Ligands organométalliques

Brinzolamide is a carbonic anhydrase inhibitor this is used for the treatment of ocular hypertension and glaucoma. Inhibition of carbonic anhydrase slows the formation of bicarbonate ions and as a result of this, it slows fluid flow in the eye, lowering the intraocular pressure. It has a high lipophilicity to enable diffusion across the blood-retinal barrier.

Celecoxib is a pyrazole derivative that acts as a selective COX-2 inhibitor. It has been shown to inhibit prostaglandin synthesis and promote apoptosis in human osteosarcoma cells. Celecoxib also inhibits tumor growth and inhibits angiogenesis in combination with paclitaxel, which is a chemotherapeutic agent. It is a nonsteroidal anti-inflammatory drug, thus a beneficial treatment in conditions such as rheumatoid arthritis, osteoarthritis, musculoskeletal pain, acute pain and juvenile rheumatoid arthritis. Furthermore it can be utilized in patients with familial adenomatous polyposis to reduce colon and rectal polyps.
Celecoxib 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.

Capecitabine is a chemotherapeutic agent that is used in the treatment of various cancers such as gastrointestinal, breast and pancreatic. This drug is a nucleotide metabolic inhibitor and inhibits DNA synthesis and slows the growth of tumor tissue. It is a prodrug of Fluorouracil.

Clioquinol is an antifungal drug and antiprotozoal drug that has been shown to inhibit the activity of protein kinase-3 and to promote apoptosis. This compound has also been found to improve iron homeostasis, which may be due to its ability to counteract the effects of oxidative stress on the mitochondria. Additionally, it has been shown to have anti-fungal properties against opportunistic fungal pathogens such as Candida albicans. Clioquinol is extracted from a plant called "Clioquinia rosea" and is produced by a chemical reaction with 2-chloroethanol.

Class 1 PI3K enzyme inhibitor; anti-neoplastic

A potent inhibitor of histone deacetylases (HDACs) of class I and II with anti-tumoral activity. The compound blocks HDAC catalytic activity by chelating zinc ion in the enzyme’s active site. Extensively used in research as epigenetic modifier able to block cell growth and downregulate proliferation-associated factors. It has also been reported that trichostatin A induces apoptosis via a histone-modification independent mechanism in oral squamous cell carcinoma cell lines. Initially discovered as anti-fungal compound from Streptomyces hygroscopicus for the control of fungal infections caused by the genus Trichophyton.

Dofetilide belongs to the class of antiarrhythmic agents. It is a class III antiarrhythmic agent, which acts by blocking the potassium ion channels in the heart. It is used for the management of normal sinus rhythm and in atrial fibrillation. In vitro studies have shown that Dofetilide can prevent arrhythmias resulting from experimental models of congestive heart failure and can prevent re-entry mechanisms that lead to tachycardia.

Aliskiren is a drug that belongs to the group of angiotensin receptor blockers. It is a renin inhibitor that is used for the treatment of hypertension, congestive heart failure, and renal impairment. Aliskiren inhibits the action of angiotensin II by blocking the binding of this hormone to its receptors.

Tolvaptan is a vasopressin receptor antagonist. It binds to the V2 receptor in the cytosol and prevents it from activating the aquaporin 2 channel, which regulates water permeability. Inhibition of vasopressin receptors in the kidneys improves fluid and electrolyte balance. Tolvaptan has been shown to be effective for treating congestive heart failure, as well as other disorders that are associated with fluid retention, such as renal dysfunction and metabolic syndrome. Tolvaptan can also be used in combination therapy with other drugs to treat these conditions.

Anti-inflammtory drug

Inhibitor of monoamine oxidase

GABA reuptake inhibitor

Inhibitor of topoisomerase TOP2

Topoisomerase II and DNA helicase inhibitor

Competitive, reversible inhibitor of α-glucosidases used for the control of postprandial hyperglycaemia in patients with type 2 diabetes mellitus. It inhibits digestive enzymes with α-glucosidase activity, which breakdown complex sugars to absorbable monosaccharides. It also reduces the levels of glycated haemoglobin (HbA1c).

Inhibitor of dipeptidyl peptidase IV; anti-diabetic agent

D8-MMAE is a chemical conjugate product, which is composed of the highly potent cytotoxic agent monomethyl auristatin E (MMAE) linked to targeting moieties, often through a stable linker. This product is synthetic in origin, derived from auristatins, which are analogs of dolastatin 10, a natural peptide isolated from marine organisms. The mode of action of D8-MMAE involves specific binding to cellular targets, typically through an antibody-drug conjugate (ADC) mechanism, where the conjugate binds to antigens on cancer cells. Once internalized, the linker is cleaved, releasing MMAE within the cell. MMAE then binds to tubulin, inhibiting cell division by disrupting the microtubule network, leading to apoptosis.

C18 Ceramide (d17:1/18:0) is a type of bioactive sphingolipid, which is synthesized endogenously and found in cell membranes. It is a specific form of ceramide, characterized by its unique acyl chain length and double-bond configuration. This compound is synthesized through the de novo pathway or generated via the hydrolysis of sphingomyelin, which is mediated by sphingomyelinases.

1-NM-PP1, also known as 1NM-PP1, is an inhibitor of the Src kinase. Studies have shown that 1-NM-PP1 inhibits analog-sensitive kinases (as-kinases) characterised by a small amino acid as gatekeeper of the ATP binding site. Tested to prevent parasitic infections, 1-NM-PP1 inhibited the Toxoplasma gondii life cycle when used at a higher concentration than 500 nM.

TAPI-1 is an inhibitor of TACE (TNF-α converting enzyme, also known as ADAM17) and matrix metalloproteinases (MMPs). It blocks the shedding of several cell surface proteins, including tumor necrosis factor-alpha (TNF-α), IL-6 receptor, and TNF receptors p60 (TNFRI) and p80 (TNFRII).