An extract from A. lappa, a burdock plant traditionally used in Japanese Kampo medicine for its antioxidant, anti-inflammatory, antiproliferative, and antiviral activity.

A sulfonyl hydrazide that inhibits BCATc (IC₅₀s = 0.81 and 0.2 µM in human and rat, respectively) with 15-fold selectivity over BCATm; blocks calcium influx into neurons (IC₅₀ = 4.8 µM) following inhibition of glutamate uptake and demonstrates neuroprotective…

11β-PGE1 is an epimerized form of PGE1 at the C-11 position. 11β-PGE1 is a less potent isomer of PGE1. It is 13% and 3.6% as potent as PGE1 in contracting the rat uterus and guinea pig ileum, respectively.

A LPA analog containing stearyl alcohol at the sn-1 position; exhibits platelet aggregating activity with an EC50 value of 9 nM versus an EC50 value of 177 nM for 1-octadecanoyl LPA.

A potent and selective inhibitor of DGAT-1 (IC₅₀ = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.

A potent blocker of HCN channels that inhibits HCN4 more potently than HCN1 (IC₅₀s = 32 and 158 nM, respectively); modulates the sinoatrial node and slows heart rate; reduces neuropathic pain in several animal models.

An endogenous CB neurotransmitter that binds to both CB1 and CB2 receptors.

A selective IGF-1R inhibitor (IC₅₀ = 0.17 µM); inhibits tumor proliferation both in vitro and in a mouse model of multiple myeloma.

A non-steroidal androgen receptor antagonist (IC50 = 36 nM); reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.

A potent, allosteric inhibitor of Akt1 and Akt2 (IC₅₀ = 58 and 210 nM, respectively) that less effectively blocks Akt3 activity (IC₅₀ = 2.2 µM); cell permeable, blocking insulin regulation of FOXO1 activity at 1 µM in rat hepatoma cells.

A product of CYP2A6 metabolism of the primary nicotine metabolite, cotinine; as a biomarker of nicotine metabolism.

Formal Name: 4-[6-methoxy-2-[(1E)-2-(3-nitrophenyl)ethenyl]-4-oxo-3(4H)-quinazolinyl]-benzoic acid CAS Number: 1237744-13-6 Molecular Formula: C₂₄H₁₇N₃O₆

A naturally occurring phospholipid produced by cells upon inflammatory stimulation; less potent than PAF C-16 and PAF C-18 in the induction of neutrophil chemotaxis, but is equipotent to PAF C-16 and PAF C-18 in promoting eosinophil migration.

GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC₅₀ value of 0.4 nM. It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.…

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.

A FAHFA in which palmitic acid is esterified to 9-hydroxy palmitic acid.

A potent, orally bioavailable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki death proteins, like Bim, leading to apoptosis; induces apoptosis in cancer cell lines expressing mutants of β-catenin 1.

Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of sPLA2. The IC₅₀ value for thioetheramide-PC is 2 µM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, thioetheramide-PC…

A melatonin metabolite first identified in rat brain that has antioxidant and free radical scavenging activities in several experimental models; may be measured in plasma as an index of melatonin synthesis and metabolism.

A homolog of EPEA, characterized by the addition of an (R)-β-methyl group at the terminal ethanolamine carbon.

A stable analog of ATP that acts as a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC₅₀ = 5.52 for P2Y11).

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.

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.

A prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.

A triazolothiadiazine that inhibits PDE4 (EC₅₀ = 18.7 nM in a cell-based assay); selectively inhibits PDE4A (IC₅₀ = 6.7 nM) over PDE4B1, PDE4B2, PDE4C1, and PDE4D2 (IC₅₀ = 48.2, 37.2, 452, and 49.2 nM, respectively).

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.

An N-hydroxysuccinimide ester of the nitroxide spin label tempyo; an active acylating agent that preferentially targets α-amino groups, used to spin label proteins and aminoacylated RNA species.

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

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 5 nM), p59fynT (IC₅₀ = 6 nM), Hck (IC₅₀ = 20 nM).

A potent and selective inhibitor of Vps34 (IC₅₀ = 25 nM in vitro); induces a rapid and pronounced loss of phosphorylation of SGK3.

A natural anthocyanin that has neuroprotective effects, reducing amyloid β-induced cytotoxicity in Neuro-2A cells; stimulates autophagy in U2OS cells.

A cell-permeable triazine compound that inhibits the human E2 ubiquitin-conjugating enzyme Rad6B; selectively docks to the Rad6B catalytic site, inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2/M arrest and apoptosis, and inhibits…