A potent ATP-competitive inhibitor of ATM kinase (IC₅₀ = 13 nM; Ki = 2.2 nM); sensitizes cells to both ionizing radiation and chemotherapeutic agents; induces senescent breast, lung, and colon carcinoma cells to undergo cell death; inhibits HIV-1 replication in C8166 human T-lymophocyte…

PGF1β is the C-9 epimer of PGF1α. It was shown to enhance respiratory rate in experimental animals when administered intravenously.

Arachidonic acid is converted by microsomal CYP450 enzymes to a variety of epoxides, ω-1 and ω-hydroxylated compounds via what is known as the epoxidase pathway. PPOH is a selective inhibitor of the epoxygenation reactions catalyzed by specific CYP450 isozymes. PPOH inhibits the…

A potent, selective antagonist of the β2-adrenergic receptor (Ki = 0.7 nM for the β2 receptor, compared with 49.5 and 611 nM for β1 and β3 receptors, respectively); active in vivo and often used to evaluate the actions of adrenergic receptor agonists.

A fluorogenic substrate that can be cleaved specifically by group I caspases.

A reversible inhibitor of Lp-PLA2 (IC₅₀ = 0.25 nM) that produces sustained inhibition of plasma Lp-PLA2 activity in humans.

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.

9β-hydroxy stereoisomer of PGF2α; much less active than PGF2α in antifertility and bronchoconstrictor activities; exhibits bronchodilating activity in guinea pigs and cats and antagonizes the bronchoconstrictor activity of PGF2α.

An antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO with an IC₅₀ value of 2.2 µM; sensitizes cells to apoptotic stimuli.

A small molecule inhibitor of nucleophosmin dimers that can prevent cell proliferation and induce apoptosis in various cancer cell lines (IC₅₀s = 1.4-4 µM).

A potent antagonist of the type III receptor tyrosine kinases PDGFRβ, FLT3, and c-Kit (IC₅₀ = 200, 220, and 170 nM, respectively); less potently inhibits CSF-1R (IC₅₀ = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.

An analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…

PGD2 is one of the five primary enzymatic prostaglandins derived directly from PGH2. PGD2 is produced abundantly in the CSF by the lipocalin-type PGD synthase, and in the periphery by myeloid cells including mast cells and basophils by a second, hematopoietic-type PGD synthase. PGD2 is chemically…

A staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC₅₀s ranging from 60-600 nM).

Eltrombopag is a small molecule, nonpeptide agonist of the thrombopoietin receptor. It selectively binds to the transmembrane domain of the receptor and stimulates megakaryocytopoiesis in primary human bone marrow cells through the JAK/STAT signaling pathway. Eltrombopag is reported to increase…

A small molecule inhibitor of human cytomegalovirus viral replication (EC₅₀ = ~5 nM with a selectivity index >15,000) that targets viral DNA cleavage and packaging.

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 metabolite of lipoxygenase-mediated oxidation of DPA; activates Nrf2-dependent antioxidant gene expression, acts as a PPARγ agonist (EC₅₀ = ~200 nM), and inhibits pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 µM).

A small molecule inhibitor of MDMX.

A selective, nonpeptide antagonist of the vasopressin V1a receptor (Ki = 1.1-6.3 nM in human); inhibits arginine vasopressin-induced human platelet aggregation with an IC₅₀ value of 3.7 nM.

5(Z),11(Z),14(Z)-Eicosatrienoic acid is a PUFA found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was…

Estrone is one of the three naturally occurring estrogens, the others being estradiol and estriol. Estrone is synthesized from androstenedione by the aromatase enzyme system in the ovaries and placenta, and is also synthesized from estradiol by 17-hydroxy steroid dehydrogenase in the liver. Serum…

A FAHFA in which oleic acid occurs at the 12-position on hydroxy stearic acid.

A second generation analog of amiloride that inhibits TRPP3-mediated Ca2+-activated (IC₅₀ = 0.14 μM) and ENaC (IC₅₀ = 10 nM); inhibits active sodium transport of human and ovine bronchial epithelial cells (IC₅₀s = 75 and 116 nM, respectively).

Oleic acid is a monounsaturated fatty acid and is one of the major components of membrane phospholipids. Oleic acid contributes about 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets. Oleic acid inhibits collagen-stimulated platelet…

A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme; blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of NETs in both mouse and human neutrophils.

A carboxylic acid-based inhibitor of aldose reductase (IC₅₀ = 0.01-15 μM) that suppresses high glucose-induced proliferation of vascular smooth muscle cells as well as prevents high glucose-induced intracellular NADH/NAD+ increase and membrane-bound protein kinase C activation.

The less predominant-occurring (~20%) stereoisomer of the endogenous oxysterol 27-hydroxy cholesterol.

CAS Number: 940929-33-9 Molecular Formula: C₃₁H₃₃ClN₂O₃ • HCl Formula Weight: 553.5

An analog of latanoprost in which the hydroxyl at C-15 is inverted relative to latanoprost; binds to the FP receptor in the cat iris sphincter muscle with an IC₅₀ value of 24 µM (tested as the free acid); potential impurity in latanoprost bulk drug preparations.

A long-acting, selective β2-adrenergic agonist with bronchodilator actions (EC₅₀ = 0.25 µM) that demonstrates 2,818-fold selectivity for β2-adrenergic receptors over β1-adrenergic receptors.

A rotenoid compound with chemopreventive and chemosensitizing effects in models of skin, mammary, colon, and lung carcinogenesis; inhibits cell growth (IC50 = 8 M), blocks PI3K/Akt signaling, suppresses COX-2 expression, and induces apoptosis of premalignant and squamous HBE cells without affecting…