Inhibitor SourceBook™ Second Edition

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Proteases Proteasome and Ubiquitination Inhibitors, continued Product Cat. No. N InSolution Proteasome Inhibitor I Proteasome Inhibitor II (Z-LLF-CHO) Proteasome Inhibitor III [Z-LLL-B(OH) 2 ] Proteasome Inhibitor IV (Z-GPFL-CHO) N Proteasome Inhibitor VII, Antiprotealide Cellpermeable? Reversible? Comments Size Price 539161 Yes Yes A 50 mM (5 mg/ 62 ml) solution of Proteasome Inhibitor I (Cat. No. 539 60) in DMSO. 539162 Yes Yes Inhibits chymotrypsin-like activity of the proteasomes (K i = 460 nM). 539163 Yes Yes Inhibits chymotrypsin-like activity of the proteasomes (K i = 30 nM). 539175 Yes Yes K i s = .5 mM for branched chain amino acid preferring, 2.3 mM for small neutral amino acid preferring, and 40.5 mM for chymotrypsin-like activities; IC 50 = 3. mM for PGPH activity. Only weakly inhibits trypsin-like proteasomal activity. 539179 Yes No An Omuralide-Salinosporamide hybrid that irreversibly inactivates the b5-subunit of the human 20S proteasome. Shown to be ~2.5-fold more potent than Omuralide (Cat. No. 426 02) and somewhat less potent than Salinosporamide A. Ro 06-9920 557550 Yes No A highly selective, irreversible inhibitor of IkBaee ubiquitination (IC 50 = 2.3 mM). Blocks NF-kB-dependent cytokine expression in human PBMNs (IC 50 ~700 nM for TNF-a, IL- b, and IL-6 inhibition) and rats. Ro 06-9920, Control 557551 Yes — A negative control compound for Ro 06-9920 (Cat. No. 557550) (IkBaee ubiquitination IC 50 >80 mM). Tyropeptin A, Synthetic 657008 Yes Yes Inhibitor of chymotrypsin-like (IC 50 = 00 ng/ml) and trypsin-like (IC 50 = .5 mg/ml) activities of the proteasome. No effect on PGPH activity even at a concentration of 00 mg/ml. Ubiquitin Aldehyde 662056 No Yes Potent and specific inhibitor of multiple ubiquitin hydrolases involved in pathways of intracellular protein modification and turnover. UCH-L Inhibitor 662086 Yes Yes A potent, reversible, competitive, and active site-directed inhibitor of UCH-L (K i = 400 nM; IC 50 = 880 nM) with ~28-fold greater selectivity over UCH-L3 (Cat. No. 662090). UCH-L3 Inhibitor 662089 Yes No A selective and potent inhibitor of UCH-L3 (IC 50 =600 nM) with ~ 25-fold greater selectivity over UCH-L (IC 50 = 75 mM). Proteasome Inhibitor Set I A set of three vials. Each set contains mg of Proteasome Inhibitor I (Cat. No. 539 60), 200 mg of Lactacystin (Cat. No. 426 00), and mg of MG- 32 (Cat. No. 474790). Cat. No. 539164 1 set $299 Proteasome Inhibitor Set II A set of three vials. Each set contains 5 mg of ALLN (Cat. No. 2087 9), 00 mg each of Epoxomicin (Cat. No. 324800), and clasto-Lactacystin b-Lactone (Cat. No. 426 02). Cat. No. 539165 1 set $313 The Ubiquitin- Proteasome Pathway A comprehensive collection of research products Order your FREE copy today! 5 mg $202 38 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem mg 5 mg $64 $ 90 00 mg $20 5 mg $ 68 50 mg $ 80 mg 5 mg $72 $25 mg $67 mg $60 50 mg $ 90 0 mg $93 0 mg $93
Transmembrane receptors of various hormones are coupled to adenylate cyclase (AC) via heterotrimeric G-proteins. Ligand binding to the receptor changes the receptor conformation, allowing it to associate with a G-protein. This results in the activation of the specific G-protein via exchange of GTP for GDP bound to the asubunit of the G-protein. The activated G-protein in turn activates AC resulting in the conversion of ATP to cAMP. cAMP then acts to regulate a wide variety of cellular processes. AC can couple with both the stimulatory and inhibitory G-proteins (G s and G i ). Interaction with G s stimulates its activity and interaction with G i inhibits its enzymatic activity. At least nine different isoforms of AC have been reported that differ in their regulatory properties and are differentially expressed in various tissues. They are integral membrane proteins that are composed of two cytoplasmic domains and two membrane-spanning domains, each of which contains six transmembrane spans. The amino acid sequence of each cytoplasmic domain, which is thought to contain a nucleotide (ATP) binding site, is well conserved among the various subtypes. Although ACs can exist in both particulate and soluble forms, the particulate form is more prevalent in mammals. Based on the conservation of their catalytic domains, three classes of ACs are described: class I-ACs are found in Gram-negative facultative anaerobes, such as E. coli; class II-“toxic' ACs, including calmodulin (CaM)-activated ACs are found in pathogenic bacteria, such as Bordetella Calbiochem • Inhibitor SourceBook Other Inhibitors of Biological Interest Other Inhibitors of Biological Interest Adenylate Cyclase Inhibitors Adenylate Cyclase Inhibitors pertussis and Bacillus anthracis; and class III-ACs are found in a wide variety of organisms ranging from bacteria to human. Class III-AC also include nine isoforms found in mammals, which are designated AC- 1 to AC-9. These nine isoforms are stimulated by the a-subunit of G s -protein and by forskolin. ACs are also capable of receiving signals from a variety of other sources, such as G i -a, protein kinase A, C, CaM kinase, and Ca 2+ /CaM. Hormonal activation of CaM-dependent adenylate cyclase occurs at very low Ca 2+ levels. The activity of AC is inhibited by high levels of Ca 2+ , which also activates CaM-dependent phosphodiesterase. References: Insel, P.A., and Ostrom, R.S. 2003. Cell. Mol. Neurobiol. 23, 305. Cui, H., and Green, R. D. 200 . Biochem. Biophys. Res. Comm. 283, 07. Schwartz, J.H. 200 . Proc. Natl. Acad. Sci. USA 98, 3482. Sunahara, R.K., et al. 996. Annu. Rev. Pharmacol. Toxicol. 36, 46 . MacNeil, S., et al. 985. Cell Calcium 6, 2 3. Product Cat. No. Comments Size Price Adenylyl Cyclase Toxins Inhibitor 116845 (Ethyl-5-aminopyrazolo[1,5-a]quinazoline-3-carboxylate) A cell-permeable inhibitor of adenylate cyclase (IC 50 = 90 mM). Adenylyl Cyclase Type V Inhibitor, NKY80 More online... www.calbiochem.com/inhibitors/AC 116850 [2-Amino-7-(furanyl)-7,8-dihydro-5(6H)-quinazolinone] A cell-permeable, potent and selective inhibitor of adenylyl cyclase (AC) type V isoform (IC 50 = 8 .3 mM, 32 mM and .7 mM for type V, III, and II, respectively) in the presence of Gsx GTPrs-Forskolin. Angiotensin II, Human 05-23-0101 (DRVYIHPF) An inhibitor of adenylate cyclase activity in spontaneously hypertensive rats. 2',5'-Dideoxyadenosine 288104 (2',5'-dd-Ado) A cell-permeable, non-competitive inhibitor of adenylate cyclase (IC 50 = 3 mM). Binds to the adenosine binding site. 0 mg $ 00 5 mg 25 mg mg 5 mg 25 mg $60 $2 $23 $34 $ 35 mg $53 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 39
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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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Raf Kinase Inhibitors Raf kinases a
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Rho Kinase (ROCK) Inhibitors, conti
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Protein Phosphatase Inhibitors Calb
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Protein Phosphatase Inhibitors, con
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Apoptosis Caspase Inhibitors Activa
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Caspase Inhibitors, continued Produ
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Other Selected Inhibitors of Apopto
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DNA Methyltransferase Inhibitors DN
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Histone Acetylase and Deacetylase I
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Related Products Histone Deacetylas
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Nuclear Import/Export Inhibitors, c
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Telomerase Inhibitors, continued Ca
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Topoisomerase Related Inhibitors, c
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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 •
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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: Proteasome and Ubiquitination Pathw
Page 143 and 144: Angiotensin-Converting Enzyme (ACE)
Page 145 and 146: ATPase Inhibitors, continued Calbio
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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
Page 155 and 156: NF-kB Activation Inhibitors NF-kB,
Page 157 and 158: NF-kB Activation Inhibitors, contin
Page 159 and 160: Phosphodiesterase (PDE) Inhibitors
Page 161 and 162: Plasminogen Activator Inhibitors Ti
Page 163 and 164: Protein Synthesis Inhibitors, conti
Page 165 and 166: Sonic Hedgehog Signaling Inhibitors
Page 167 and 168: Why can’t I make serial dilutions
Page 169 and 170: Calpastatin, Human, Recombinant, Do
Page 171 and 172: InSolution Microcystin-LR, Microcys
Page 173 and 174: RNA Polymerase III Inhibitor ......
Page 175 and 176: 324875 ............................
Page 177 and 178: Trademarks CALBIOCHEM®
Page 179 and 180: Your #1 Resource for Inhibitors! We
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