Enzyme Modulators

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.

Inhibitor of PARP1 and PARP2 enzymes

Inhibitor of tyrosinase in melanocytes: skin whitener

Dual COX/5-LO inhibitor; anti-inflammatory; analgesic

A selective and potent inhibitor of phosphodiesterase 2 (PDE2). Raises cAMP and cGMP levels in neurons, improves social recognition and object memory in murine animals. Reverses anxiolytic effects induced by oxidative stress in mice by blocking cGMP-PKG signaling.

γ-secretase inhibitor; reduces amyloid-β in brainÂ

Inhibitor of pan-class I PI3K family of lipid kinases; antineoplastic

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.

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.

Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.

Inhibitor of 5-lipoxygenase activating protein_x000D_

Inhibitor of protein kinase CK2

Polmacoxib is a non-steroidal anti-inflammatory drug (NSAID), which is derived through synthetic chemical processes. It functions as a selective cyclooxygenase-2 (COX-2) inhibitor. By selectively inhibiting the COX-2 enzyme, polmacoxib reduces the conversion of arachidonic acid to prostaglandins that mediate inflammation and pain, while sparing the COX-1 enzyme that protects gastric mucosa and maintains platelet function.