13(S)-HODE is the LO metabolite of linoleic acid. 13(S)-HODE modulates the PAF, LTB4, and fMLP-induced calcium influx in human PMNL. The mechanism by which 13(S)-HODE elicits its inhibitory effect is still unclear. The use of biotinylated 15(S)-HETE as a probe for detecting binding proteins and/or…

Steroisomer of PGF1α with both C-9 and C-11 hydroxyls inverted.

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

Molecular Formula: C₂₉H₂₂N₃O₁₄ • 5K

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

An orally bioavailable, reversible inhibitor of JAK1 and JAK2 (IC₅₀s = 5.9 and 5.7 nM, respectively) that has been shown to inhibit cytokine-induced phosphorylation of STAT3 in healthy human volunteers.

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.

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 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…

An endogenous, maturation-inducing steroid that at 1 µg/ml induces germinal vesicle breakdown in oocytes from several teleost species; can also influence spermiation by stimulating milt production when administered at 5 mg/kg to various male teleosts.

A potent, selective, and cell-permeable inhibitor of the BRPF1 bromodomain (IC₅₀ = 80 nM); disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.

The Rho family of GTPases regulates diverse signal transduction pathways. One member, the cell division control protein 42 homolog (Cdc42), is involved in filopodia function, cell polarity, cell cycling, and other processes. CASIN is an indole-based small molecule that inhibits activation of the…

Formal Name: 3,4-dichloro-N-(1-methylbutyl)-benzamide CAS Number: 7497-07-6 Molecular Formula: C₁₂H₁₅Cl₂NO

A potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC₅₀s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.