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 =…

Travoprost is the Alcon trade name for fluprostenol isopropyl ester, an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. Fluprostenol isopropyl ester is a prodrug which is converted by esterase enzymatic activity in the cornea to yield the corresponding…

A derivative of testosterone and ethisterone that binds androgen receptors and sex hormone-binding globulin causing a 3-fold increase in free testosterone; possesses weak androgenic effects and inhibits the production of gonadotropins.

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.

An inhibitor of PDGF-BB tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.

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).

POL is a common triglyceride component in seed and vegetable oils including olive, sesame, soybean, canola, corn, hazelnut, and many others. POL is one of the standard triglyceride components used for the USP analysis of sesame oil for pharmaceutical applications.

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

A natural intermediate in the pteridine pathway that can be produced naturally from 7-oxobiopterin or in vitro by the oxidation of pterin by xanthine oxidase.

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.

An ATP-competitive Pim-1 kinase inhibitor (IC₅₀ = 50 nM) that displays selectivity over the related kinases, Pim-2 and MEK1/2 (IC₅₀s = >20 µM).

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

A cytotoxic, quinoline alkaloid that inhibits the DNA enzyme topoisomerase I (Top I) by binding the Top1-DNA cleavage complex and inducing DNA-strand breaks; has strong anti-tumor activity and induces DNA damage at concentrations as low as 51 nM in whole cells and 12 nM in isolated nuclei in in…

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

An aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC₅₀ = 140 nM) without effect on SIRT1 or SIRT3-6; increases α-tubulin acetylation in HeLa cells.

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

An ATP-competitive inhibitor of JAK1 and JAK2 (IC₅₀s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms.

An aminoglycoside antibiotic that shows potent activity against a broad spectrum of bacteria.

An analog of adenosine monophosphate that has antiviral activity; converted by cellular enzymes to tenofovir diphosphate, an obligate chain terminator that inhibits the activity of HIV reverse transcriptase and HBV polymerase.

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 prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.

A potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

A lysyl amide prodrug of the benzothiazole 5-fluoro 203, a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1, which leads to the formation of DNA adducts and cell cycle arrest.

Selectively inhibits ALK1 (IC₅₀ = 46 nM) and ALK2 (IC₅₀ = 32 nM) with >300-fold selectivity over ALK3, ALK6, and VEGF type 2 receptor; inhibits BMP4 signaling with an IC₅₀ value of 152 nM in a functional assay.

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

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 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.