A potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC₅₀ values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.

A potent inhibitor that blocks dopamine uptake (IC₅₀ = 1-51 nM); effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors.

A reversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase; blocks H2S synthesis in rat liver preparations with an IC50 value of 6.5 µM.

A calcimimetic compound that can allosterically activate or positively modulate the human CaSR; dose-dependently decreases circulating levels of PTH in both normal individuals and patients with primary hyperparathyroidism in clinical trials.

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

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.

Raclopride is a selective dopamine D₂/D₃ receptor antagonist with K_i values of 1.8, 3.5, 2,400, and 18,000 nM for D₂, D₃, D₄, and D₁ receptors, respectively. It passes the blood brain barrier and can be used in in vivo…

A selective, nonpeptide AT2R antagonist (IC₅₀ = 5.6 nM vs. 100 nM for AT1R) that has been used to selectively examine the specific roles for AT1R and AT2R in hypertensive and other vascular research-related models.

A partial receptor agonist of mGlu4, effective at 100 µM, with no activity at other mGlu receptor subtypes; induces apoptosis of T cells at 300-500 µM.

Pinolenic acid is a PUFA found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO…

A multi-target inhibitor that potently blocks EGFR and HER2 (IC₅₀s = 2.4 and 16.4 nM, respectively) and inhibits the activity of class I and class II HDACs at nanomolar concentrations (e.g., IC₅₀s = 4.5, 12.6, 13.2, and 11.4 nM for HDAC1, 2, 4, and 5, respectively).

A natural isoflavone which is biotransformed by intestinal bacteria to give the phytoestrogens daidzein and equol, resulting in antithrombotic, antiallergic, and other salutary effects; modulates serotonin receptors when given intraperitoneally; suppresses LPS-mediated activation of NF-κB in…

Selective, nonpeptide antagonist of the CRH-R1 (Ki = 1 nM) that, consequently, reduces the release of corticotropin in response to chronic stress.

An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

Furegrelate is a potent inhibitor of thromboxane synthase with little effect on other enzymes essential for arachidonate metabolism. The IC₅₀ value is 15 nM for human platelet microsomal thromboxane synthase.

A potent inhibitor of ROCK-II, PRK-2, MSK1, and MAPKAP-K1b with IC50 values of 1.9, 4, 5, and 15 µM, respectively; has been shown to reduce blood vessel constriction, decreases pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in a diabetic rat model; drug…

A natural alkaloid with antiviral properties, inhibiting the replication of hepatitis B alone and in combination with lamivudine; prevents fibrosis in a number of organs including liver, at least in part by interfering with TGF-β signaling.

An oxidizing reagent that reacts with nitric oxide to form nitric dioxide and corresponding imino nitroxides.

A receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively); effective in treating problems related to the lower urinary tract.

CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.

A natural triterpene which stimulates wound healing; induces cell cycle arrest and apoptosis in breast cancer cells (IC50 = 5.9 µM for MCF-7 cells); blocks angiogenesis in glioblastomas; down regulates BACE1 while increasing ADAM10 maturation in primary rat cortical neurons; protects against…

A plant lectin that selectively cross-links cell-surface glycoproteins and affects the initiation of cell agglutination, mitogenesis, and apoptosis; widely used in affinity chromatography purifications of various glycoproteins and cellular structures; also used to induce liver injury in…

A minor alkaloid produced in plants of the Solanaceae family, including tobacco; detection in urine is used as an indicator of tobacco use; diminishes Aβ production, reduces the transcription and protein levels of β-secretase, and dose dependently inhibits NF-κB activation.

A COX-2-selective NSAID (IC₅₀s = 11.8 and 143 μM for COX-2 and COX-1, in vitro); inhibits acute exudation and leukocyte migration as well as prevents bone and cartilage destruction in adjuvant arthritis animals models.

A derivative of the alkaloid camptothecin that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin, a potent inhibitor of DNA topoisomerase I; demonstrates a broad spectrum of antitumor activity against metastatic colorectal cancer, small cell lung cancer, and several other…

A widely distributed primary PG occuring in many species; causes contraction of vascular, bronchial, intestinal, and myometrial smooth muscle, and also exhibits potent luteolytic activity.

An orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.

A selective inhibitor of human collagenase-3, also known as MMP-13, producing 89% inhibition at 10 µg/ml; used to evaluate the role of MMP-13 in diverse processes.

A naturally-occurring amino acid which is a stable antioxidant; scavenges free radicals and oxidants, controls NF-κB activation, and inhibits inflammatory gene expression; blocks oxidative DNA damage and cell death.

An ATP-competitive Chk1 inhibitor (Ki = 0.49 nM) that demonstrates 100-fold selectivity over Chk2; abrogates DNA damage-induced cell cycle arrest in tumor cell lines and xenografts, potentiating the antiproliferative effects of various chemotherapeutics.

An NMDA open-channel blocker (Ki = 1.2 μM at -60 mV) and uncompetitive antagonist with known anti-Parkinsonian, anti-epileptic, anti-stroke, and anti-Alzheimer’s disease properties; 12 μM blocks 90% of NMDA receptor activity and prevents NMDA-receptor mediated neurotoxicity in rat…

A potent and selective inhibitor of class I α-mannosidases and serves as a key inhibitor of glycoprotein biosynthesis; inhibits both human ER α-1,2-mannosidase I and Golgi class I mannosidases (Golgi α-mannosidase IA, IB, and IC) exhibiting Ki values of 130 and 23 nM,…