Inhibitor SourceBook™ Second Edition

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Neurobiology/Neurodegeneration Neurobiology/Neurodegeneration Amyloidogenesis Inhibitors Ab (b-amyloid) peptide is a major component of neuritic plaques and cerebrovascular amyloid deposits in the brains of patients with Alzheimer's disease (AD). The cellular origin of amyloid precursor protein (APP) that gives rise to Ab is now well understood. Morphological evidence suggests that APP-immunoreactive neurites, often capped by Ab deposits, are one of the major sources of parenchymal amyloid. However, other cells, including Amyloidogenesis Inhibitors astroglia, microglia, and vascular cells, may contribute to the formation of Ab. A long-standing hypothesis has been that Ab deposits are neurotoxic and are causative factors in the development and progression of AD. Hence, the development of inhibitors of Ab fibrillogenesis has become an important area of research. More online... www.calbiochem.com/inhibitors/amyloidogenesis Product Cat. No. Comments Size Price Ab 40 Fibrillogenesis Inhibitor 171581 [Ab16-20m; Ac-K(Me)LV(Me)FF-NH 2 ; Amyloid b 40 Fibrillogenesis Inhibitor] Cell-permeable pentapeptide based on the core domain of Ab, which contains N-methyl amino acids in alternate positions. Displays stability towards denaturation and is resistant to chymotrypsin. Ab 42 Fibrillogenesis Inhibitor I 171586 (Amyloid b 42 Fibrillogenesis Inhibitor I; iAb5; LPFFD) Design is based on the central hydrophobic region in the N-terminal domain of Ab. Binds to the monomeric/dimeric Ab peptides with high affinity (K d ~70 nM). Ab 42 Fibrillogenesis Inhibitor II 171587 (Amyloid b 42 Fibrillogenesis Inhibitor II; RVVIA-NH 2 ) Contains the C-terminal sequence of Ab 42 with Gly 38 to Arg substitution, which results in improved solubility and potency. Ab 42 Fibrillogenesis Inhibitor III 171588 (Amyloid b 42 Fibrillogenesis Inhibitor III; Ac-LPFFD-NH 2 ; iAb5p) A modified analog of Ab 42 Fibrillogenesis Inhibitor I (Cat. No. 7 586). Can cross the blood brain barrier. Exhibits greater stability against proteolytic degradation. Ab 42 Fibrillogenesis Inhibitor IV 171589 [Ac-LP-(NMe)-FFD-NH 2 ; Amyloid b 42 Fibrillogenesis Inhibitor IV; iAb5p-A1] A modified analog of the end protected Ab 42 Fibrillogenesis Inhibitor III (Cat. No. 7 588) that acts as a b-sheet breaker. Has increased in vivo metabolic stability (t ½ >24 hours in human plasma and in rat brain homogenate). Clioquinol 233165 (5-Chloro-7-iodo-8-hydroxyquinoline) A metal ion chelator that crosses the blood-brain barrier and acts as a neurotoxic antibiotic. Reported to dissolve senile plaques and reduce amyloid’s ability to clump together, apparently by trapping Cu 2+ and Zn 2+ that reduces the build-up of these deposits. Diclofenac Sodium 287840 A cell-permeable, non-selective cyclooxygenase inhibitor (IC 50 = 60 nM and 200 nM for ovine COX- and COX-2 respectively) and potent non-steroidal anti-inflammatory drug with analgesic activity. Strongly inhibits insoluble transthyretin (TTR) amyloid fibril formation. Also inhibits liver phenol sulfotransferase activity (IC 50 = 9.5 mM). Flurbiprofen 344079 A non-steroidal anti-inflammatory agent that acts as a potent cyclooxygenase inhibitor (IC 50 = 5 nM for LPS-induced COX in human peripheral blood cells). Reduces Ab loads and Congo Red staining in APP+PS transgenic mice. Genistein 345834 An isoflavone that acts as a potent inhibitor of transthyretin (TTR) tetramer dissociation and amyloidogenesis. Binds to TTR with negative cooperativity (K d = 40 nM; K d2 = .4 mM). Prevents acid-mediated fibril aggregation. 96 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem mg 5 mg $77 $289 5 mg $ 35 5 mg $ 35 5 mg $ 35 5 mg $20 g $45 g $28 00 mg $38 20 mg 50 mg $73 $ 46
Amyloidogenesis Inhibitors Calbiochem • Inhibitor SourceBook Neurobiology/Neurodegeneration Product Cat. No. Comments Size Price Niflumic Acid 481987 A phenolic product with antifungal, antitumor, and antioxidative properties. A specific inhibitor of COX- (ED = 5 mM). Also inhibits 50 the hydroxyperoxidase activity of COX- (ED = 3.7 mM). Strongly 50 inhibits insoluble transthyretin (TTR) amyloid formation. g $39 Resveratrol 554325 A phenolic product with antifungal, antitumor, and antioxidative properties. A specific inhibitor of COX- (ED = 5 mM). Also inhibits 50 the hydroxyperoxidase activity of COX- (ED = 3.7 mM). Promotes 50 intracellular degradation of Ab peptide via a proteasome-dependent process. 25 mg $4 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 97
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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
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Isozyme Specificities of Selected P
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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
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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 and 90: Cyclooxygenase (COX) Inhibitors, co
Page 91 and 92: HMG-CoA (3-Hydroxy-3-Methylglutaryl
Page 93 and 94: Lipoxygenase (LOX) Inhibitors Lipox
Page 95 and 96: Phospholipase Inhibitors Several si
Page 97: Sphingomyelinase Inhibitors Ceramid
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
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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
Page 141 and 142: Transmembrane receptors of various
Page 143 and 144: Angiotensin-Converting Enzyme (ACE)
Page 145 and 146: 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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