CAS Number: 1228817-38-6 Molecular Formula: C₂₆H₃₆N₆O₃ Formula Weight: 480.6

A benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC₅₀ = 3.8 µM); also a negative modulator of GABAA receptors, reversibly inhibiting both evoked and spontaneous inhibitory postsynaptic currents (IC₅₀ =…

An intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase; excess cystathionine in the urine is a hallmark of cystathioninuria.

An indole-based, time-dependent inhibitor of Icmt (IC₅₀ = i = 0.14 µM for the final complex); decreases mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death in PC3 prostate cancer cells.

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.

A substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication; participates in G-protein-related signal transduction where it is converted to GDP through the action of GTPases.

A ceramide analog that contains a mixture of all four possible stereoisomers.

A non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC₅₀s = ~ 0.45 to 0.9 μM).

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

The major active lignin in fruits of the burdock plant A. lappa that demonstrates potent antiviral, anti-inflammatory, and antiproliferative activity.

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.

A selective β₃-adrenergic receptor antagonist.

A pan-caspase inhibitor that blocks apoptosis, prevents the production of cytokines, and inhibits T cell proliferation dose-dependently at 1-100 μM.

A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

A small molecule inhibitor of tankyrase 1 and 2 (IC₅₀ = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

A selective inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to AA; orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.

A selective, potent, and cell-permeable inhibitor of mTOR (IC₅₀ = 4.3 nM) which blocks signaling through both mTORC1 and mTORC2; induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines and reduces tumor growth in nude mice with PTEN-null tumors.

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 activator of PLC that stimulates superoxide generation, increase in cytoplasmic calcium, and inositol phosphate formation in human neutrophils when used at a concentration of 15-50 µM; promotes the hydrolysis of phosphatidylinositol bisphosphate by all PLC isoforms.

An ATP/GTP-competitive inhibitor of CK2 (IC₅₀ = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC₅₀ = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.

An analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol

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.…

A selective inhibitor of cFMS kinase (IC₅₀ = 0.03 μM) that prevents CSF-1-induced monocyte growth with an IC₅₀ value of 0.14 μM; at 75-100 mg/kg, inhibits joint connective tissue and bone degradation in mouse models of arthritis.

A mycotoxin produced in food and animal feeds; activates estrogen receptors, alters hormone levels, and hasten pre-pubertal development; can cause uterine, rectal, and vaginal prolapse, abortion, and infertility in older animals.

A Ca2+-selective ionophore for biological membranes that can be used in microelectrodes for the determination of resting Ca2+-activities and of slowly changing Ca2+ levels.

An inhibitor of EGF receptor kinase with an IC50 value of 1 µM in HT-22 cells.

A trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.

A analog of tenovin-1; elevates p53 activity in MCF-7 cells at 10 µM and reduces growth of ARN8 melanoma xenograft tumors in SCID mice at a dose of 50 mg/kg.

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 side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of SREBPs; has been implicated in a variety of metabolic events including cholesterol homeostasis and atherosclerosis as well as antitumor and immunomodulating activities.

MAHMA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 1 minute and 3 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.

A prenylflavonoid with potent estrogenic activity that inhibits both ERα and ERβ (IC₅₀s = 57 and 68 nM, respectively); effective in vivo, suppressing bone loss and temperature changes in rat models of osteoporosis and postmenopausal hot flashes.