine glycosylase OGG1 with IC50 in submicromolar range. The compound inhibits binding of OGG1 to its substrate 8-oxoguanine, a guanine analog generated in the presence of reactive oxygen species (ROS). It was shown that TH5487 decreases inflammation level by inhibiting the base excision DNA repair in mice and altering the OGG1 chromatin dynamics. The compound also has implications in cancer biology since OGG1 inhibitors sensitise tumours to chemotherapy.

Wee1 inhibitor with an IC50 of 5.2 nM

Immune suppressant; prevents pro-inflammatory cytokine release

Inhibitor of immunophilin FKBP12 and mTOR signalling with immunosuppressant activity. Zotarolimus inhibits proliferation of endothelial cells and smooth muscle cells and is employed in vascular interventional therapies.

Selective and reversible inhibitor of the multicatalytic 26S proteasome. The inhibition of protein breakdown affects several metabolic pathways and leads to cell death. The compound is effective in treating multiple myeloma because it prevents the binding of myeloma cells to bone marrow stroma and inhibits osteoclast differentiation.

Inositol monophosphatase (IMPase) inhibitor

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. 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&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 B-Raf kinase mutant

Indomethacin is a nonsteroidal anti-inflammatory drug that inhibits the production of prostaglandin PGE2. It is used to treat pain, fever, and inflammation. Indomethacin's mechanism of action is not well understood, but it may be due to interference with the ability of PMNs to bind to the surface of bacteria or to release reactive oxygen species. The drug has been shown to reduce mitochondrial membrane potential in mammalian cells, leading to apoptosis. This effect on mitochondria may also contribute to Indomethacin's anti-inflammatory effects. Indomethacin 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.