Enzyme Modulators

IBMX is a competitive non-selective phosphodiesterase inhibitor that raises cAMP and activates PKA. It also inhibits TNFα and leukotriene synthesis. This chemical compound reduces inflammation and is an adenosine receptor antagonist. IBMX 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.

Nabumetone is a non-steroidal anti-inflammatory drug that is used in the treatment of osteoarthritis and rheumatoid arthritis. This drug is also a cyclooxygenase inhibitor and works by inhibiting this enzyme so that pain and inflammation is reduced. Nabumetone 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.

Azathioprine belongs to the group of immunosuppressant drugs that suppress the immune system by inhibiting the production of white blood cells (leukocytes). It is used to treat inflammatory diseases, such as rheumatoid arthritis, lupus, and Crohn's disease. Azathioprine is metabolized in the liver. Additionally, this drug inhibits DNA synthesis by binding to nuclear DNA, preventing RNA transcription and protein synthesis in susceptible cells. Azathioprine 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.

Rofecoxib is a non-steroidal anti-inflammatory drug that is used to treat osteoarthritis, acute pain and migraine attacks. This drug is also a COX-2 inhibitor. As a result, it reduces inflammation and pain. Rofecoxib 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 and specific inhibitor of checkpoint kinase CHK2 with IC50 of 3 nM. CCT 241533 binds to the ATP pocket of CHK2 and shows minimal cross-reactivity against related kinases. CCT 241533 blocked the activity of CHK2 and impaired DNA repair in response to DNA damage in human tumoral cell lines. The compound did not potentiate genotoxicity of several genotoxic compounds but it did potentiate the cytotoxicity of a PARP inhibitor olaparib.

Orlistat is a drug that has been approved for the treatment of obesity. It inhibits gastric and pancreatic lipases, which are enzymes that break down dietary fats into smaller molecules to facilitate absorption. Orlistat has been shown to reduce coronary heart disease in patients with type 2 diabetes. Orlistat has also been shown to have a significant upregulation of gene expression associated with disease activity when injected into the skin of patients with primary pulmonary hypertension. Orlistat 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.

MET tyrosine kinase inhibitor; anti-proliferative; pro-apoptotic

This product 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.

Axltide-is a substrate peptide for use in kinase assays and is based on the mouse insulin receptor substrate 1 (IRS1) (amino acid 979-989).IRS1 is a membrane-proximal adaptor protein, which binds to, and is phosphorylated by, the insulin receptor (IR) at its tyrosine residue. IRS1 transmits the extracellular signal for insulin to serine/threonine kinases, such as Akt which then deliver the signal into the cell to mediate the various actions of insulin.

Inhibitor of TGF-α, CTGF, ERK1/2, NF-κB and FasL; anti-inflammatory

Cyclosporine U is a cyclic polypeptide immunosuppressant, which is a derivative of the natural product Cyclosporine A, produced by the fermentation process involving the filamentous fungus *Tolypocladium inflatum*. It primarily acts by inhibiting the activity of calcineurin, a phosphatase enzyme, which in turn blocks the transcription of interleukin-2 and other cytokines. This mechanism suppresses the activation of T-lymphocytes, a crucial component in the immune response. Cyclosporine U is employed extensively in clinical settings to prevent organ rejection in transplant patients by modulating the immune response. It is also utilized in the treatment of various autoimmune diseases such as psoriasis and rheumatoid arthritis, where the immune system mistakenly attacks the body’s own tissues. Despite its clinical significance, careful monitoring of blood concentrations is essential due to its narrow therapeutic index and the potential for nephrotoxicity and other adverse effects. The development and refinement of derivatives like Cyclosporine U continue to be an active area of research aimed at enhancing efficacy and reducing side effects.

RIPK2 protein kinase inhibitor; EGFR inhibitor

Autocamtide-2-related inhibitory peptide is a calmodulin-dependent protein kinase II (CaMKII) inhibitor.CAMK represents a class of Ca2+/calmodulin-dependent protein kinase enzymes. CAMKs are activated by increases in the concentration of intracellular calcium ions (Ca2+) and transfers phosphates from ATP to defined serine or threonine residues in other proteins. Activated CAMK is involved in the phosphorylation of transcription factors and therefore, in the regulation of expression of responding genes.

Topoisomerase II inhibitor; chemotherapeutic drug

COX-2 enzyme inhibitor; anti-inflammatory

Inhibitor of topoisomerase TOP2

TAS 6417 hydrochloride is a small-molecule inhibitor, which is synthesized via chemical processes in pharmaceutical research. It functions primarily as a potent and selective inhibitor of specific mutant forms of the epidermal growth factor receptor (EGFR). By targeting these EGFR mutations, TAS 6417 hydrochloride disrupts the signaling pathways that are crucial for the proliferation and survival of cancer cells. The compound is primarily utilized in the context of scientific research for understanding and developing targeted cancer therapies, particularly in relation to non-small cell lung cancer (NSCLC). Researchers employ TAS 6417 hydrochloride to investigate the biochemical pathways and to test its efficacy and safety in preclinical models. The inhibitor's ability to target specific mutations positions it as a valuable tool in elucidating the mechanisms of resistance and sensitivity in cancer treatment strategies.

Inhibitor of 3β-hydroxysteroid dehydrogenase in steroid biosynthesis

Cyclooxygenase inhibitor; NSAID; an opthalmic analgesic

Inhibits FGFR family of kinases; antineoplastic; anti-angiogenic

Inhibitor of monoamine oxidase; anti-bacterial agent

Inhibitor of metalloendopeptidase neprilysin

Inhibitor of acetylcholinesterase

Inhibits tankyrase (TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively), by binding to the catalytic poly-ADP-ribose polymerase (PARP) domain. This stabilizes cytoplasmic protein Axin, mediating β-catenin depletion and thereby suppresses Wnt signalling pathway. XAV 939 has anti-proliferative and pro-apoptotic effects on neuroblastoma and colorectal cancer cells.

Potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 2.4 nM. Its anti-inflammatory activity was examined in a mouse model for acute colitis. The compound protected from intestinal inflammation by prevention of infiltration of CD19+ B-cells into the lamina propria of colonic epithelium and attenuated neutrophil activation. Its broad anti-inflammatory response involved decrease in 24 inflammatory chemokines and cytokines. Also, it is a potent inhibitor of cell proliferation in pancreatic cancer cell lines.

COX1 inhibitor; blocker of Ca2+-activated non-selective cation channels

Glucokinase activator

Fluvastatin is a statin that lowers blood cholesterol and triglycerides by inhibiting HMG-CoA reductase, an enzyme that plays a critical role in the synthesis of cholesterol. Fluvastatin has also been shown to reduce the incidence of myocardial infarction, and to reduce atherosclerotic lesions in animal models, reducing the incidence of cardiovascular disease. Fluvastatin also has been shown to inhibit the activation of toll-like receptor 4 (TLR4) by lipopolysaccharide (LPS), which may be related to its anti-inflammatory effects. Furthermore, through lowering blood cholesterol, Fluvastatin also inhibits tubulointerstitial injury and prevents renal damage caused by high concentrations of the lipid.  Fluvastatin 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.

Casein kinase (CK1ε and CK1Ύ) inhibitor

p38α MAP kinase inhibitor; JNK2α2 protein kinase inhibitor

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.

Inhibitor of COX1 cyclooxygenase

Lifirafenib is a targeted anticancer therapy, which is a small molecule inhibitor sourced through pharmaceutical development processes. Its mode of action involves the selective inhibition of the RAF kinase family, including B-RAF, which plays a critical role in the MAPK/ERK signaling pathway. By targeting these kinases, Lifirafenib effectively disrupts the aberrant signaling that contributes to tumor growth and survival in certain cancers with mutations such as BRAF V600E. Lifirafenib is primarily used in the treatment of cancers with identified aberrations in the RAS/RAF/MEK/ERK pathway, including certain forms of melanoma and thyroid and colorectal cancers. This drug holds therapeutic potential due to its ability to target specific genetic alterations, thereby providing a more personalized approach to cancer treatment. As with other targeted therapies, Lifirafenib is subject to ongoing clinical trials to better understand its efficacy, tolerability, and broader applications across various oncological indications.

MAP kinase kinase (MEK) inhibitor. Binds to MEK-1, preventing phosphorylation and activation by Raf or MEK kinase. PD 098059 enhances self-renewal in stem cells. Has anti-growth and anti-proliferative effects on AML cells. Anti-apoptotic effect on AML cells observed in synergy with Nutlin-3a.

Lenvatinib is a tyrosine kinase inhibitor that is used to treat cancers such as solid tumours. This drug inhibits the activity of VEGR receptors. It also inhibits other receptors such as fibroblast growth factor. Lenvatinib base 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 stearoyl-CoA desaturase SCD1 with IC50 of 6.3 nM, as measured in the SCD1-expressing human microsomes.  A 939572 exhibited anticancer activity as it reduced cell proliferation and triggered cell killing in human non-small cell lung carcinoma cells. A 939572 inhibited tumour growth in an in vivo model for gastric carcinoma and reduced the oleic acid:stearic acid ratio in mouse liver and plasma.

Inhibitor of ecto-ATPase which blocks the hydrolysis of nucleoside diphosphates and triphosphates in extracellular space. The compound inhibits NTPDase1, NTPDase 3, NTPDase 8 and NPP1and prolongs the effect of ATP on purinergic P2 receptors in environment with physiological concentrations of nucleotides. The compound has variable effectiveness as ecto-ATP inhibitor in mouse, rat, human and guineia pig tissues.

A potent Met kinase inhibitor (IC50 = 3.9 nM). Also inhibits Axl, Ron, and Tyro-3 (IC50 = 1.1, 1.8 and 4.3 nM, respectively). Anti-proliferative in Met-driven tumors in vitro and in vivo. Induces polyploidy in breast cancer cells and thereby chemoresistance.

Inhibitor of EGFR, HER2 and HER4 tyrosine kinases

Simvastatin is a lipid-lowering agent that belongs to the group of statins. It is prescribed for the treatment of hypercholesterolemia, coronary heart diseases, and other conditions related to high cholesterol levels. Simvastatin inhibits the production of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in the synthesis of cholesterol. Simvastatin 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.

Rivastigmine is a cholinergic agent that is used in the treatment of dementia in Parkinson’s and Alzheimer’s disease. This drug is a carbamate derivative that binds to and inactivates cholinesterase such as acetylcholinesterase and butyrylcholinesterase. This leads to an increase concentration of acetylcholine at cholinergic synapse. Rivastigmine tartrate 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.

This product 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.

VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic

Bestatin is a competitive protease inhibitor. It inhibits aminopeptidase N and is being studied for the use and treatment for acute myelocytic leukemia. Bestatin 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.

Etoricoxib is a cyclooxygenase-2 (COX-2) inhibitor, which is a type of nonsteroidal anti-inflammatory drug (NSAID). It works by blocking the enzyme COX-2 that is involved in the production of certain hormones called prostaglandins. These hormones are involved in the inflammation (swelling and heat) associated with conditions such as arthritis. By blocking the action of the COX-2 enzyme, Etoricoxib reduces the production of prostaglandins and thus, reduces the inflammation and pain. Etoricoxib 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.

Nilotinib is a kinase inhibitor that is used for the treatment of Chronic Myeloid Leukemia (CML). This drug is also used for the treatment of CML that is resistant to imatinib. Nilotinib inhibits the tyrosine kinase activity of the BCR-ABL protein. It also inhibits PDGFR and c-kit. Nilotinib HCl monohydrate 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.

Vorinostat is a histone deacetylase inhibitor which interferes with gene transcription regulatory mechanisms. It is used to treat cutaneous manifestations in patients with progressive, persistent, or recurrent cutaneous T- cell lymphoma (CTCL) following prior systemic therapies. This drug inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II). Vorinostat 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.

Anti-inflammatory; inducer of P450 II B family

PAC 1 is a small-molecule apoptosis inducer, derived from synthetic sources, with a unique mode of action targeting the apoptotic pathways in cancer cells. PAC 1 functions by selectively activating procaspase-3, an inactive precursor of the caspase enzymes, which play a crucial role in the execution phase of cell apoptosis. By facilitating the conversion of procaspase-3 to its active form, PAC 1 enhances the apoptotic response in cancer cells, promoting cell death and offering potential therapeutic advantages. In scientific research, PAC 1 is utilized extensively for its ability to sensitize cancer cells to apoptosis, making it a valuable tool in the development of cancer treatments. Its applications extend to studying apoptotic pathways and evaluating cancer cell responses to therapeutic agents. The specificity of PAC 1 for cancer cells over normal cells underscores its potential as a targeted therapeutic approach. Researchers are exploring its efficacy in combination with other chemotherapeutic agents to optimize cancer treatment regimens, aiming to reduce tumor resistance and improve patient outcomes.

Angiotensin-converting enzyme inhibitor