A derivative of halopemide which potently inhibits both PLD1 (IC₅₀ = 25 nM) and PLD2 (IC₅₀ = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.

A potent inhibitor of neprilysin, a membrane metallo-endopeptidase that cleaves peptide hormones, such as enkephalins, glucagon, and bradykinin (Ki = 4-140 nM); produced in vivo via the metabolism of the prodrug acetorphan.

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

A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells. It completely blocks…

A symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC₅₀ = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.

A potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC₅₀ values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.

A selective non-peptide agonist of the δ-opioid receptor (Ki = 0.18 nM, IC₅₀ = 2.73 nM) that is over 2,000-fold less effective at the μ-opioid receptor; effectively activates µ/δ receptor heteromers (EC₅₀ = 52.8 nM) but not κ/δ or μ/κ heteromers.

A potent inhibitor of tubulin polymerization with strong inhibitory activity on tumor cell growth.

A selective, potent, and cell-permeable inhibitor of mTOR (IC₅₀ = 4.3 nM) which blocks signaling through both mTORC1 and mTORC2; induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines and reduces tumor growth in nude mice with PTEN-null tumors.

2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…

A selective inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to AA; orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.

Lyso-PC is the ubiquitous lipid species generated following PLA2 hydrolysis of phosphatidylcholine. The hydrolysis of phospholipids by arachidonyl-selective PLA2s is the initiating event in many eicosanoid-based signal transduction pathways. Many other reactions also generate phosphatidylcholine…

An intermediate in the generation of adenine and methionine that is produced by the decarboxylation of SAM; a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 μM for A1, A2A, A2B, and A3, respectively); inhibits several enzymes at higher concentrations.

A fluorescent probe commonly used to identify dead cells; excitation at 488-535 nm and emission maximum of 617 nm.

Molecular Formula: C₁₃H₁₅IN₂O₂

A potent, competitive inhibitor of HMG-CoA reductase (Ki = 0.12 nM).

A cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC₅₀ = 0.82-14 μM); inhibits glucagon-induced gluconeogenesis in primary hepatocytes.

A broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.

DepNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity.{8928} FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its endogenous substrate AEA. It also will hydrolyze fatty acid amides…

A phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling; stimulates PI hydrolysis and proliferation through human CaSR (pEC₅₀ values are 6.9 and 7.4, respectively) in the presence of calcium.

An isomer of Vitamin E that has less potent antioxidant properties than α-tocotrienol.

A potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively; blocks IL-6 signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM); reduces splenomegaly, decreases circulating levels of IL-6 and TNF-α, eliminates…

An irreversible inhibitor of ornithine decarboxylase that suppresses polyamine biosynthesis; displays antiangiogenic, cytostatic, and antiparasitic effects.

A potent and selective inhibitor of reticulocyte 15-LO-1.

An intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase; excess cystathionine in the urine is a hallmark of cystathioninuria.

CAS Number: 1000998-59-3 Molecular Formula: C₂₂H₂₁ClN₂O₆ Formula Weight: 444.9

A hydroxyethyl ether rapamycin derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM; orally available with superior pharmacokinetics and pharmacodynamics over rapamycin.

A thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.

Mn(III)TMPyP is a cell-permeable SOD mimic and peroxynitrite decomposition catalyst. The rate constants for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M−1s−1 and ~2 x 106 M−1s−1, respectively.

A post-synaptic α1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia; displays high-affinity with non-selectivity for the three known human α1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for α1A, α1B,…

An inhibitor of ferroptosis induced in MEFs by Gpx4 deletion (IC₅₀ = 22 nM) or by the ferroptosis inducers BSO, erastin, and RSL3; does not interfere with apoptosis, necroptosis, or necrosis; effectively suppresses ferroptosis in vivo when administered intraperitoneally.

A cell-permeable analog of cGMP that preferentially activates cGMP-dependent protein kinase; 1 µM-0.1 mM inhibits acetylcholine-induced increases in intracellular calcium concentrations.