An N-cyanosulphonamide that selectively blocks the sodium/bicarbonate cotransporter (NBC, also known as SLC4A7) with a Ki value of 1.7 µM, with full inhibition occurring at ~30 µM in myocytes; prevents changes in pH associated with depolarization and hyperpolarization of ventricular myocytes.

An inhibitor of HDAC, including HDAC1 (IC₅₀ = 0.1-0.2 μM); induces growth suppression and cell death of certain types of cancer cells in culture.

A synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC?; selectively and reversibly inhibits the translocation of PKC? to intracellular membranes, blocking activation.

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

An activator of sGC that binds to a regulatory site, resulting in activation in an NO-independent manner (Kd = 3.2 nM); reduces hypertension, limits cardiomyocyte hypertrophy, protects against ischemia/reperfusion injury, and reduces morbidity and mortality in response to endotoxic shock.

Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…

C-6 NBD ceramide is a biologically active fluorescent analog of short chain, membrane-permeable ceramides. It is as effective as C-6 ceramide in the inhibition of viral glycoprotein transport through the Golgi. C-6 NBD ceramide has been used as a fluorescent substrate for the activity of…

CAS Number: 1228817-38-6 Molecular Formula: C₂₆H₃₆N₆O₃ Formula Weight: 480.6

A selective ERRβ/γ receptor agonist (EC₅₀ = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.

An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the α-linolenyl analog of MAFP has not been completely investigated.

A cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

A potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53); has been used in cells and in animals.

A cell-permeable ACL inhibitor (IC₅₀ = 0.13 µM) that has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.

A broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells; effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC₅₀s range from 3-12.5 µg/ml).

A cell-permeable inhibitor of SIRT1 (IC₅₀ = 56 µM) and SIRT2 (IC₅₀ = 59 µM); less effectively inhibits SIRT5 (IC₅₀ >300 µM) and has no effect on class I and II HDACs; sensitizes H460 lung cancer cells to etoposide and paclitaxel; blocks a…

ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC₅₀s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…

A small molecule radiosensitizer that has proven to be an effective and nontoxic immunochemical hypoxia marker for human squamous cell carcinomas of the cervix, head and neck.

An analog of ceramide that inhibits alkaline ceramidase (IC50 ~5 µM); suppresses growth of HL-60 cancer cells in culture.

A fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

A synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.

A membrane-permeable cationic dye that is a substrate for P-gp and is rapidly exported from cells with functional P-gp; also accumulates within mitochondria and can be used to both localize mitochondria and study their properties.

A quorum sensing signal molecule that controls the expression of many virulence genes as a function of cell population density and can also chelate ferric iron at physiological pH.

The primary metabolite of mycophenolic acid, an inhibitor of inosine monophosphate dehydrogenase that prevents lymphocyte proliferation and activation; typically used as an internal standard for therapeutic drug monitoring analyses of serum or whole blood by HPLC or LC-MS to confirm that patients…

20-HETE is a major biologically active CYP450 metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an…

A potent, selective inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM); bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model; decreases hepatic necrosis and apoptosis after orthotopic liver transplantation in rats.

An antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO with an IC₅₀ value of 2.2 µM; sensitizes cells to apoptotic stimuli.

DAN-1 EE is a fluorescent indicator for the bioimaging of NO. DAN-1 EE is a cell permeable derivative of DAN, a molecule which has been used extensively in the quantitation of nitrate and nitrite using fluorescence spectroscopy. Upon entry into the cell, DAN-1 EE is transformed into the less cell…

One of the phenolic antioxidants present in extracts of rosemary; inhibits the formation of tumors derived using irritants such as TPA and DMBA.

A natural isoflavone which promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.

An ethyl ester prodrug of the JMJD3 selective histone demethylase inhibitor GSK-J1; reduces LPS-induced proinflammatory cytokine production, including that of TNFα (IC50 = 9 µM) in human primary macrophages.