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.

A selective inhibitor of PDE4 (IC₅₀ = 72 nM) that antagonizes the Hedgehog signaling pathway; activates localized PKA signaling, which, in turn, regulates Gli processing and translocation.

A synthetic analog of PGF2β.

11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense). Boswellic acids are specific, non-redox inhibitors of leukotriene synthesis via 5-lipoxygenase that demonstrate anti-inflammatory…

A methylsulfanylimidazole that inhibits p38 MAP kinase (IC₅₀ = 0.90 µM in vitro); potently blocks the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC₅₀s = 0.37 and 0.044 µM, respectively).

A mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…

A trichothecene mycotoxin that can infect grain crops causing alimentary toxic aleukia in humans and animals; inhibits protein synthesis, disrupts membrane phospholipid metabolism, increases lipid peroxides in the liver, and is highly cytotoxic to macrophages (IC50 = 19.47 nM), altering the…

A colorimetric substrate whose amino acids YVAD have been shown to be a preferred cleavage site for caspase-1 and -4.

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

AD140 is an orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that binds to the androgen receptor with a Ki value of 7 nM. At 0.03-0.3 mg/kg, it has been shown to stimulate muscle weight increase without affecting prostate or seminal vesicle in castrated male rats. At…

An insect hormone used as an inducer of ecdysone-inducible mammalian expression systems.

A selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).

A photosensitizer used during photodynamic therapy to eliminate abnormal blood vessels in the eye that are associated with conditions such as macular degeneration; also inhibits autophagosome formation by directly targeting and modifying p62, a scaffold and adaptor protein that binds both…

An orally bioavailable inhibitor of HDAC1, HDAC3, and HDAC6 (IC₅₀s = 43-72 nM), resulting in hyperacetylation of histone H4 in multiple myeloma cells; abrogates cell growth and strongly induces apoptosis in multiple myeloma cells (IC₅₀s = 2.5-3 µM); dose-dependently…

A selective β₃-adrenergic receptor antagonist.

A mycotoxin that selectively inhibits RNA polymerase II (1 µg/ml), preventing translocation of the enzymes on DNA; used in molecular biology to distinguish among types of RNA polymerase in a sample and to arrest RNA synthesis in transcription studies.

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…

CWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC₅₀s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…

A hydrophobic diterpene ester that rapidly induces cell death in proliferating keratinocytes through plasma membrane and mitochondrial disruption; causes inflammation due, at least in part, to activation of PKC, leading to antibody-dependent cellular cytotoxicity.

N-2PIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-2PIA inhibits human recombinant and ovine COX-2 with IC₅₀ values of 0.06 and 0.125 µM, respectively. It is over 400 times less potent as an inhibitor of…

An endogenous, maturation-inducing steroid that at 1 µg/ml induces germinal vesicle breakdown in oocytes from several teleost species; can also influence spermiation by stimulating milt production when administered at 5 mg/kg to various male teleosts.

A fluorogenic substrate for chitinases and chitotriosidases.

A selective inhibitor of CaMKII, competitively blocking CaM binding to the kinase (Ki = 370 nM); inhibits histamine-induced aminopyrine uptake in parietal cells (IC₅₀ = 300 nM).

A cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively; does not alter HDAC1 activity.

A stable analog of ATP that acts as a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC₅₀ = 5.52 for P2Y11).

Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

PGF1α is the putative metabolite of DGLA via the COX pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10−11 M. PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the…

An internal standard for the quantification of 5-POHSA by GC- or LC-MS.

A potent, selective chemical probe for the methyl lysine reading function of L3MBTL3 (Kd = 120 nM; IC₅₀ = 40 nM) that competitively displaces mono- or dimethyl-lysine containing peptides.

A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC₅₀s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…

6-keto prostaglandin F_1α (6-keto PGF_1α) is the inactive, non-enzymatic hydrolysis product of PGI₂. 6-keto PGF_1α serves as a useful marker of PGI₂ biosynthesis in vivo. When [ 3 H]-PGI₂ is injected into healthy human…

A TZD that increases the sensitivity of cells to insulin, stimulating insulin-induced PI3K activity at submicromolar concentrations; increases insulin effectiveness in obese NIDDM subjects; promotes adipocyte differentiation by up-regulating the expression of UCP-2.