A potent, orally bioavailable, ATP-competitive small-molecule dual inhibitor of c-MET (IC₅₀ = 8 nM) and ALK (IC₅₀ = 20 nM) receptor tyrosine kinases; shows antitumor efficacy in multiple tumor models implanted in athymic mice that express activated c-MET or ALK fusion proteins…

A selective, orally available inhibitor of MEK1 (IC₅₀ = 4.2 nM); induces differentiation and apoptosis in cancer cells lines.

AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors. AH 6809 blocks the PGE2-induced accumulation of cAMP in COS cells transfected with the human EP2 receptor. It also blocks the accumulation of Ca2+ in Xenopus oocytes…

An activated fluorescent molecule (excitation: 494 nm, emission: 519 nm) used for labeling proteins; reacts optimally with sulfhydryl groups on cysteine side chains at pH 7, forming a stable thioether bond.

An internal standard for the quantification of oleoyl serotonin by GC- or LC-MS.

A protopanaxatriol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-diabetic actions; protects against DNA damage and apoptosis induced by ultraviolet light.

An internal standard for the quantification of OEA by GC- or LC-MS.

2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…

A thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner; prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection; can affect intracellular GSH concentration and ROS balance.

A mixture of trans (3R/7R and 3S/7S) isomers; induces the synthesis of proteinase inhibitors in plant leaves; in cancer cells, suppresses proliferation and induces apoptosis; inhibits hexokinase that is bound to mitochondria; methyl jasmonate derivatives also have potential as anti-inflammatory agents.

2-Hydroxymyristic acid is an inhibitor of protein myristoylation requiring about 0.5 mM concentration for full inhibition of acylation.

K252c is a cell-permeable PKC inhibitor (IC₅₀s = 2.45 and 25.7 µM for PKC and PKA, respectively). It induces apoptosis in human chronic myelogenous leukemia cancer cells. In human foreskin fibroblast cells, it reduces focus formation induced by human cytomegalovirus (HCMV) strains…

A derivative of thiouracil which has long been used to correct hyperthyroidism; also used as a genetic marker for taste, since only some people detect it as a bitter taste.

A calcimimetic compound that can allosterically activate or positively modulate the human CaSR; dose-dependently decreases circulating levels of PTH in both normal individuals and patients with primary hyperparathyroidism in clinical trials.

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 polyene macrolide used in the treatment of infections caused by C. albicans, A. fumigatus, and parasitic L. protozoans, as well as in tissue culture to prevent fungi from contaminating cell cultures; binds with ergosterol in fungal cell membranes, altering membrane permeability and ultimately…

C-6 NBD ceramide is a biologically active fluorescent analog of short chain, membrane-permeable ceramides. It is as effective as C-6 ceramide in the inhibition of viral glycoprotein transport through the Golgi. C-6 NBD ceramide has been used as a fluorescent substrate for the activity of…

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…

A symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC₅₀ = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.

(±)15-HETE is one of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid. The biological activity of (±)15-HETE is similar to that of its constituent enantiomers (Item Nos. 34720 and 34710).

13,14-dihydro-15-keto PGF1α is a metabolite of PGF1α that has been reported in the rat stomach. The measurement of 13,14-dihydro-15-keto PGF1α can be used as a marker of the in vivo production of PGF1α.

An irreversible inhibitor of ornithine decarboxylase that suppresses polyamine biosynthesis; displays antiangiogenic, cytostatic, and antiparasitic effects.

4-Pyrimidinecarboxaldehyde, dimethyl acetal is a synthetic intermediate useful for pharmaceutical synthesis.

A high-affinity fluorescent calcium indicator (Kd = 115 nM for calcium) that is ideal for monitoring low levels of calcium, as are found in resting cells; may be used to buffer intracellular calcium transients.

A lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells; induces a strong mitochondrial burst of reactive oxygen species at 60-240 µM, resulting in cell death; demonstrates both in vitro and in vivo anti-tumor activity.

A reversible inhibitor of the cis-Golgi ArfGEF, GBF1 (IC₅₀ = 3.3 µM); induces rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network, preventing bidirectional transport of endocytic cargo.

Formal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C₁₆H₁₃F₃N₄O Formula Weight: 334.3

A competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

An intermediate in the HMG-CoA reductase pathway derived directly from farnesyl pyrophosphate and used in the biosynthesis of terpenes and terpenoids; also serves as a substrate in the prenylation of a variety of critical intracellular proteins including small GTPases.

An inhibitor of DPP-4 (IC₅₀ = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…

A nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.