14 products were found matching "Cay13950"!

Cafestol is a natural diterpene which is abundant in unfiltered coffee. It elevates serum cholesterol and triglycerides in humans, an effect which does not seem to occur in monkeys, hamsters, rats, or gerbils. Dietary cafestol does increase total cholesterol and triglycerides in ApoE3Leiden mice, an effect which is...

K252b is an indolocarbazole isolated from the actinomycete Nocardiopsis, first described as an inhibitor of protein kinase C. However, as this compound does not freely pass through the cell membrane, it is used to inhibit extracellular kinases (ectokinases) of cells in culture. K252b inhibits receptor-mediated...

SQ 22,536 is an inhibitor of adenylyl cyclase with an IC50 value of 13 µM for inhibition of prostaglandin E1-stimulated increase in cAMP in intact platelets. It has been used to evaluate adenylyl cyclase activity during iloprost-induced vasorelaxation of isolated pulmonary veins or aorta in several research...

Methotrexate (MTX) is similar in structure to folic acid (Cay-20515) and aminopterin (Cay-21802). It acts by inhibiting the metabolism of folic acid and blocking key enzymes in the synthesis of purines and pyrimidines required for cell proliferation. MTX is known to induce adenosine release, which mediates many of...

Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to beta-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production...

Plants from the mint genus Lagochilus have been used in traditional medicines of the east. Lagochiline is a polyphenolic natural product isolated from Lagochilus spp. which is thought to provide some of the benefits of the herb. The physiological, immunological, and toxicological properties of this compound remain...

Rotenone is a classical inhibitor of complex I of the mitochondrial electron transport chain, inhibiting NADH/DB oxidoreductase and NADH oxidase with IC50 values of 28.8 and 5.1 nM, respectively. In substantia nigra pars compacta neurons, it activates ATP-sensitive potassium channels and increases the production of...

19(R)-hydroxy PGE1 is the major prostaglandin found in the semen of primates, including man. It is an agonist for the EP1 and EP3 receptor subtypes, and exhibits contractile activity on smooth muscle preparations. It has an EC50 of 320 nM for contracting guinea pig ileum, which express EP1 receptors, and an EC50 of...

Mycophenolate mofetil is a prodrug form of mycophenolic acid (Cay-21716). It is converted to mycophenolic acid via carboxylesterase 1 (CES1) and CES2. Mycophenolate mofetil (1 and 10 µg/ml) inhibits thymidine incorporation in primary rat aortic smooth muscle cells. In vivo, mycophenolate mofetil (12.5 mg/kg)...

JNJ-5207787 is an antagonist of the neuropeptide Y (NPY) receptor Y2 that blocks peptide YY binding (IC50 = 100 nM). It displays 100-fold selectivity for Y2 over other NPY receptors and has minimal effect on a panel of 50 receptors, ion channels, and transporters, except for sodium channel 2. JNJ-5207787 is...

EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2). It acts competitively with the EZH2 substrate S-adenosylmethionine. EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases...

Timolol is a non-selective beta-adrenergic receptor antagonist with log Kd values of -8.27, -9.86, and -6.8 for binding to human beta1-, beta2-, and beta3-adrenoceptors, respectively. It has been reported that only the (S) enantiomer contributes to the beta-blocking effects of racemic timolol, but the weakly active...