Inhibitor SourceBook™ Second Edition

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Cell Division/Cell Cycle/Cell Adhesion Telomerase Inhibitors Telomerase is a specialized ribonucleoprotein composed of a catalytic subunit telomerase reverse transcriptase (TERT), and two other subunits known as telomerase associated protein 1 (TP1), and a ~445-nucleotide long telomerase RNA component (TR). Telomerase stabilizes telomere lengths by adding hexameric (TTAGGG) repeats to the ends of chromosomes, thereby circumventing the cumulative damage that normally occurs during mitotic cell division. Telomerase recognizes the G-rich strand of an existing telomere repeat sequence and elongates it in the 5´-to-3´ direction. Progressive loss of telomeres, a key feature of normal cells, is considered to be a major regulator of cellular senescence. Tumor cells overcome this problem by overexpressing telomerase. As cancer cells divide more often, on an average, they possess shorter telomeres than normal cells. Hence, without an active telomerase to maintain telomere length, cancer cells could reach critically short telomere at a faster pace than normal cells. Telomerase activity, which is practically undetectable in normal cells, is detected in the majority of tumor cells. The presence of telomerase activity is correlated with poor clinical outcome in cancer patients. Hence, telomerase inhibitors Telomerase Inhibitors are considered as potential therapeutic agents for the management of tumor progression. Promising approaches for telomerase inhibition include the use of mutant dominant/negative versions of human TERT (hTERT) and the use of antisense oligonucleotides directed against the template RNA component (hTR) of the telomerase holoenzyme. These telomerase inhibitors reduce telomerase activity and lead to progressive shortening of telomeres with each cell division, ultimately causing cells to undergo apoptosis. References: Altshuler, M.L., et al. 2003. Biochemistry (Mosc). 68, 275. Mokbel, K. 2003. Curr. Med. Res. Opin. 19, 470. Wu, X., et al. 2003. J. Natl. Cancer Inst. 95, 2 . Gomez, D., et al. 2002. Cancer Res. 62, 3365. Shay, J.W., et al. 200 . Hum. Mol. Gen. 10, 677. Rahat, M.A., et al. 999. Cancer 85, 9 9. Roos, G., et al. 998. Int. J. Cancer 79, 343. Wen, J., et al. 998. Mol. Diagn. 3, 29. Kim, N.W. 997. Eur. J. Cancer 33, 78 . Shay, J.W. 997. J. Cell. Physiol. 173, 266. Harrington, L., et al. 997. Science 275, 973. Product Cat. No. Comments Size Price 3´-Azido-3´- deoxythymidine InSolution AZT, Triphosphate, Tetralithium Salt 3´-Deoxy-2´,3´- didehydrothymidine Ellipticine, 9-Hydroxy-, Hydrochloride (–)-Epigallocatechin Gallate More online... www.calbiochem.com/inhibitors/telomerase 194348 (AZT) Inhibitor of HIV- reverse transcriptase that blocks the incorporation of nucleotides into newly synthesized DNA. Causes irreversible telomere shortening. 194950 (AZTTP) A reverse transcriptase inhibitor that acts by docking to the active site of HIVreverse transcriptase. Also reported to inhibit telomerase activity in vitro (IC 50 = 30 mM). 257920 A reverse transcriptase inhibitor that causes a consistent and rapid telomere shortening in vegetatively growing Tetrahymena. 324680 (9-HE, HCl) An antitumor alkaloid that is reported to inhibit telomerase activity in cultured pancreatic cancer cells, in a time- and concentration-dependent manner, possibly through inhibition of protein kinases. It also acts as a potent inhibitor of topoisomerase II (IC 50 = 3.3 mM). 324880 {EGCG; (2R,3R)-2-(3,4,5-Trihydroxyphenyl)-3,4-dihydro-1[2H]-benzopyran-3,5,7triol-3-(3,4,5-trihydroxybenzoate)} A polyphenolic constituent of green tea with potent antitumor, anti-inflammatory, and antioxidant properties. Strongly and directly inhibits telomerase activity in cell-free systems and in cancer cell lines. PIPER 528120 {N,N´-bis[2-(1-Piperidino)ethyl]-3,4,9,10-perylenetetracarboxylic Diimide; Telomerase Inhibitor IV} A perylene-based ligand that potently inhibits human telomerase activity by binding to G-quadruplex DNA. The strongest binding site for PIPER appears to be the 3'-boundary of the G-quadruplex. Can also bind non-specifically to nucleic acids. 0 mg $39 mmol $ 60 25 mg $76 0 mg $55 0 mg $39 0 mg $85 80 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
Telomerase Inhibitors, continued Calbiochem • Inhibitor SourceBook Cell Division/Cell Cycle/Cell Adhesion Product Cat. No. Comments Size Price Telomerase Inhibitor III, Sodium Salt Telomerase Inhibitor III, Negative Control, Sodium Salt Telomerase Inhibitor VI, Sodium Salt 581004 [5´-d(TTAGGG)-3´; TAG-6] A short hexameric phosphorothioate oligonucleotide (PS-ODN) telomere mimic that inhibits telomerase activity in cell lysates and lengthens cell doubling time in vitro and in vivo at concentrations less than 2.5 mM. 581007 [5´-d(TGTGAG)-3´] A control containing scrambled sequence of the short hexameric phosphorothioate oligonucleotide PS-ODN (Cat. No. 58 004). Useful as a control in experiments to show the specificity of PS-ODN-mediated biological effects. 581006 (5´-CAGUUAGGGUUAG-3´; 2´-O-MeRNA) A 3-nucleotide 2'-O-MeRNA possessing terminal phosphorothioate linkages. Potently inhibits telomerase activity (IC 50 = 2 nM at 23˚C and 3 nM at 37˚C). Telomerase Inhibitor IX 581011 [N,N´-bis(2,3-Dihydroxybenzoyl)-1,3-phenylenediamine; MST-312] A cell-permeable, potent, and reversible inhibitor of telomerase activity (IC = 670 nM, TRAP lysate prepared from U937 cells). Prolonged treatment with 50 MST-3 2 has been reported to result in telomere shortening and growth arrest in U937 cells. Does not inhibit the activity of Taq DNA polymerase (IC > 3 mM). 50 TMPyP4 613560 [meso-5,10,15,20-Tetrakis-(N-methyl-4-pyridyl)porphine, Tetratosylate] A potent inhibitor of human telomerase (IC = 6.5 mM). TMPyP4 binds strongly 50 to DNA quadruplexes by stacking on the G-tetrads at the core of the quadruplex, resulting in telomerase inhibition. Fluoresces highly in the presence of quadruplex DNA. To view our collection of telomerase-related antibodies, visit our antibody resource www.calbiochem.com/antibodyresource 50 nmol $75 50 nmol $76 00 nmol $ 53 0 mg $ 03 25 mg $73 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 8
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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
Page 31 and 32: Myosin Light Chain Kinase (MLCK) In
Page 33 and 34: Phosphatidylinositol 3-Kinase (PI 3
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Page 37 and 38: Protein Kinase A (PKA; cAMP-Depende
Page 39 and 40: Isozyme Specificities of Selected P
Page 41 and 42: Protein Kinase C (PKC) Inhibitors,
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
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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 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
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Page 125 and 126: Tissue Inhibitors of Matrix Metallo
Page 127 and 128: Protease Inhibitors The proper func
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Protease Inhibitors, continued Sele
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Protease Inhibitor Cocktails, conti
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N Animal-Free Protease Inhibitor Co
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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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