A specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.

Formal Name: 3,4-dichloro-N-(1-methylbutyl)-benzamide CAS Number: 7497-07-6 Molecular Formula: C₁₂H₁₅Cl₂NO

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

8-hydroxy Guanine is produced by oxidative damage of DNA or RNA by reactive oxygen and nitrogen species, including hydroxyl radical and peroxynitrite. It serves as a measure of oxidative stress in biological systems.

A potent inhibitor of several CDKs with selectivity for Cdk2 (IC₅₀s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells.

A selective ERRβ/γ receptor agonist (EC₅₀ = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.

The four tocopherols (α, β, .delta., and γ) and four tocotrienols (α, β, .delta., and γ) are forms of vitamin E, which is known for its antioxidant activity. Tocotrienols are found at high concentrations in palm oil and rice bran. Recent studies show tocotrienols…

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 naturally occurring agonist for the nuclear receptor Nur77 (IC₅₀ = 0.278 nM); induces apoptosis in cancer cells and retards xenograft tumor growth; induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat/high cholesterol diet.

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.

RD162 is a second-generation androgen receptor (AR) antagonist. It inhibits binding of 18 F-FDHT to AR in human prostate cancer cells with an IC₅₀ value of 30.9 nM. RD162 completely suppresses VCaP cell proliferation at 1 µM and induces apoptosis of VCaP cells at 10 µM.…

The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR family of proteins, is coordinated by synthesis of diffusible acylhomoserine lactone (AHL) molecules. C6-HSL is a small diffusible signaling molecule involved in quorum sensing, controlling gene…

CAY10499 is a potent inhibitor of human HSL exhibiting an IC50 of 90 nM for the recombinant enzyme. The in vivo pharmacological efficacy of CAY10499 has not been reported.

A highly selective, non-ATP competitive inhibitor of p38/mitogen-activated protein kinase-activated protein kinase 2 (IC₅₀ = 0.11 μM); inhibits TNF-α (IC₅₀ = 4.4 μM) and IL-6 (IC₅₀ = 5.2 μM) secretion from the human THP-1 acute monocytic leukemia cell line.

The first identified small molecule inhibitor of BLM helicase (IC₅₀ = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC₅₀s ≥ 50 μM); 25-50 μM dose-dependently inhibits the proliferation of BLM-expressing PSNF5…

A peptide antagonist of PAR2 which blocks activation by trypsin (IC₅₀ = ~50 μM) but not by the synthetic agonist SLIGRL-NH2; does not affect thrombin-induced activation of PAR1 or trypsin-mediated proteolysis of casein; used to study PAR2 action in cells and in animals.

A potent inhibitor of DNA topoisomerase I that induces cytoxicity and DNA damage in human HT-29 colon adenocarcinoma cells (IC₅₀s = 33 nM and 0.28 μM, respectively; demonstrates a broad spectrum of antitumor activity against a variety of other tumors including ovarian cancer, cervical…

Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC₅₀s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for…

A flavonoid isolated from the root of the traditional Chinese herb S. baicalensis with anti-inflammatory, antioxidant, antitumor, and neuroprotective activities at concentrations from 5-75 μM.

A selective non-peptide agonist of the δ-opioid receptor (Ki = 0.18 nM, IC₅₀ = 2.73 nM) that is over 2,000-fold less effective at the μ-opioid receptor; effectively activates µ/δ receptor heteromers (EC₅₀ = 52.8 nM) but not κ/δ or μ/κ heteromers.

A potent lipid signaling molecule that exhibits a wide range of biological activities; it enhances cell growth and inhibits the normal apoptotic response to a variety of stimuli.

A tetraline that inhibits monoamine transporters with selectivity for the serotonin transporter (IC₅₀s = 70, 520, and 720 nM for the serotonin, dopamine, and norepinephrine transporters, respectively).

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.

A selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC₅₀ = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC₂₅ = 0.45 nM); attenuates β-amyloid…

An aminooxy analog of ornithine that irreversibly inhibits aminotransferases, including ornithine aminotransferase (Ki = 2 µM); cytotoxic to a range of organisms.

A phorbol ester that is commonly used to activate certain types of protein PKC and, indirectly, certain MAP kinase pathways; prolonged treatment with PMA produces various effects, ranging from tumorigenesis to hematopoietic differentiation.

A potent, selective inhibitor of p110δ.

A heptose that inhibits glucokinases and hexokinases from diverse organisms through competition with D-glucose (Ki = 0.25 mM); blocks glucose oxidation and glucose-mediated insulin release from pancreatic islet cells.

Thioester analogs of glycerophospholipids, in combination with Ellman’s reagent, are convenient colorimetric substrates for the measurement of phospholipase activity. HEPC is a truncated analog of phosphatidylcholine with the entire sn-1 substituent deleted, and with a hexadecylthioester in…

A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC₅₀ = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a…

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.

An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.