A hepatotoxic monocylic pentapeptide that acts as a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively.

An ATP-competitive inhibitor of p38 MAPK isoform p38α (IC₅₀s = 5 nM) and p38β (97% inhibition at 1 µM); has little effect on a range of other kinases, including p38γ and p38δ; blocks the phosphorylation of HSP27, a p38 MAPK substrate, in response to…

BW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…

An inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs; reduces ethylene-mediated plant changes in growth and development; inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.

An angiotensin II receptor blocker with a high affinity for the AT1 receptor (Ki = 2.7 nM) and exceptionally high bioavailability (60-80%); an insurmountable antagonist of AT1; act as a cardiovascular protective agent by effectively reducing blood pressure; also useful in treating diabetes and…

A cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

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.

An orally bioavailable, selective inhibitor of EZH2 (Ki = 2.5 nM); blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC₅₀s range from 2-90 nM); induces apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and promotes their…

A selective GPR55 inverse agonist that antagonizes GPR55 constitutive activity (IC₅₀ = 15 μM); blocks GPR55-mediated endothelial wound healing and reverses LPI-inhibited platelet aggregation.

An analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

A potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC₅₀ = 3.2 and 26 µM, respectively).

A selective inhibitor of ASK1 (IC₅₀ = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

An abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum; avidly binds several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus, in some cases altering viral infectivity.

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.

The oxidized form of NADPH; serves as a cofactor in various biological reactions.

An inhibitor of respiration in animals and bacteria; binds at the quinone reduction site of succinate:ubiquinone oxidoreductase (SQR; Complex II) in animals, preventing ubiquinone from binding; inhibits NADH fumarate reductase in bacteria; inhibits photosystem II in plants.

A more lipophilic, stabilized form of HPA.

DETA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 20 hours and 56 hours at 37°C and 22-25°C, pH 7.4, respectively, to liberate 2 moles of NO per mole of parent compound.

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 monoacylglycerol that is metabolized by monoacylglycerol lipase; an agonist of GPR119 (EC₅₀ = 2.5 µM), stimulating the release of glucagon-like peptide-1 from intestinal L-cells.

A polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.

A broad spectrum tyrosine kinase inhibitor that blocks angiogenesis through its actions on VEGFR isoforms; has low nanomolar efficacy against VEGFR1 (FLT1), VEGFR2, VEGFR3 (FLT4), and KIT, as well as CSF1R, PDGFRA, and PDGFRB; effective in vivo and useful in the management of certain types of cancer.

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.

A product of CYP2A6 metabolism of the primary nicotine metabolite, cotinine; as a biomarker of nicotine metabolism.

A membrane-permeant, fluorescent Na+ indicator dye; increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm.

A substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

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

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.

A lipid peroxidation product derived from oxidized ω-6 PUFAs such as linoleic acid and arachidonic acid which is widely used as a marker of lipid peroxidation.