Inhibitor SourceBook™ Second Edition

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Other Inhibitors of Biological Interest Inhibitors of Mitochondrial Function, continued Product Cat. No. Comments Size Price Ru360 557440 [(m)[(HCO 2 )(NH 3 )4Ru] 2 OCl 3 ] A cell-permeable oxygen-bridged dinuclear ruthenium amine complex that has been shown to bind to mitochondria with high affinity (K d = 340 pM). Specifically blocks Ca 2+ uptake into mitochondria in vitro (IC 50 = 84 pM) and in situ in intact myocytes (complete block after incubation with ~ 0 mM of Ru360 for 30 min). Does not affect other cellular Ca 2+ transport processes involved in cardiac muscle contraction, even at micromolar levels. ( set = 0 × 0 mg) SFK 565833 (Suppressor of FK-506 1) A cell-permeable amidine compound that has been shown to interact with Por p (YVDAC ), a channel protein in the outer mitochondrial membrane, and to modulate ionic balance in Saccharomyces cerevisiae. It suppresses the ability of FK-506 to inhibit yeast growth in high NaCl-containing media (IC 50 ~ .5–2.5 mM), while in low NaCl-containing media, it causes mitochondrially-induced death by stimulating the release of reactive oxygen species (ROS). Valinomycin, Streptomyces fulvissimus Mitochondrial Permeability Transition Pore Reagents Set Contains g of Adenosine 5'-Diphosphate, Potassium Salt (Cat. No. 7 05), 500 mg of Bongkrekic Acid, Triammonium Salt (Cat. No. 20367 ), 5 mg of Carboxyatractyloside, Atractylis gummifera (Cat. No. 2 6200), and 00 mg of Cyclosporin A, Tolypocladium inflatum (Cat. No. 239835). Cat. No. 475876 1 set $325 676377 A cyclododecadepsi-peptide ionophore antibiotic. Potassium ionophore of the mobile ion-carrier type that transports alkali metal ions across artificial or biological lipid membranes. Induces K + conductivity in cell membranes at concentrations as low as 0 -8 M. Often used in membrane electrode systems for determining K + concentration. Uncouples oxidative phosphorylation by binding to sites on membranes rich in sulfhydryl groups. Induces apoptosis in murine thymocytes. Also reported to inhibit NGF-induced neuronal differentiation. 52 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem 500 mg mg set $ 46 $255 $352 0 mg $ 26 25 mg 00 mg $65 $225
NF-kB Activation Inhibitors NF-kB, a eukaryotic transcription factor plays an important role in inflammation, autoimmune response, cell proliferation, and apoptosis by regulating the expression of genes involved in these processes. It consists of homo- or heterodimers of different subunits, which belong to a family of Rel/NF-kB proteins. Five different Rel proteins [p50, p52, p65 (Rel A), RelB, and c-Rel] have been identified thus far. The most prevalent activated form of NF-kB is a heterodimer of p50 or p52 subunit and p65, which contains transactivation domains necessary for gene induction. In unstimulated cells, NF-kB is sequestered in the cytoplasm in an inactive form, bound to regulatory proteins called inhibitors of kB (IkB), of which IkBa and IkBb are considered to be the most important. IkBa is associated with transient NF-kB activation, whereas IkBb is involved in sustained activation. The activity of NF-kB is tightly regulated by interaction with inhibitory IkB proteins. In most resting cells, NFkB is sequestered in the cytoplasm in an inactive form associated with inhibitory molecules, such as IkBa, IkBb, IkBh, p105, and p100. This interaction blocks the ability of NF-kB to bind to DNA and results in the NF-kB complex being primarily localized to the cytoplasm due to a strong nuclear export signal in IkBa. Stimulation of cells by inflammatory cytokines, UV light, or reactive oxygen species leads to the rapid phosphorylation, ubiquitination, and ultimately Calbiochem • Inhibitor SourceBook Other Inhibitors of Biological Interest proteolytic degradation of IkB, which frees NF-kB from the NF-kB-IkB complex. NF-kB then translocates to the nucleus where it binds to kB enhancer elements of proinflammatory target genes to induce transcription. NFkB is highly activated at sites of inflammation in diverse diseases and induces transcription of pro-inflammatory cytokines, chemokines, adhesion molecules, MMPs, COX-2, and inducible nitric oxide (iNOS). Hence, NF-kB has been considered as a desirable target for therapy in various inflammatory diseases. In most cancer cells, NF-kB is constitutively active and resides in the nucleus. In some cases, this may be due to chronic stimulation of the IKK pathway, while in others the gene encoding IkBa may be defective. Such continuous nuclear NF-kB activity not only protects cancer cells from apoptotic cell death, but may even enhance their growth activity. Designing antitumor agents to block NF-kB activity or to increase sensitivity to conventional chemotherapy may have great therapeutic value. References: Pande, V., and Ramos, M. J. 2005. Curr. Med. Chem. 12, 357. Bouwnecster, T. et al. 2004. Nat. Cell Biol. 6, 97. Marienfeld, R., et al. 2003. J. Biol. Chem. 278, 9852. Ghosh, S., and Karin M. 2002. Cell 109, S8 . Delhase, M., et al. 999. Science 284, 309. Rahman, A., et al. 999. J. Immunol. 162, 5466. Miyazawa, K., et al. 998. Am. J. Pathol. 152, 793. Zandi, E., et al. 998. Science 281, 360. Stancovski, I., and Baltimore, D. 997. Cell 91, 299. Baldwin, A.S. Jr. 996. Annu. Rev. Immunol. 14, 649. More online... www.calbiochem.com/inhibitors/NFKB Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 53
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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
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Cyclooxygenase (COX) Inhibitors, co
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HMG-CoA (3-Hydroxy-3-Methylglutaryl
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Lipoxygenase (LOX) Inhibitors Lipox
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Phospholipase Inhibitors Several si
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Sphingomyelinase Inhibitors Ceramid
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Amyloidogenesis Inhibitors Calbioch
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Secretase Inhibitors Deposition of
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Page 111 and 112: Characteristics of various forms of
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Page 115 and 116: Proteases Anthrax Lethal Factor (LF
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Page 119 and 120: Collagenase Inhibitors (Also see Ma
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Page 143 and 144: Angiotensin-Converting Enzyme (ACE)
Page 145 and 146: ATPase Inhibitors, continued Calbio
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Page 159 and 160: Phosphodiesterase (PDE) Inhibitors
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Page 165 and 166: Sonic Hedgehog Signaling Inhibitors
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Page 171 and 172: InSolution Microcystin-LR, Microcys
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Page 177 and 178: Trademarks CALBIOCHEM®
Page 179 and 180: Your #1 Resource for Inhibitors! We
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