A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC₅₀s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

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

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 40 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; promotes stem cell differentiation.

A potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.

Reactive oxygen species (ROS) play important roles in the initiation and progression of many disease processes. Most fluorescent probes for ROS detection, such as 2,7-dichlorofluorescein (DCFH), function by an oxidative mechanism and are useful for total oxidant detection but are not selective for…

L-Arginine serves as a common substrate for both NOS and arginase in the cell. NOS catalyzes the oxidation of arginine to citrulline and NO with Nω-hydroxy-L-arginine (NOHA) formed as an intermediate. Arginase, on the other hand, catalyzes the hydrolysis of arginine into urea and L-ornithine.…

An antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC₅₀ values range from 240-440 nM); orally bioavailable, having anti-proliferation as well as apoptotic actions in various tumor models; affects multiple signaling pathways.

A prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling that may activate TRPV1 and TRPV4.

A natural nitroaryl-substituted polyketide that exhibits antitumor, antifungal, and insecticidal activities; non-competitive inhibitor NADH:ubiquinone oxidoreductase of bovine heart, N. crassa, and E. coli (IC₅₀s = 0.07, 0.08, and 22 nmol/mg protein, respectively).

A selective, irreversible inhibitor of IL-1b converting enzyme (ICE; Caspase-1); neuroprotective in a rat model of cerebral ischemia.

PGF1β is the C-9 epimer of PGF1α. It was shown to enhance respiratory rate in experimental animals when administered intravenously.

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.

A selective, reversible inhibitor of V-ATPases in mammalian, plant, or fungal cells with an IC₅₀ value in the 4-400 nM range; at 100 nM, the related bafilomycin A1 blocks V-ATPase-mediated acidification of lysosomes during autophagy, preventing protein degradation.

A minor impurity produced in the synthesis of (+)-cloprostenol; 20-fold less active than (+)-cloprostenol in terminating pregnancy in the hamster.

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…

A potent inhibitor of autotaxin (IC50 = 2.8 nM in an in vitro enzyme assay); at 30 mg/kg, reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).

Ro 3-1314 is an inhibitor of both COX and lipoxygenase. Ro 3-1314 inhibits ram seminal vesicle COX with a Ki of 0.6 µM. It is a more effective inhibitor of COX-1 than of 15-LO, inhibiting 95% and 68%, respectively, of these enzymatic activities when used at a concentration of 48 µM.

A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC₅₀s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.

An irreversible antitumor agent that induces non-apoptotic cell death selectively in tumor cells expressing the small T oncoprotein and oncogenic Ras (IC₅₀s = 1.25-5 µg/ml).

An inhibitor of non-structural protein 5A of hepatitis C virus; effectively reduces or eliminates certain genotypes of hepatitis C virus in vivo, particularly when used in combination with other agents.

15(R)-PGF2α is the C-15 epimer of the naturally occurring mammalian autacoid PGF2α. It has only 25% of the potency of PGF2α in hamster antifertility studies, which may be due to reduced affinity for FP receptors. Compared to PGF2α, 15(R)-PGF2α has a binding affinity of…

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 colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

The L isomer of the biologically important D-myo-inositol-1,4,5-triphosphate; does not evoke a rise in intracellular calcium when added to cells.

A metabolite of the nucleoside reverse transcriptase inhibitor, zidovudine, formed by direct conjugation by UGT2B7.

A proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase; inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 µM, respectively.

A covalent Cdk7 inhibitor (IC₅₀s = 3.2-15.6 nM in vitro) that displays broad anti-proliferative activity against cancer cell lines, particularly T-ALL cell lines with characteristic misregulation of T cell lineage-specific transcription factors.

1-Hexadecyl lysophosphatidic acid is an ether analog of LPA containing a hexadecyl group at the sn-1 position. LPA binds to five different GPCRs to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility.

A more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).

A reversible, cell-permeable inhibitor of GSK3α and GSK3β (IC₅₀ = 0.65 and 0.58 nM, respectively); stimulates glycogen synthase in cells (EC₅₀ = 106 nM), potentiates insulin-dependent glucose transport in isolated muscle strips, and improves glucose disposal in…

A potent, selective inhibitor of aldose reductase (IC₅₀ = 47 nM in vitro) used to improve the cytotoxic effects certain anticancer agents; inhibits PGF2α and PGE2 production in human endometrial cells (EC₅₀ = 10 μM).

IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor that demonstrates IC₅₀ values of 59 and 12 nM for human IDO enzymatic activity and HeLa cell assays, respectively. It is inactive against tryptophan 2,3-dioxygenase (TOD; IC₅₀ > 10 µM).