Irsogladine

背景介绍 Irsogladine is a selective PDE4 inhibitor that facilitates gap junction intercellular communication through muscarinic acetylcholine receptor binding. It is a potent inhibitor of angiogenesis in wild-type and plasminogen activator-deficient mice. Inhibition of PDE4 prevents the hydrolysis of cAMP, an important secondary messenger molecule that is heavily involved in signal transduction. 产品介绍 Phosphodiesterase 4 (PDE4) inhibitor that displays gastroprotective properties. Prevents gastric mucosal injury induced by monochloramine and ischemia-reperfusion. Activates gap-junctional intercellular communication improving gastric mucosal barrier function. Inhibits superoxide production in human neutrophils and inhibits in vitro and in vivo angiogenesis.

Dyphylline

背景介绍 Dyphylline is a selective A1 and A2 adenosine receptor antagonist. Decreases ABCG2 protein in cells and inhibits mPGES-1 (IC50 = 200 µM). Shows bronchodilatory and vasodilatory effects in vivo. 产品介绍 Dyphylline is a PDE inhibitor and a bronchodilator used to treat and/or prevent the symptoms of bronchial asthma, chronic bronchitis, and emphysema.

Cycloheximide

背景介绍 Cycloheximide has been reported to inhibit both the synthesis of proteins and macromolecules, as well as affect apoptosis in eukaryotes. Inhibition of protein synthesis is believed to be mediated through DNA translation arrest, as demonstrated in rat thymocytes. Although Cycloheximide has been reported to induce apoptosis in various cells, it has also been shown to inhibit or delay induced apoptosis. These observations suggest that Cycloheximide's effect on apoptosis may not be solely through protein translation arrest and that other mechanisms may be involved. Cycloheximide has also been reported to inhibit FKBP12 (peptidylprolylisomerase hFKBP12, PPIase hFKBP12) via competitive inhibition.

Cisplatin

背景介绍 Cisplatin induces cytotoxicity by interaction with DNA to form intrastrand crosslinks which activate several signal transduction pathways, including Erk, p53, p73, and MAPK, which culminates in the activation of apoptosis. Stimulates the immune responses by activating macrophages and other cells of the immune system. Cisplatin-treated macrophages show increased antigen presentation function in vitro. Treatment increased cellular NF-?B content and translocation in macrophages. 产品介绍 Potent anticancer agent that blocks DNA synthesis. Induces apoptosis via p53-dependent and -independent mechanisms. Inhibits X-linked inhibitor of apoptosis protein (XIAP) expression and activates caspase-3. In certain glioma cell lines, sensitizes cells to TNF-α-induced apoptosis.

Aminophylline

背景介绍 Aminophylline is a bronchodilator that is used together with other medicines to treat the acute symptoms of asthma, bronchitis, emphysema, and other lung diseases. Aminophylline is also a competitive adenosine receptor antagonist and it is thought to have potential therapeutic value for cardiac ischemia. 产品介绍 Aminophylline is a non-selective phosphodiesterase (PDE) inhibitor with an IC50 of 0.12 mM. Inhibition of PDE prevents the breakdown of secondary messenger molecules cAMP and cGMP, which play a vital role in signal transduction.

TAME-HCL

SL-01

产品介绍 Inhibits the p53-MDM2 interaction (20 µM). Inhibits U2Os cell growth (EC50=10 µM). Has also been shown to inhibit bovine chymotrypsin A-gamma.

1,10-Phenanthroline, Monohydrate

产品介绍 1,10-phenanthroline (o-phenanthroline) is a chelator with high affinity for divalent metal ions. When complexed with copper, it possesses nuclease activity that has been used to study DNA-protein interactions. While not specific for DUBs, it has been shown to be a potent inhibitor of JAMM-type isopeptidases through chelation of the active site Zn²⁺ ion. As such, o-phenanthroline is widely used when preparing cell lysates for enrichment of proteins bearing K63-linked polyubiquitin chains which are especially sensitive to DUBs in the JAMM family.

Nutlin-3

产品介绍 Cis-imidazoline analog that inhibits the interaction between p53 and its negative regulator MDM2 (IC50 = 0.09 µM). It induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53, but not in cells with mutated p53. Nutlin-3 also inhibits the growth of human tumor xenografts in nude mice by 90% at a dose of 200 mg/kg.