A potent and selective inhibitor of PLD1, both in vitro (IC₅₀ = 46 nM) and in cells (IC₅₀ = 11 nM); also effective as a PLD2 inhibitor at higher concentrations (IC₅₀ = 933 nM in vitro; 1,800 nM in cells); strongly inhibits the invasive migration of several breast…

A purine derivative that reversibly antagonizes aryl hydrocarbon receptor signaling (IC₅₀ = 127 nM in CD34+ cells); induces a 50-fold increase in human embryonic stem cells expressing CD34 (EC₅₀ = 120 nM) and a 17-fold increase in stem cells that retain the ability to engraft…

A secondary metabolite produced by fungi; inhibits IgE production by mouse B cells in culture (IC₅₀ = 3.6 μM) and dose-dependently (0.4-25 μg/ml) stimulates neuritogenic activity in rat pheochromocytoma PC12 cells; demonstrates nematicidal activity at 300 μg/ml.

A natural meroterpene that has retinol-like effects on gene expression and properties of the skin; has antioxidant and antibacterial actions; inhibits DNA polymerase and UDP-glucuronosyltransferase 2B7 (IC50 = 41 µM).

A sulfated form of taurocholic acid that may be involved in the elimination and detoxification of bile acids during hepatobiliary diseases.

ApNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate AEA (Item No. 90050). It also will hydrolyze…

An antitumor antibiotic that crosslinks double stranded DNA and is widely used as a tool to selectively inhibit DNA synthesis and mutagenensis, to stimulate genetic recombination, chromosome breakage and sister chromatid exchange, and to induce DNA repair.

A CYP17 inhibitor (IC₅₀ = 300 nM) that competitively blocks synthetic androgen binding (EC₅₀ = 845 nM) and antagonizes the androgen receptor in transcriptional activation assays; inhibits the growth of castration-resistant prostate cancer cells (IC₅₀ = 2.9 µM).

A sesterterpenoid fungal phytotoxin that binds and irreversibly antagonizes calmodulin, blocking the activation of calmodulin-dependent phosphodiesterase with an IC₅₀ value of 9 μM.

An activator of sGC that binds to a regulatory site, resulting in activation in an NO-independent manner (Kd = 3.2 nM); reduces hypertension, limits cardiomyocyte hypertrophy, protects against ischemia/reperfusion injury, and reduces morbidity and mortality in response to endotoxic shock.

A specific Akt inhibitor that has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells (IC₅₀ = 30-60 nM in vitro); inhibits Akt, PDK1, and FLT3 in acute myelogenous leukemia cells, decreasing the colony-forming ability of these cells (IC₅₀…

A broad-spectrum antibiotic that inhibits protein synthesis by inducing miscoding; commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells.

A selective, cell permeable inhibitor of CaMKII (IC₅₀ = 900 nM).

A non-cholestatic regioisomer of E217G that acts as a substrate for MRP2, competing with E217G for MRP2-mediated transport (IC₅₀ = 14.2 µM).

A synthetic PGA1 analog with structural features similar to 15-deoxy-Δ12,14-PGJ2, a ligand for PPARγ.

DAF-2 diacetate is a sensitive fluorescent indicator for the detection and bioimaging of NO. It is a cell-permeable derivative of DAF-2. Upon entry into the cell, DAF-2 diacetate is transformed into the less cell-permeable DAF-2 by cellular esterases thus preventing loss of signal due to diffusion…

A synthetic heptapeptide that acts as a specific substrate for PKA.

A selective dual inhibitor of mTORC1 and mTORC2.

A phosphonic analog of ATP and agonist of P2X1 and P2X3 (EC50 = ~1 µM); ~1,000-fold less potent at P2X2, P2X receptors 4-7, and P2Y receptors; used as a stable analog of ATP to study the interaction of ATP with kinases and other proteins.

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.

An intermediate produced from vitamin D2 by cytochrome P450 isoforms in vertebrates; subsequently metabolized to 1,25-dihydroxy vitamin D2, which is an agonist for the vitamin D receptor.

ICI 192605 is a potent antagonist of the thromboxane A₂ receptor (TP) that blocks contraction of isolated guinea pig trachea induced by U-46619 (Item No. 16450; K_d = 0.398 nM). It is used to study the role of TP signaling in tissues and animals.

Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases.

A synthetic version of the endogenous antidiuretic hormone arginine vasopressin; acts as an agonist at human vasopressin V1a, V1b, and V2 receptors with Ki values of 62.4, 5.8, and 23.3 nM, respectively.

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 macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis; induces mitotic arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate,…

A potent inhibitor of PI3K isoforms α, δ, and γ (IC₅₀s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ; has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo.

8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.

PLC catalyzes the hydrolysis of phosphatidyl inositol (4,5) bisphosphate (PIP2) on the cytoplasmic side of the cell membrane to yield diacylglycerol and inositol-1,4,5-triphosphate (IP3). This reaction initiates a well-known signal transduction pathway common to most cells. PLC thio-PIP2 is an…

Spontaneously hypertensive rats fed a diet which includes γ-tocotrienol show significant reduction of systolic blood pressure and an increase of nitric oxide synthase activity in blood vessels. γ-Tocotrienol at 20 µM induces apoptosis of malignant sympathoadrenal (+SA) murine…

A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC₅₀s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC₅₀s = 0.92 and 1.04 µM for mouse…

A selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol; improves insulin sensitivity, lowers plasma, glucose and increases mitochondrial capacity in diet-induced obese and diabetic leptin-deficient ob/ob mice after one week of treatment with an oral dose of…