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

A natural isoflavone which promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.

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…

A stimulator of sGC, increasing the activity of recombinant sGC dose-dependently, from 0.1 nM to 100 μM, up to 92-fold; in vitro, relaxes vessels and inhibits platelet aggregation at nM concentrations; in vivo, decreases blood pressure dose-dependently, prolongs bleeding time, and reduces thrombosis.

A phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling; stimulates PI hydrolysis and proliferation through human CaSR (pEC₅₀ values are 6.9 and 7.4, respectively) in the presence of calcium.

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A potent, selective inhibitor of p110δ.

A dual inhibitor of c-Src and Abl (IC50 = 2.7 and 30 nM, respectively); less effectively inhibits other kinases; blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival; reduces osteoclast bone resorption.

A form of biotin with a terminal azide group; is used to add biotin to other molecules that bear either an alkyne group, through click chemistry, or a phosphine group, using Staudinger ligation.

A potent and selective inhibitor of reticulocyte 15-LO-1.

An ATP-competitive inhibitor of Cdk1, 2, 4, 5, 6, and 9 with IC₅₀ values of 210, 47, 100, 13, 170, and 50s = 40-940 nM in vitro) and human tumor xenograft models, inhibiting cell cycle progression and inducing apoptosis.

An irreversible inhibitor of carnitine palmitoyltransferase 1, a mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver); also acts as a direct agonist of PPARα.

A fluorescent substrate for calpain and papain (excitation max: 360 nm; emission max: 460 nm) that is used for measuring the chymotrypsin-like peptidase activity of the 20S proteasome.

A selective SIP1 agonist (EC₅₀ = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC₅₀ = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.

FeTMPyP is a synthetic porphyrin complexed with iron, which acts as a peroxynitrite decomposition catalyst. The rate constant for decomposition of peroxynitrite by FeTMPyP is 2.2 x 106 M−1s−1 with a turnover number of 360 ± 170 s−1. The predominant product (>90%) of this…

An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC₅₀ = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

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.

DuP-697 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK-966 (rofecoxib), SC-58125, and celecoxib. DuP-697 is a potent and time-dependent inhibitor of COX-2. When tested on isolated recombinant enzymes, DuP-697 is at least 50 times more potent in the…

A selective inhibitor of PDGF receptor kinase with an IC50 value of20 µM in human bone marrow; inhibits the EGF receptor with an IC50 value of 820 µM.

A quinazolinone derivative that selectively inhibits dynamin GTPase activity in yeast and mammalian cells (IC₅₀ = 1-10 μM); prevents apoptosis by inhibiting mitochondrial outer membrane permeabilization.

A selective inhibitor of ASK1 (IC₅₀ = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

An analog of (−)-blebbistatin that is stable to prolonged irradiation at 450-490 nm and has been successfully used in fluorescent live cell imaging.

A long-acting muscarinic receptor antagonist that binds equally to human muscarinic M1, M2, and M3 receptors (Kds = 0.04, 0.02, and 0.01 nM, respectively); dissociates slowly from M1 and M3 receptors, which are located on bronchial smooth muscle and submucosal glands, and more rapidly from M2…

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

A NO donor with a half-life of three hours at 37°C, pH 7.4; liberates two moles of NO per mole of parent compound.

An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

An estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.

A non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.

A small molecule inhibitor of KCNJ1 (IC₅₀ = 294 nM) which also causes 70% inhibition of KCNJ13 at 10 µM; has no effect on the related channels KCNJ2 (Kir2.1) and KCNJ10 (Kir4.1) at a concentration of 10 µM.

A potent inhibitor of LSD1 (IC₅₀ = 0.02 µM) that less effectively inhibits MAO-A and MAO-B (IC₅₀s = 1.38 and 0.72 µM); blocks the expression of IE genes of HSV and hCMV in mammalian cells; represses HSV primary infection in mice and blocks HSV reactivation from…

A divalent cation ionophore, commonly used to facilitate the movement of Ca2+ into cells, triggering the activation of intracellular calcium-dependent pathways; also used to produce apoptosis through calcium overload, as occurs during hypoxic or oxidative stress.

A pan FGFR inhibitor (IC₅₀s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively); suppresses proliferation of cancer cells with wild-type FGFR3 overexpression and in an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3.