Inhibitor SourceBook™ Second Edition

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Neurobiology/Neurodegeneration Secretase Inhibitors, continued Product Cat. No. Comments Size Price g-Secretase Inhibitor VII 565768 [Compound A; MOC-LL-CHO (MOC = menthyloxycarbonyl)] A cell-permeable, reversible inhibitor of Ab and p3 secretion (Ab 40 IC 50 = 2.3 mM; Ab 42 IC 50 = 3 mM). Reported to be more potent (IC 50 = 900 nM and 740 nM for Ab 40 and Ab 42 , respectively) in the presence of C99 inhibitor ( 0 mM). g-Secretase Inhibitor IX 565770 {DAPT; N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester} A cell-permeable dipeptide that reduces Ab production by blocking g-secretase (Ab total IC 50 = 5 nM, Ab 42 IC 50 = 200 nM). Reported to be functionally active in both HEK293 cells and neuronal cultures without affecting the secretion of amyloid-b precursor protein. N InSolution g-Secretase Inhibitor IX 565784 {DAPT; N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester} A 25 mM (5 mg/462 ml) solution of g-Secretase Inhibitor IX (Cat. No. 565770) in DMSO. InSolution g-Secretase Inhibitor X 565771 {L-685,458; {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)- 1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester} g-Secretase Inhibitor XI 565772 Supplied as a mM solution in 372 ml of DMSO. A cell-permeable, highly specific and potent inhibitor of g-secretase (Ab IC = total 50 7 nM, Ab IC = 48 nM, and Ab IC = 67 nM in SH-SY5Y cells 40 50 42 50 overexpressing spbA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease. Exhibits over 00fold greater selectivity for g-secretase than for cathepsin D. (7-Amino-4-chloro-3-methoxyisocoumarin; JLK6) A cell-permeable, active site-directed, irreversible serine protease inhibitor that acts as a highly selective, potent inhibitor of g-secretase. Blocks production of both amyloid-b (Ab ) and Ab < 00 mM in 40 40 42 HEK293 cells expressing wild-type and Swedish mutant b-amyloid precursor protein. g-Secretase Inhibitor XII 565773 (Z-IL-CHO) A cell-permeable, reversible dipeptide aldehyde that reduces Ab production by blocking g-secretase in vitro (Ab IC = 7.9 mM; 40 50 Ab IC = 7.6 mM) and in cultured CHO cells that stably overexpress 42 50 APP695 (Ab IC = .5 mM; Ab IC = 8.3 mM). Also blocks the 40 50 42 50 generation of g CTF (g-secretase-generated C-terminal fragment). Does not affect the formation of amyloid-b precursor protein. g-Secretase Inhibitor XIII 565774 (Z-YIL-CHO) A cell-permeable, reversible inhibitor of g-secretase. In TPA-stimulated T47- 4 cells, it abolished nuclear localization of ErbB-4 receptor tyrosine kinase by inhibiting the formation of the s80 ErbB-4 fragment. g-Secretase Inhibitor XIV 565775 [Z-Ct-Bu)-IL-CHO] A cell-permeable, reversible inhibitor of g-secretase that reduces Ab production (Ab IC = 90 nM; Ab IC = 780 nM) in solubilized 40 50 42 50 membrane preparations and in cultured APP695 expressing CHO cells (Ab IC = 80 nM; Ab IC = 20 nM). 40 50 42 50 g-Secretase Inhibitor XVI 565777 (DAPM; N-[N-3,5-Difluorophenacetyl]-L-alanyl-S-phenylglycine Methyl Ester) A cell-permeable g-secretase inhibitor with anti-aggregation property (Ab IC ~ 0 nM in 7PA2 cells). Prevents early Ab oligomerization by 50 selectively blocking the Ab dimer and trimer formation. InSolution g-Secretase Inhibitor XVII 565778 (31C; WPE-III-31C) Supplied as a 5 mM (500 mg/ 56 ml) solution in DMSO. A cellpermeable (hydroxyethyl) urea peptidomimetic that acts as a transition-state analog inhibitor of g-secretase (IC 50 = 300 nM for Ab production in whole cells). Binds the presenilin-g-secretase complex (PS -NTF, PS -CTF, Nicastrin, and C83 APP CTF). mg $ 07 5 mg $93 5 mg $93 250 mg $254 5 mg $98 5 mg $ 57 5 mg $ 73 5 mg $ 73 5 mg $96 500 mg $ 56 02 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
Calbiochem • Inhibitor SourceBook Neurobiology/Neurodegeneration Product Cat. No. Comments Size Price InSolution g-Secretase Inhibitor XIX 565787 {(2S,3R)-3-(3,4-Difluorophenyl)-2-(4-fluorophenyl)-4-hydroxy-N- ((3S)-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)butyramide} Supplied as a 5 mM ( 00 mg/37 ml) solution in DMSO. A cell-permeable, highly potent g-secretase inhibitor (IC 50 = 60 pM towards Ab 40 secretion in SH-SY5Y cells overexpressing spbA4CTF). N g-Secretase Inhibitor XX 565789 A cell-permeable, potent g-secretase inhibitor. Significantly lowers both the brain and plasma Ab 40 levels by ~72% in Tg2576 mutant APP transgenic mouse model ( 00 mM/kg, b.i.d.). Also potently inhibits Notch processing (IC 50 = .7 nM in SupT cells), and induces conversion of proliferative crypt cells into post-mitotic goblet cells in both C57BL/6 and APC Min mouse model ( 0 mM/kg, i.p.). N g-Secretase Inhibitor XXI 565790 A cell-permeable, potent, and selective peptidomimetic and nontransition-state analog inhibitor of g-secretase and Notch processing (IC 50 = 300 pM for Ab 40 in CHO cells overexpressing wild type bAPP; 240 pM for Ab 40 , 370 pM Ab 42 and 320 pM for NICD, respectively, in HEK293 cells stably transfected with bAPP 695 and mNotchDE(M 727V); 00 pM for both Ab 40 and Ab 42 in SH-SY5Y cells stably transfected with SPA4CT). Also lowers Ab levels in several APP transgenic mouse model. Reported to bind to presenilins and suppress the proteolytic ability to cleave several transmembrane protein substrates, including APLP and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75 NTR . Yet, at higher concentrations (200-400 mM) only weakly affects presenilin activity. N Secretase Inhibitors, continued g -Secretase Inhibitor I 40 565765 [N-trans-3,5-Dimethoxycinnamoyl)-Ile-leucinal; t-3,5-DMC-IL-CHO] A potent, cell-permeable, reversible inhibitor of g-secretase that preferentially inhibits the secretion of Ab (>90%) vs. Ab (~ 5%). -40 -42 IC = ~ 5 mM for Ab , ~22 mM for Ab , and >50 mM for Ab in 50 total -40 -42 CHO cells stably transfected with cDNA encoding bAPP695. Reported to be be about 0-fold more potent than Z-Val-Phe-CHO (MDL 28 70; Cat. No. 208722). g -Secretase Inhibitor II 40 565766 (N-tert-Butyloxycarbonyl-Gly-Val-Valinal) A cell-permeable, substrate-based (g -site) g-secretase inhibitor that 40 is reported to preferentially (> 90%) inhibit Ab cleavage at site 40 vs. 42, in a dose-dependent fashion, in transiently transfected 293T cells over-expressing APP695NL. Related Products InnoZyme TACE Activity Kit The InnoZyme TACE Activity Kit is a specific and sensitive assay kit designed to measure human TACE activity in cell lysates and biological samples and for screening enzyme inhibitors. An anti-human TACE monoclonal antibody pre-coated on a 96-well plate captures human TACE. The activity of captured TACE is measured using an internally quenched fluorescent substrate, MCA-KPLGL-Dpa-AR-NH 2 . Cleavage of the scissile amide bond, G-L, releases the fluorophore from the quenching molecule, Dpa, resulting in an increase in fluorescence. The level of fluorescence is directly related to the enzyme activity. kit = 96 tests Cat. No. CBA042 1 kit $425 00 mg $ 73 500 mg $ 9 500 mg $ 9 mg $99 mg 5 mg $50 $ 79 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 03
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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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Protein Tyrosine Kinase (PTK) Inhib
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Page 53 and 54: Protein Tyrosine Kinase (PTK) Inhib
Page 55 and 56: 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 and 98: Sphingomyelinase Inhibitors Ceramid
Page 99 and 100: Amyloidogenesis Inhibitors Calbioch
Page 101 and 102: Secretase Inhibitors Deposition of
Page 103: 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
Page 149 and 150: Inhibitors of Glycoprotein Processi
Page 151 and 152: Heat Shock Protein Inhibitors Heat
Page 153 and 154: 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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