An orally bioavailable, specific, broad spectrum JAK inhibitor (IC₅₀s = 10, 18, 99, and 84 nM for JAK1, JAK2, JAK3, and JAK4, respectively); blocks cell-based JAK signaling induced by IL-2, IL-4, IL-6, IL-13, or IL-31 with IC₅₀ values ranging from 36 to 249 nM.

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.

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

A non-nucleoside DNA methyltransferase inhibitor (IC₅₀ = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.

A plant hormone with diverse roles in disease resistance, plant development, and response to stresses; regulates gene expression and may contribute to epigenetic changes at the chromatin level.

An antibacterial lipopeptide that targets Gram-positive bacteria and may be useful against drug resistant strains; also inhibits peptidoglycan synthesis.

DPI is an irreversible inhibitor of iNOS and eNOS with IC₅₀ values of 50 nM and 0.3 µM, respectively. This inhibition is potent, irreversible, and time and temperature dependent. NADPH, NADP+, and 2'5'-ADP block the inhibitory action of DPI. Similarly, FAD or FMN protect…

CYP1B1 is mainly an extrahepatic enzyme which oxidatively metabolizes both endogenous (steroids; eicosanoids) and exogenous xenobiotics such as polyaromatic hydrocarbons. TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM. It is 50-fold selective for the inhibition of CYP1B1…

A selective dual inhibitor of mTORC1 and mTORC2.

An indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).

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.

An active, deacetylated metabolite of T-2 toxin; inhibits protein synthesis and cell proliferation in plants; causes acute and chronic toxic effects in animals that ingest contaminated plant materials.

An inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC₅₀ = 5.6 µM); blocks SREBP-mediated gene expression; inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells; reduces hepatic fat…

A selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 (IC₅₀ = 22 nM).

An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC₅₀ values of 0.6 and 5 µM, respectively.

An internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-MS.

A selective inhibitor of 15-hydroxy PGDH (IC₅₀ = ~10 µM).

An antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC₅₀ = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…

A semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM); has applications in breast cancer and hormone-refractory prostate cancer; intended for research applications.

A natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.

A synthetic PGA1 analog with structural features similar to 15-deoxy-Δ12,14-PGJ2, a ligand for PPARγ.

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

8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the…

A selective allosteric inhibitor of Bcr-Abl (IC₅₀s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…

Eltrombopag is a small molecule, nonpeptide agonist of the thrombopoietin receptor. It selectively binds to the transmembrane domain of the receptor and stimulates megakaryocytopoiesis in primary human bone marrow cells through the JAK/STAT signaling pathway. Eltrombopag is reported to increase…

An N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.

A water soluble prodrug analog of AEA with similar activity to that of AEA in the growth inhibition of C6 glioma cells; also a structural variant of LPA, however, its effects on the various LPA receptors have not been tested.

A potent, competitive inhibitor of HO activity in vitro (Ki = 14 nM); inhibits hepatic, renal, and splenic HO activity in vivo for extended periods of time; blocks bilirubin production in vivo, decreasing HO activity in animal models of hyperbilirubinemia.

An ATP-competitive inhibitor of JAK1 and JAK2 (IC₅₀s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms.

An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.

A small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…

A synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1; phosphorylated by Cdk5 with a Km value of 5 µM.