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A derivative of (±)8(9)-EET which is stable enough to ship and handle routinely.
A natural methylated diketopiperazine that potentiates the cytotoxicity of vincristine; directs the intracellular accumulation of vincristine in cancer cells to a similar degree as verapamil, a P-glycoprotein inhibitor, over a range of 1 to 20 µg/ml.
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.
A skeletal muscle relaxant that has applications in reducing muscle spasm, limitations in normal motion, and pain caused by musculoskeletal conditions.
An anionic oligopeptide-based bola-amphiphile that contains a hexane moiety flanked by a glycylglycine group at each end, which creates distinct hydrophilic and hydrophobic regions.
A derivative of the alkaloid camptothecin that is converted by tissue carboxylesterase to 7-ethyl-10-hydroxycamptothecin, a potent inhibitor of DNA topoisomerase I; demonstrates a broad spectrum of antitumor activity against metastatic colorectal cancer, small cell lung cancer, and several other...
MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.
A potential metabolite of PGD2, presumably produced from the known metabolite 13,14-dihydro-15-keto PGD2.
A member of the InsP family of small, soluble second messengers.
Racemic version of a CYP450 metabolite of arachidonic acid.
A synthetic intermediate useful for pharmaceutical synthesis.
A flavonoid originally isolated from the roots of Scutellaria baicalensis Georg; inhibits platelet 12-LO with an ID50 value of 0.12 µM, with minimal inhibition of platelet COX-1 (IC50 = 0.83 mM); inhibits lipid peroxidation, as assessed by production of TBARS, with an...
A selective inhibitor of 12-LO with an IC50 value of 5.1 µM.
11-deoxy PGF2α is a synthetic analog of PGF2α. It is a more potent agonist than PGF2α at inducing smooth muscle contractions of rabbit aorta, dog saphenous vein, and guinea pig trachea. It is approximately 20% less potent than U-46619.
A specific suicide substrate for CYP2C9 and CYP2C10 whereby its oxidation inactivates CYP2C10 with a t½max of 3.4 minutes and a KI value of 4.3 µM.
Functions as a potent laxative by inducing chloride secretion in colonic mucosa and releasing acetylcholine, which stimulates contraction of intestinal smooth muscle; also demonstrates anti-tumor activity (ED50s = 1-13 µM), inducing apoptosis in various cancer cells.
Leukotriene E4 (LTE4) is a product of the 5-lipoxygenase (5-LO) pathway in activated mast cells, eosinophils, and monocytes. LTA4, the primary 5-LO metabolite, is rapidly converted to LTC4 and sequentially to LTD4 and LTE4. While plasma levels of LTC4 are virtually undetectable, exogenously...
Antigen: native protein purified from bovine brain Host: rabbit Cross-Reactivity: (+) human, rat, and mouse synapsin I Application(s): IF, IHC, IP, and WB
A full agonist of the serotonin 5-HT1A receptor and antagonist of 5-HT2A (Kis = 1 and 49 nM, respectively); also binds to dopamine D4 receptors (Kis = 4-24 nM); reduces 5-HT in the prefrontal cortex and dorsal raphe of conscious rats while increasing extracellular noradrenaline and dopamine.
A selective inhibitor of diacylglycerol lipase (IC50 = 4 µM) that demonstrates relatively weak inhibition of phospholipases A2 and C; elevates the concentration of diacylglycerol, which leads to activation of PKC.
Nuclear factor E2-related factor 2 (Nrf2) is a transcription factor that plays a key role in maintaining redox homeostasis via its interaction with a cysteine-rich protein Kelch-like ECH-associated protein 1 (Keap1). In resting cells, Nrf2 and Keap1 form a tight complex, which is targeted for...
A biologically active peroxidation product of linoleic acid; activates an ARE in neuronal cells and induces the expression of ARE-regulated cytoprotective genes; also stimulates the synthesis of aldosterone and corticosterone in adrenal cells when supplied at 1-5 μM.
A substrate for β-galactosidase, the lactose repressor, the galactose-binding protein, the β-methylgalactoside transport system, and thiogalactoside transacetylase.
A polypharmacological cancer therapeutic; potently inhibits RET (IC50 = 2 nM) and reduces the activity of numerous other kinases by more than 80% when given at 1 μM in Drosophila; interferes with kinases downstream of RET, including Src, Raf, and S6K.