Inhibitor SourceBook™ Second Edition

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Lipid Signaling Cyclooxygenase (COX) Inhibitors, continued Product Cat. No. Comments Size Price Sulindac 574100 {Aflodac; (Z)-5-Fluoro-2-methyl-1-[p-(methylsulfinyl)benzylidene]indene-3-acetic Acid; MK-231} A prodrug that is metabolized to a pharmacologically-active sulfide derivative that potently inhibits COX-2 activity. Inhibits chemical carcinogenesis in rodent models and causes regression of adenomas by an apoptotic mechanism. g $46 Sulindac Sulfide 574102 {(Z)-5-Fluoro-2-methyl-1-[p-(methylthio)benzylidene]indene-3-acetic Acid} A selective inhibitor of COX- (ID = 500 nM) versus COX-2 (ID = 4 mM). 50 50 Reduces Ab load independently of COX inhibition. 42 5 mg $67 Sulindac Sulfone 574105 {Exisulind; FGN-1; (Z)-5-Fluoro-2-methyl-1[p-(methylsulfonyl)benzylidene]indene- 3-acetic Acid} A sulfone metabolite of Sulindac (Cat. No. 574 00) that has anti-cancer properties but lacks COX inhibitory activity. Also inhibits cell growth and induces apoptosis. 5 mg $67 Cyclooxygenase Inhibitor Set Provided as a 4 vial set. Each set contains 00 mg of Meloxicam (Cat. No. 444800), and 5 mg each of NS-398 (Cat. No. 349254), SC-560 (Cat. No. 5656 0), and Sulindac Sulfide (Cat. No. 574 02). Cat. No. 239783 1 set $309 Fatty Acid Amide Hydrolase Inhibitors Product Cat. No. Comments Size Price 0 mg $63 FAAH Inhibitor I 341248 4-Benzyloxyphenyl-n-butylcarbamate, Fatty Acid Amide Hydrolase Inhibitor I, URB532 A cell-permeable carbamate compound that acts as a potent, selective, and irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC 50 = 396 nM in brain membranes). Shown to block anandamide (Cat. No. 72 00) breakdown in cultured rat cortical neurons (IC 50 = 2 4 nM) and inhibit brain FAAH activity (ID 50 = 0.6 mg/kg) and modulate anxiety in rats. FAAH Inhibitor II 341249 3′-Carbamoyl-biphenyl-3-yl-cyclohexylcarbamate; Cyclohexylcarbamic acid-3′carbamoyl-biphenyl-3-yl Ester; URB597 A cell-permeable carbamate compound that acts as a potent, selective, and irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC = 4.6 nM in brain 50 membranes). Shown to block anandamide (Cat. No. 72 00) breakdown in rat cortical neurons (IC = 500 pM) and modulate anxiety in rats (IC = 0. 5 mg/kg). 50 50 Fatty Acid Synthase Inhibitors 5 mg $60 Product Cat. No. Comments Size Price Arachidonylserotonin 181350 AA-5-HT; N-Arachidonyl-5-hydroxytryptamine A novel synthetic arachidonic acid derivative that potently inhibits anandamide hydrolysis in both cell-free preparations and intact cells without affecting anandamide uptake. 5 mg $74 Cerulenin, Cephalosporium 219557 (2R, 3S)-2, 3-epoxy-4-oxo-7, 10-trans, trandocecadienamide 5 mg $77 caerulens A fungal toxin that binds to and irreversibly inhibits fatty acid synthase activity. Fatty Acid Synthase 341325 C75; 3-Carboxy-4-octyl-2-methylenebutyrolactone; trans-4-Carboxy-5-octyl-3- mg $70 Inhibitor, C75 methylenebutyrolactone A cell-permeable a-methylene-g-butyrolactone compound that potently inhibits FAS (fatty acid synthase) activity and stimulates CPT- (carnitine palmitoyltransferase- ), two key enzymes involved in the fatty acid biosynthesis. Acts centrally (reduces NPY expression) and peripherally (activates CPT- and fatty acid oxidation activity) to cause reduced food intake and body weight in mice. Promotes cell cycle arrest in human cancer cells culminating in apoptosis. 5 mg $244 88 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
HMG-CoA (3-Hydroxy-3-Methylglutaryl Coenzyme A) Reductase Inhibitors HMG-CoA reductase catalyzes the 4-electron reduction of HMG-CoA to CoA and mevalonate, with oxidation of two molecules of NADPH. Regulation of the expression of hepatic HMG-CoA reductase is critical in maintaining normal cholesterol levels in serum and tissues. HMG-CoA reductase inhibitors (statins) are competitive inhibitors of this enzyme and have hypocholesterolemic properties. These inhibitors have close resemblance to HMG-CoA. During cholesterol biosynthesis they competitively inhibit the conversion of HMG-CoA to mevalonate, thereby reducing cholesterol biosynthesis in hepatic cells. This results in the enhanced synthesis of LDL-C receptors and increased uptake of LDL-C particles, which enhances cholesterol clearance from the plasma. Ultimately, LDL-C and total cholesterol concentrations are reduced. HMG-CoA (3-Hydroxy-3-Methylglutaryl Coenzyme A) Reductase Inhibitors Calbiochem • Inhibitor SourceBook Lipid Signaling HMG-CoA reductase inhibitors differ in their pharmacokinetic properties and drug interaction profiles. For example, Lovastatin and Simvastatin are extensively metabolized by CYP3A4, an isozyme of the P450 system, and thus have the potential to interact with other drugs competing for or inhibiting this isoform. Both Lovastatin and Simvastatin are prodrugs in the lactone form and must be converted to active metabolites by the liver. On the other hand, pravastatin is not extensively metabolized by the P450 system. It is administered in its active hydroxyl acid form and is more hydrophilic and less protein-bound. Product Cat. No. Comments Size Price Cerulenin, Cephalosporium caerulens 219557 An antifungal antibiotic that inhibits sterol and fatty acid biosynthesis. In fatty acid synthesis, reported to bind in equimolar ratio to b-keto-acyl-ACP synthase. In sterol synthesis, inhibits HMG-CoA synthetase activity. Fluvastatin, Sodium Salt 344095 {(±)-(3R´,5S´,6E)-7-[3-(4-Fluorophenyl)-1-isopropylindol-2-yl]-3,5-dihydroxy-6heptenoate, sodium} A synthetic HMG-CoA reductase inhibitor (IC 50 = 40– 00 nM for human liver microsomes) that acts as anti-hypercholesterolemic agent. Lovastatin 438185 (Mevinolin; MK-803) An anti-hypercholesterolemic agent that inhibits the activity of 3-hydroxy- 3-methylglutaryl coenzyme A (HMG-CoA) reductase. Lovastatin, Sodium Salt 438186 Carboxylate form of Lovastatin (Cat. No. 438 85) that is active in whole cells and cell-free assays. Mevastatin 474700 (Compactin) An antibiotic that acts as a potent inhibitor of HMG-CoA reductase, thus suppressing Ras farnesylation. Mevastatin, Sodium Salt 474705 Carboxylate form of Mevastatin (Cat. No. 474700) that is active in whole cells and in cell-free assays. Pravastatin, Sodium Salt 524403 {(bR,dR,1S,2S,6S,8S,8aR)-1,2,6,7,8,8a-Hexahydro-b,d,6-trihydroxy-2methyl-8[(2S)-2-methyl-1-oxobutoxyl]-1-naphthaleneheptanoic Acid Na; 3b- Hydroxycompactin, Na} A water-soluble, competitive inhibitor of HMG-CoA reductase that potently blocks in vivo cholesterol synthesis (K i ~ nM). Simvastatin 567020 (MK-733) A lipophilic HMG-CoA reductase inhibitor that blocks Ras function through inhibition of farnesylation. Simvastatin, Sodium Salt More online... www.calbiochem.com/inhibitors/HMG 567021 Carboxylate form of Simvastatin (Cat. No. 567020) that is active in whole cells and in cell-free preparations. 5 mg $77 25 mg $ 73 25 mg $98 5 mg $ 40 50 mg $87 5 mg $96 25 mg $72 50 mg $ 64 5 mg $ 40 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 89
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Inhibitor SourceBook Second Editio
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Calbiochem • Inhibitor SourceBook
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Akt (Protein Kinase B) Inhibitors,
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Calmodulin-Dependent Protein Kinase
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Casein Kinase (CK) Inhibitors Casei
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Checkpoint Kinase Inhibitors Eukary
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Cyclin-Dependent Kinase (Cdk) Inhib
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Glycogen Synthase Kinase-3 (GSK-3)
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Glycogen Synthase Kinase Inhibitors
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c-Jun N-Terminal Kinase (JNK/SAP Ki
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Mitogen-Activated Protein (MAP) Kin
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MAP Kinase Inhibitors, continued Ca
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Myosin Light Chain Kinase (MLCK) In
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Phosphatidylinositol 3-Kinase (PI 3
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Protein Kinase A (PKA; cAMP-Depende
Page 39 and 40: Isozyme Specificities of Selected P
Page 41 and 42: Protein Kinase C (PKC) Inhibitors,
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Page 47 and 48: Protein Tyrosine Kinase (PTK) Inhib
Page 57 and 58: Raf Kinase Inhibitors Raf kinases a
Page 59 and 60: Rho Kinase (ROCK) Inhibitors, conti
Page 61 and 62: Protein Phosphatase Inhibitors Calb
Page 63 and 64: Protein Phosphatase Inhibitors, con
Page 65 and 66: Apoptosis Caspase Inhibitors Activa
Page 67 and 68: Caspase Inhibitors, continued Produ
Page 69 and 70: Other Selected Inhibitors of Apopto
Page 73 and 74: DNA Methyltransferase Inhibitors DN
Page 75 and 76: Histone Acetylase and Deacetylase I
Page 77 and 78: Related Products Histone Deacetylas
Page 79 and 80: Nuclear Import/Export Inhibitors, c
Page 83 and 84: Telomerase Inhibitors, continued Ca
Page 85 and 86: Topoisomerase Related Inhibitors, c
Page 87 and 88: Lipid Signaling Acetyl-CoA Carboxyl
Page 89: Cyclooxygenase (COX) Inhibitors, co
Page 93 and 94: Lipoxygenase (LOX) Inhibitors Lipox
Page 95 and 96: Phospholipase Inhibitors Several si
Page 97 and 98: Sphingomyelinase Inhibitors Ceramid
Page 99 and 100: Amyloidogenesis Inhibitors Calbioch
Page 101 and 102: Secretase Inhibitors Deposition of
Page 103 and 104: Secretase Inhibitors Calbiochem •
Page 107 and 108: Glutathione S-Transferase (GST) Inh
Page 109 and 110: Guanylate Cyclase Inhibitors, conti
Page 111 and 112: Characteristics of various forms of
Page 113 and 114: Nitric Oxide Synthase (NOS) Inhibit
Page 115 and 116: Proteases Anthrax Lethal Factor (LF
Page 117 and 118: the ratio of active (76 kDa) to ina
Page 119 and 120: Collagenase Inhibitors (Also see Ma
Page 121 and 122: Matrix Metalloproteinase (MMP) Inhi
Page 123 and 124: Matrix Metalloproteinase Inhibitors
Page 125 and 126: Tissue Inhibitors of Matrix Metallo
Page 127 and 128: Protease Inhibitors The proper func
Page 129 and 130: Protease Inhibitors, continued Calb
Page 131 and 132: Protease Inhibitors, continued Calb
Page 133 and 134: Protease Inhibitors, continued Sele
Page 135 and 136: Protease Inhibitor Cocktails, conti
Page 137 and 138: N Animal-Free Protease Inhibitor Co
Page 139 and 140: Proteasome and Ubiquitination Pathw
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Transmembrane receptors of various
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Angiotensin-Converting Enzyme (ACE)
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ATPase Inhibitors, continued Calbio
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Inhibitors of Glycoprotein Processi
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Heat Shock Protein Inhibitors Heat
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Inhibitors of Mitochondrial Functio
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NF-kB Activation Inhibitors NF-kB,
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NF-kB Activation Inhibitors, contin
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Phosphodiesterase (PDE) Inhibitors
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Plasminogen Activator Inhibitors Ti
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Protein Synthesis Inhibitors, conti
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Sonic Hedgehog Signaling Inhibitors
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Why can’t I make serial dilutions
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Calpastatin, Human, Recombinant, Do
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InSolution Microcystin-LR, Microcys
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RNA Polymerase III Inhibitor ......
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324875 ............................
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Trademarks CALBIOCHEM®
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Your #1 Resource for Inhibitors! We
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