Activators & Inhibitors

2,6-Dimethylquinoline (Legacy Tebubio ref. 282T37784). 2,6-Dimethylquinoline is a natural product extracted from the roots of Peucedantu praeruptorum. 2,6-Dimethylquinoline is an inhibitor of CYP1A2 and CYP2B6 with an IC50 of 3.3 and 480 µM, respectively.

1-Palmitoyl-2-linoleoyl PE (Legacy Tebubio ref. 282T37785). Phosphatidylethanolamines are important components of cell membranes and biochemical pathways of fatty acid synthesis. 1-Palmitoyl-2-linoleoyl PE (PLPE) is one of the many phosphatidylethanolamines that may be present in cellular membranes. It has been used in studies involving the biosynthesis of anandamide via the phospholipase A2 (PLA2) and lysoPLD pathways. PLPE can also be used as a specific substrate to assess the activity of sPLA2-IIA in the presence of other phospholipids.

1-thio-β-D-Glucose (sodium salt) (Legacy Tebubio ref. 282T37786). 1-thio-β-D-Glucose is an analog of β-D-glucose in which sulfur replaces the hydroxyl group at the one position. The thiol group allows diverse chemical reactions, including click chemistry and polymerization. 1-thio-β-D-Glucose can be labeled with technetium-99m for analytical and diagnostic procedures. It can also be used as a substrate for glucose oxidase, which leads to the production of 1-thio-β-D-gluconic acid.

10-Nitrolinoleic acid (Legacy Tebubio ref. 282T37787). 10-Nitrolinoleate is the product of nitration of linoleate by NO-derived reactive species. Other nitrolinoleates detected in human plasma and urine include 9-, 12-, and 13-nitrolinoleate. Nitrolinoleates activate peroxisome proliferator-activated receptor γ (PPARγ; Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake. Nitrolinoleates can also be metabolized by smooth muscle cells to produce nitrite derivatives which in turn form NO, leading to increased cGMP production and smooth muscle relaxation. Through the same mechanism, nitrolinoleate-derived NO suppresses leukocyte adhesion, in part through nitrosation of CD40. Alteratively, nitrolinoleates can act independently of NO/cGMP and PPARγ signaling to suppress neutrophil and macrophage functions.

Resorufin benzyl ether (Legacy Tebubio ref. 282T37788). Resorufin benzyl ether is a fluorometric probe that acts as a substrate for cytochrome P450 (CYP)3A4. It is typically used near its apparent Km value of 30 μM to screen the inhibition/activation potential of test compounds, to predict potential drug-drug interactions, or to monitor other CYP450 activities. Upon enzyme cleavage, resorufin benzyl ether generates a red fluorescent product (ex. 571 nm/em. 585 nm).

Crocin II (Legacy Tebubio ref. 282T3779). Crocin II (Crocetin gentiobiosylglucosyl ester) has anti-inflammatory and anti-apoptotic effects against gastric ischemia-reperfusion injury in rats, the effect of crocin is mainly mediated by reducing the protein expression of iNOS and caspase-3. Crocin II can ameliorate CCl4-induced liver injury via inhibition of inflammatory cytokines, caspase3 and oxidative stress along with modulation of liver metabolizing enzymes favoring elimination of CCl4 toxic metabolite. Crocin II has antihyperlipidemic effect, may be due to the inhibition of pancreatic lipase and crocin, and its metabolite, Crocin II , can improve hyperlipidemia. Crocin has antidepressant effects by increasing CREB, BDNF and VGF levels in hippocampus.

TAK-700 salt (Legacy Tebubio ref. 282T37790). TAK-700 salt is a potent and highly selective inhibitor of human 17,20-lyase with an IC50 of 38 nM and is over 1000-fold more selective than other CYPs such as 11-hydroxylase and CYP3A4.

A-971432 (Legacy Tebubio ref. 282T37791). A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 &#181M, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 &#181M) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s disease when administered at a dose of 0.1 mg/kg.[1] [2] A-971432 (0.1 mg/kg per day, i.p.) decreases the number of errors made in a horizontal ladder task and increases latency to fall in the rotarod test in R6/2 mice. It also increases spontaneous alternation in the t-maze in aged mice when administered at a dose of 0.1 mg/kg.[1]

A2A receptor antagonist 1 (Legacy Tebubio ref. 282T37792). A2A receptor antagonist 1 (CPI-444 analog) is an inhibitor of the adenosine A2A receptor and A1 receptor with Ki values of 4 nM and 264 nM, respectively.