A potent and selective inhibitor of PLD1, both in vitro (IC₅₀ = 46 nM) and in cells (IC₅₀ = 11 nM); also effective as a PLD2 inhibitor at higher concentrations (IC₅₀ = 933 nM in vitro; 1,800 nM in cells); strongly inhibits the invasive migration of several breast…

A potent, selective inhibitor of Stearoyl-CoA desaturase 1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.

A chromogenic substrate for N-acetyl-D-galactosaminidase that generates a yellow solution upon cleavage.

A sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles; selectively inhibits the growth of influenza A and B viruses in plaque reduction assays (IC₅₀s = 5-14 nM) and to directly inhibit influenza A and B virus neuraminidases…

A potent inhibitor of VEGF receptors, inhibiting VEGFR1, 2, and 3 with IC₅₀ values of 130, 23, and 18 nM, respectively; orally bioavailable in vivo, blocking VEGF-induced angiogenesis and preventing the growth of primary tumors and spontaneous peripheral metastases in mice.

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

A selective, potent inhibitor of ERK2 (Ki = 2 nM); inhibits proliferation of COLO 205 cells (IC50 = 0.54 µM).

A small molecule pan activator of Ras-related GTPases, activating Rac1, cdc42, Ras, and Rab-2A with EC₅₀ values of 20, 100, 141, and 355 nM, respectively.

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.

Enzymatically-derived PGE2 is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings…

A plant growth regulator with anticancer activity.

A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

TTP 22 is a thienopyrimidine compound that inhibits casein kinase 2 (CK2) with an IC₅₀ value of 100 nM (Ki = 40 nM). It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM.

A dibenzoxazepine which acts as a selective antagonist of PGE2 at the human EP1 receptor (IC₅₀ = 6.7 µM); at doses between 0.3-300 µM, is a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach and trachea.

A natural yellow carotenoid, which can be found in plants, egg yolks, and in the human retina; a lipid-soluble antioxidant that can circulate in the plasma and confer cardioprotective, anti-inflammatory, and anti-angiogenic effects.

A primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration; inhibits BRD4 binding and action in vitro or in cells; arrests the growth of leukemia T cells in vitro (EC₅₀ = 91 nM) and rapidly suppresses leukemia burden in mice.

An inhibitor of PDGF-BB tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.

The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1 and CRTH2/DP2. 15(R)-15-methyl PGD2 is a potent,…

Piriprost is a structural analog of PGI2 with low IP receptor-mediated activity. Piriprost inhibits 5-LO with an IC₅₀ value around 100 µM, as measured by the release of 5-HETE from cultured myometrial cells. Piriprost inhibits the release of histamine and leukotrienes from isolated…

An antagonist of REV-ERBα (EC₅₀ = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112; stimulates the expression of the REV-ERBα target genes G6Pase and PEPCK in liver cells; used to elucidate the role of REV-ERBα in regulating glucagon…

A stable and efficient hole-transport material in organic light-emitting devices and in ssDSSCs; yields high ssDSSC efficiency due to its excellent pore-filling property into mesoporous titania films.

PGD2 is one of the five primary enzymatic prostaglandins derived directly from PGH2. PGD2 is produced abundantly in the CSF by the lipocalin-type PGD synthase, and in the periphery by myeloid cells including mast cells and basophils by a second, hematopoietic-type PGD synthase. PGD2 is chemically…

A selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.

A selective inhibitor of BAZ2A (Kd = 109 nM; IC₅₀ = 130 nM) and BAZ2B (Kd = 170 nM; IC₅₀ = 180 nM) bromodomains.

A potent, reversible, orally bioavailable inhibitor of Pim-1, -2, and -3 (IC₅₀s = 5, 25, and 16 nM, respectively); dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1; acts synergistically with chemotherapeutic drugs.

An internal standard for the quantification of creatinine by GC- or LC-MS.

A γ-secretase inhibitor that blocks Notch processing (IC₅₀ = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose.

A potent inhibitor of calcium release-activated calcium channels in lymphocytes (IC₅₀ = 100 nM); also inhibits lung IL-4 and CysLT generation in animal models of asthma.

A sesterterpenoid fungal phytotoxin that binds and irreversibly antagonizes calmodulin, blocking the activation of calmodulin-dependent phosphodiesterase with an IC₅₀ value of 9 μM.

An antifungal antibiotic that selectively inhibits succinate dehydrogenase (complex II; IC50s = 12 and 3.7 nM in nematode and mammalian mitochondria, respectively, versus IC50s > 100 μM for inhibition of complex I and complex III enzymes); has cardioprotective effects against simulated…

A potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO₃- secretion in the stomach.