20 products were found matching "Cay10010498"!

Hydrogen sulphide (H2S), a naturally occurring gasotransmitter, is a potent vasodilator and pro-inflammatory mediator. DL-Propargyl glycine (PAG) is an irreversible inhibitor of the H2S synthesizing enzyme cystathionine-gamma-lyase (CSE). PAG blocks H2S synthesis activity in rat liver preparations with an IC50 value...

Brevetoxin B is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. It binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal,...

Manumycin A is an antibiotic that acts as a potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity. It inhibits rat brain FTase with a Ki value of 1.2 µM, thereby preventing Ras activation which requires farnesylation at the C-terminus for membrane attachment. It exhibits significant...

Tranylcypromine is an irreversible, mechanism-based inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 20.7 µM in a cell-free assay). It also irreversibly inhibits monoamine oxidase A (MAO-A) and MAO-B with IC50 values of 2.3 and 0.95 µM, respectively. Tranylcypromine inhibits nucleosomal demethylation of...

(+)-Cloprostenol is a synthetic analog of prostaglandin F2alpha (PGF2alpha). It is an FP receptor agonist and a potent luteolytic agent in rats and hamsters. It is 200 times and 100 times more potent than PGF2alpha in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with...

Prostaglandin A2 (PGA2) blocks cell cycle progression of NIH 3T3 cells at the G1 and G2/M phase. It has antitumor effects, targeting scaffold/matrix attachment region-binding protein 1 (SMAR1) through an Hsp70-dependent mechanism. PGA2 also induces apoptosis in HL-60 cells. Prostaglandin A2-biotin (PGA2-biotin) is...

HA-130 is a reversible inhibitor of autotaxin, completely blocking the hydrolysis of the substrate bis-pNPP with an IC50 value of 28 nM. It does not affect the activity of any proteasomal protease or related enzymes. HA-130 rapidly decreases plasma lysophosphatidic acid levels in mice when given intravenously (1...

Three known isoforms of SREBP (sterol regulatory element binding protein) transcription factors have been characterized: SREBP-1a, SREBP-1c, and SREBP-2. SREBP-1c acts primarily to activate genes required for fatty acid synthesis, such as acetyl-CoA carboxylase, fatty acid synthase, and long chain fatty acid...

JWH 081 is a synthetic cannabinoid (CB) that shows a high-affinity for the central CB1 receptor with a Ki value of 1.2 nM and ten-fold reduced affinity for the peripheral CB2 receptor (Ki = 12.4 nM). JWH 081 7-methoxynaphthyl isomer differs structurally from JWH 081 by having the methoxy group attached to the...

Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis. CJ-42794 is a selective antagonist of EP4 (Ki = 3.16 nM) that less...

15-Lipoxygenase inhibitor 1 is a 15-lipoxygenase (15-LO) inhibitor (IC50 = 18 µM). It scavenges DPPH (Cay-14805) radicals in a cell-free assay (IC50 = 69.6 µM).Formal Name: 4-methyl-2-(4-methylpiperazinyl)pyrimido[4,5-b]benzothiazine. CAS Number: 928853-86-5. Synonyms: 15-LO Inhibitor 1, 4-MMPB. Molecular Formula:...

(S)-AM1241 binds to cannabinoid (CB) receptors and is selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively, in a membrane assay using human receptors). (S)-1241 acts as an agonist at human, rat, and mouse CB2 receptors but shows greater activity at human CB2 (EC50 = 131 nM) than at rat...