Enzyme Modulators

Mevastatin is a drug that inhibits the synthesis of cholesterol and has been used to treat hypercholesterolemia. It binds to the hydroxyl group at position 3 on the mevalonate molecule, which prevents the formation of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) and consequently reduces the production of cholesterol. Mevastatin has been shown to inhibit mitochondrial functions in wild-type strain yeast cells and myeloma cell lines, which may be due to receptor activity.

Parecoxib is a COX-2 inhibitor and belongs to the group of pharmacological agents. It is a prodrug of valdecoxib that is used for the treatment of osteoarthritis and rheumatoid arthritis, as well as other conditions where the reduction in pain and inflammation are desired.

Inhibits lysophosphatidylserine hydrolysis by the integral membrane serine hydrolase ABHD12 (IC50 = 1.3 µM). Raised levels of lysophosphatidylserine were observed in mouse brain in vivo and in primary human macrophages. DO 264 had proinflammatory effects, following infection with lymphocytic choriomeningitis virus (LCV) clone 13 in mice, resulting in severe inflammatory lung damage.

Nafamostat is a broad-spectrum serine protease inhibitor produced by chemical synthesis. Nafamostat is effective through its antioxidant and anti-inflammatory activity. This drug is involved in inhibiting various enzyme systems such as coagulation and fibrinolytic systems.

Inhibits Jak kinases; immunosuppressive; anti-inflammatory

Potent inhibitor of phosphodiesterase type 9 (PDE9), tested in human and murine in vitro assays (IC50 values: 55 nM and 100 nM, respectively). BAY 73-6691 induces long-term potentiation and improves memory in rodents. BAY 73-6691 has been studied as a potential therapy for Alzheimer’s disease.

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.

Potently inhibits PARP-1 and PARP-2 enzymes, orally bioavailable and crosses blood-brain barrier. Sensitises cancer cells to DNA-damaging chemotherapy and radiotherapy. Combination therapies investigated in clinical trials for solid and blood malignancies.

Cilastatin is a renal dehydropeptidase inhibitor drug that is used to prevent degradation of imipenem. It is used to treat a variety of infections in combination with imipenem. This drug blocks the mechanism of imipenem which is hydrolyzed by dehydropeptidase-I.

A potent, reversible and slow-binding inhibitor of delta-5 desaturases (D5Ds), by binding to the desaturase domain. Inhibiting D5D has therapeutic applications in inflammatory diseases. This is due to the increase in anti-inflammatory DGLA-derived eicosanoids and decrease in pro-inflammatory AA-derived eicosanoids.

Sildenafil is a potent inhibitor of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDE5), consequently preventing the degradation of cGMP in the smooth muscle cells of the pulmonary vasculature and penis. For this reason Sildenafil can be used to increase blood flow, decrease inflammation and mucus production in the lungs and also can be used in the treatment of erectile dysfunction in men. This is largely due to the increased availability of cGMP which can cause the relaxation of the smooth muscles to be prolonged.

Inhibitor of myosin?II?specific ATPase which blocks the myosin heads in an actin-detached state, disrupts contractility of myosin-actin filaments and stabilizes super-relaxed state of muscle fibres. It inhibits skeletal muscle myosin, non-muscle myosin II and heart muscle myosin.

PI3K/mTOR kinase inhibitor; anti-neoplastic

Inhibitor of FGFR kinase

Aurora kinase inhibitor

Inhibitor of cyclin dependend kinases

Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib tosylate has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib tosylate also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.
Sorafenib tosylate 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 Wnt signaling pathway by targeting porcupine, a membrane-bound O-acyltransferase involved in the palmitoylation and secretion of Wnt. Anti-cancer properties of LGK 974 have been demonstrated in various tumor models of breast cancer, head and neck squamous cell carcinoma and glioblastoma. Blocks LPS-mediated inflammatory response in epithelial and endothelial cells.

A potent and selective inhibitor of cell death-inducing kinase RIP2 (IC50 = 5 nM). Reduces release of pro-inflammatory cytokines. Inhibits production of TNF-α and IL-6 in intestinal explants from patients with Crohn's disease and ulcerative colitis.

Inhibitor of the histone methyltransferase SETD8 that supresses methylation of the K20 residue in histone 4. UNC 0379 treatment of human glioma reduced recruitment of 53BP1 protein to double strand breaks and sensitised cells to radiotherapy without altering cell cycle kinetics.

Inhibitor of aurora kinases