A broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.

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.

A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.

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.

An imidazole that potently antagonizes the α2-adrenoceptor (Ki = 1.6 nM); shows selectivity over the α1-adrenoceptor (Ki = 13,300 nM) and is a poor antagonist at a wide variety of other receptors and channels.

An antifungal agent that acts as an inverse agonist to disrupt Hh signaling (IC₅₀ = 0.8 μM); treatment at 100 mg/kg twice per day has been shown to suppress the growth of medulloblastomas from a Ptch+/-p53-/- mouse allograft model.

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…

A competitive antagonist of capsaicin activation of the TRPV1 (IC₅₀s = 24.5 and 85.6 nM for human and rat, respectively); reverses thermal and mechanical hyperalgesia in a rat model of inflammatory pain.

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.…

A fluorescent probe commonly used to identify dead cells; excitation at 488-535 nm and emission maximum of 617 nm.

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 biotinylating reagent that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.

An inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ; blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ; selectively toxic to some carcinoma cell lines expressing the…

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

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).

An HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in vitro (IC50 = 930 nM).

An L-type calcium channel blocker that is selective over N-, R-, P/Q- and T-type calcium channels; displays antihypertensive activity, lowering arterial blood pressure without altering cardiac contractility.

A flavonoid compound that acts as a powerful antioxidant; inhibits TBARS formation with an IC50 value of 6.34 µM; blocks oxLDL uptake by U937-derived macrophages at 20 µM; demonstrates potent chemopreventative potential by binding JAK1/STAT3 to inhibit neoplastic transformation of…

A cyclic nitrone spin trap that can be used for the detection and characterization of thiyl radicals, hydroxyl radicals, and superoxide anions in vitro or in vivo.

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

A benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC₅₀ = 3.8 µM); also a negative modulator of GABAA receptors, reversibly inhibiting both evoked and spontaneous inhibitory postsynaptic currents (IC₅₀ =…

Mn(III)TBAP is a cell-permeable SOD mimic. At a concentration of 30 µM, it decreases the doubling time of SOD-null E. coli. by 2-fold.

A cell-penetrating peptide inhibitor of calpain (IC₅₀ = 5 nM) which completely abolishes calpain activity in platelets; also a potent inhibitor of cathepsin K (IC₅₀ = 0.11 nM).

A skeletal muscle relaxant that has applications in reducing muscle spasm, limitations in normal motion, and pain caused by musculoskeletal conditions.

A rotenoid compound with chemopreventive and chemosensitizing effects in models of skin, mammary, colon, and lung carcinogenesis; inhibits cell growth (IC50 = 8 M), blocks PI3K/Akt signaling, suppresses COX-2 expression, and induces apoptosis of premalignant and squamous HBE cells without affecting…

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 metabolite of vinclozolin, a dicarboximide fungicide, that acts as an effective antagonist of the androgen receptor (Ki = 9.7 µM in rat).

An amino acid derivative and an intermediate, by-product, or modulator of several metabolic pathways, including the activated methyl cycle and cysteine biosynthesis; also a product of SAM-dependent methylation of biological molecules, including DNA, RNA, and histones, and other proteins.

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…