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 pyridine regio-isomer of the JMJD3 inhibitor GSK-J4; cell-permeable and hydrolyzed to a free base, which is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal negative control molecule.

An NMDA open-channel blocker (Ki = 1.2 μM at -60 mV) and uncompetitive antagonist with known anti-Parkinsonian, anti-epileptic, anti-stroke, and anti-Alzheimer’s disease properties; 12 μM blocks 90% of NMDA receptor activity and prevents NMDA-receptor mediated neurotoxicity in rat…

A thiazide-like diuretic that targets the Na+-Cl- cotransporter responsible for salt reabsorption in the distal convoluted tubule of the kidney (IC₅₀ = 0.3 µM in rat); inhibits human carbonic anhydrase isoforms VII, XII, and XIII (Kis = 2.1, 5.4, and 15 nM, respectively).

A prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid injection; inhibits thymidylate synthase (EC₅₀ = 0.6 nM), interfering with DNA synthesis; used to treat various cancers, particularly metastases to the liver.

An irreversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase (CSE) (IC50 value of 55 µM).

A plant hormone with diverse roles in disease resistance, plant development, and response to stresses; regulates gene expression and may contribute to epigenetic changes at the chromatin level.

A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC₅₀ values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.

An analytical reference material categorized as a phytocannabinoid; intended for research and forensic applications

CYP1B1 is mainly an extrahepatic enzyme which oxidatively metabolizes both endogenous (steroids; eicosanoids) and exogenous xenobiotics such as polyaromatic hydrocarbons. TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM. It is 50-fold selective for the inhibition of CYP1B1…

A selective, irreversible inhibitor of BTK (IC₅₀ = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481; inhibits osteoclast function and reduces osteoclast-stimulated proliferation of multiple myeloma cells in animal models of…

Hydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…

A competitive, non-NMDA glutamate receptor antagonist (IC₅₀s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively, versus IC₅₀ = 25 μM for NMDA receptors).

Docosatrienoic acid is a rare ω-3 fatty acid not readily detected in normal phospholipid PUFA pools. It inhibits [3H]-LTB4 binding to pig neutrophils at a concentration of 5 µM.

A metabolically stable adenosine analog that binds to adenosine A1, A2A, and A3 receptors with Ki values of 300, 80, and 1,900 nM, respectively; anticonvulsive activity in a rat model of generalized seizures.

A nonpurine inhibitor of xanthine oxidoreductase (Ki = 0.7 nM) that has proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.

5-Bromotetralone is a synthetic intermediate useful for pharmaceutical synthesis.

An inhibitor of p53-Mdm2 interaction (IC50 = 0.09 µM); induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53.

Piriprost is a structural analog of PGI2 with low IP receptor-mediated activity. Piriprost inhibits 5-LO with an IC₅₀ value around 100 µM, as measured by the release of 5-HETE from cultured myometrial cells. Piriprost inhibits the release of histamine and leukotrienes from isolated…

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

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…

An amino acid derivative and an intermediate, by-product, or modulator of several metabolic pathways, including the activated methyl cycle and cysteine biosynthesis; also a product of SAM-dependent methylation of biological molecules, including DNA, RNA, and histones, and other proteins.

A progesterone analog (i.e., a progestin); does not bind the ER, however, two of its A-ring metabolites can bind ER and possess weak estrogenic activity.

A positive allosteric modulator of the M1 mAChR; dose-dependently reduces the concentration of acetylcholine required to activate M1; the effective range for potentiation is 0.1 to 100 μM with 3 nM acetylcholine; restores impairment in reversal learning in a mouse model of Alzheimer’s disease.

A selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC₅₀ = 1.5 μM); blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.

A receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively); effective in treating problems related to the lower urinary tract.

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

An irreversible inhibitor of the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC₅₀ = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC₅₀ = 14 nM) with minimal cross reactivity to other proteases; induces cell cycle arrest and…

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.

NAM is a potent, irreversible inhibitor of MAGL or MAGL-like activity in rat cerebellar membranes, exhibiting an IC50 value of 140 nM. Inhibition of MAGL by the sulfhydryl-reactive maleimide group of NAM suggests a critical cysteine residue is present in the substrate-binding site of the enzyme.

Inhibits Gli1-mediated transcription (EC₅₀ = 5 μM) in a variety of cell types disrupting the hh signaling pathway downstream of Smo and Sufu; displays antiproliferative and antitumor activity against Ewing sarcoma family of tumor cells.

2-(hydroxymethyl)-Pyrimidine is a synthetic intermediate useful for pharmaceutical synthesis.