Inhibitor SourceBook™ Second Edition

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Phosphorylation/Dephosphorylation Protein Kinase C (PKC) Inhibitors, continued Product Cat. No. Comments Size Price Protein Kinase C e Translocation Inhibitor Peptide Protein Kinase C e Translocation Inhibitor Peptide, Negative Control 539522 (EAVSLKPT; PKC e Translocation Inhibitor Peptide) An octapeptide that selectively inhibits the translocation of PKC e to subcellular sites. Inhibition of PKC e translocation is known to specifically block phorbol ester or norepinephrine-mediated regulation of contraction in cardiomyocytes. 539542 (LSETKPAV) A scrambled peptide with an identical amino acid composition to that of PKC e Translocation Inhibitor Peptide (Cat. No. 539522). Useful as a negative control for this PKC e translocation inhibitor. Ro-3 -7549 557508 {2-[1-3(Aminopropyl)indol-3-yl]-3(1-methyl-1H-indol-3-yl)maleimide, Acetate; Bisindolylmaleimide VIII, Acetate} Ro 3 -7549, Immobilized A selective PKC inhibitor that acts at the ATP binding site of PKC (IC 50 = 58 nM for rat brain PKC). IC 50 values for individual PKC isozymes are as follows: 53 nM for PKC a , 95 nM for PKC bI , 63 nM for PKC bII , 2 3 nM for PKC g , and 75 nM for PKC e . 557509 An immobilized form of the PKC inhibitor Ro-3 -7549 (Cat. No. 557508) that is covalently attached to hydrophilic acrylic beads via an 8-carbon spacer. Useful to affinity-precipitate PKC and other functionally related proteins from cell or tissue extracts. Binding capacity: ≥3 mg purified PKC a per gram of dry beads. Ro-3 -8220 557520 {3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide; Bisindolylmaleimide IX, Methanesulfonate} N InSolution Ro-3 -8220 A competitive, selective inhibitor of PKC (IC 50 = 0 nM) over PKA (IC 50 = 900 nM), CaM kinase (IC 50 = 7 mM) and phosphorylase protein kinase. 557521 {3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide; Bisindolylmaleimide IX, Methanesulfonate} A 5 mM (500 mg/ 8 ml) solution of Ro-3 -8220 (Cat. No. 557520) in H 2 O. Ro-3 -8425 557514 {2-[8-(Aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-3-(1-methyl-1H-indol- 3-yl)maleimide, HCl; Bisindolylmaleimide X, HCl} A potent and selective inhibitor of PKC (IC 50 = 5 nM for rat brain PKC). Exhibits some degree of isozyme specificity (IC 50 = 8 nM for PKC a , 8 nM for PKC bI , 4 nM for PKC bII , 3 nM for PKC g , and 39 nM for PKC e ). Shows slight selectivity for the conventional PKC isozymes PKC a , PKC b , and PKC g over the Ca 2+ -independent PKC isozyme PKC e . Ro-32-0432 557525 {Bisindolylmaleimide XI, HCl; 2-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido [1,2-a]indol-3-yl}-3-(1-methyl-1H-indol-3-yl)maleimide, HCl} A selective cell-permeable PKC inhibitor. Displays about a 0-fold greater selectivity for PKC a (IC 50 = 9 nM) and a 4-fold greater selectivity for PKC bI (IC 50 = 28 nM) over PKC e (IC 50 = 08 nM). Rottlerin 557370 (Mallotoxin) An inhibitor of PKC d (IC 50 = 3-6 mM) and PKC θ . Also inhibits PKC a , PKC b , and PKC g isoforms, but with significantly reduced potency (IC 50 = 30-42 mM). Has reduced inhibitory activity on PKC e , PKC h , and PKC x (IC 50 = 80- 00 mM). Also known to inhibit CaM kinase III (IC 50 = 5.3 mM). Safingol 559300 (L-threo-Dihydrosphingosine) A lyso-sphingolipid PKC inhibitor that competitively interacts at the regulatory phorbol binding domain of PKC. Inhibits enzymatic activity and 3 H-phorbol dibutyrate binding of purified rat brain PKC (IC 50 = 37.5 mM and 3 mM, respectively). Inhibits human PKC a in MCF-7 DOXR cells (IC 50 = 40 mM). Sangivamycin 559307 (7-Deaza-7-carbamoyladenosine; NSC-65346) A cytotoxic purine nucleoside that acts as a selective and potent inhibitor of PKC (IC 50 = 0 mM). The inhibition is competitive with respect to ATP and non-competitive with respect to histone and lipid cofactors. D-erythro-Sphingosine, Free Base, Bovine Brain D-erythro-Sphingosine, Free Base, High Purity 567725 (trans-D-erythro-2-Amino-4-octadecene-1,3-diol; Ceramide; Cerebroside) A potent and selective inhibitor of PKC (PKC; IC 50 = 2.8 mM) and insulin receptor tyrosine kinase. PKC inhibition is competitive with respect to diacylglycerol, phorbol dibutyrate, and Ca 2+ . 567726 (trans-D-erythro-2-Amino-4-octadecene-1,3-diol; Ceramide; Cerebroside) A highly purified preparation of Cat. No. 567725 containing >99% of the erythro isomer. A potent and selective inhibitor of PKC (IC 50 = 2.8 mM) and insulin receptor tyrosine kinase. PKC inhibition is competitive with respect to diacylglycerol, phorbol dibutyrate, and Ca 2+ . 5 mg $ 56 5 mg $ 56 mg $95 set $ 32 500 mg $83 500 mg $83 mg $95 40 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem 500 mg mg $70 $ 2 0 mg $77 mg $ 2 mg $87 0 mg $69 0 mg $83
Calbiochem • Inhibitor SourceBook Phosphorylation/Dephosphorylation Product Cat. No. Comments Size Price D-erythro-Sphingosine, Dihydro- D-erythro-Sphingosine, N,N-Dimethyl- N Scytonemin, Lyngbya sp. N Protein Kinase C (PKC) Inhibitors, continued Staurosporine, Streptomyces sp. 300230 (Sphinganine) Biosynthetic precursor of sphingosine. Inhibits PKC in Chinese hamster ovary cells (IC 50 = 2.9 mM). 0 mg $79 310500 A PKC inhibitor (IC 50 = 2 mM) that also enhances src kinase activity. 5 mg $8 565715 (SCY) A cell-permeable, dimeric indolo-phenol compound that acts as a selective, reversible, non-toxic, and mixed type inhibitor of polo-like kinase (Plk ; IC 50 = 2.0 mM) and PKC bI (IC 50 = 3.4 mM) and exhibits anti-proliferative and anti-inflammatory properties. Also inhibits several other cell cycle regulatory kinases, and PKC bII (IC 50 = .2 mM, .4 mM, 3.0 mM, and 2.7 mM for Myt , Chk , Cdk /B, and PKC bII ). At higher concentrations, affects the activities of PKA and Tie2 (IC 50 > 0 mM). 569397 A potent, cell-permeable broad spectrum inhibitor of protein kinases. Inhibits CaM kinase (IC 50 = 20 nM), MLCK (IC 50 = .3 nM), PKA (IC 50 = 7 nM), PKC (IC 50 = 700 pM), and PKG (IC 50 = 8.5 nM). 00 mg 250 mg mg $98 Tamoxifen Citrate 579000 A potent synthetic anti-estrogen. A reversible inhibitor of PKC (IC 50 = 0 mM). 00 mg $4 Tamoxifen, 4-Hydroxy-, (Z)- 579002 [(Z)-4-Hydroxytamoxifen; 4-OH-TAM] An active metabolite of the widely used therapeutic anti-estrogen agent, tamoxifen (Cat. No. 579000) that is more potent than the parent compound. Inhibits PKC by modifying its catalytic domain. TER 4687 581800 [(±)-2N,N-Dimethylaminomethyl-1-indanone, HCl] Blocks the association between protein kinase C θ -V and p59fyn in a yeast reporter assay. Prevents normal translocation of PKC θ in T cells. Has no effect on other PKC isozymes in Jurkat or normal T cells. Vitamin E Succinate 679130 (a-Tocopheryl Succinate; VES) Enhances the immune response and induces cellular differentiation and/or growth inhibition. VES has been shown to modulate adenylate cyclase and cAMP-dependent proteins, inhibit protein kinase C activity, bind to a cellular vitamin E binding protein, suppress c-myc and c-H-ras oncogene expression, and regulate TGF-b protein production. Also shown to induce apoptosis in RL cells. Exhibits antioxidant properties. Polo-like Kinase Inhibitor Scytonemin, Lyngbya sp. To view all PKC research-related products and to request your free PKC wall poster, visit our PKC Interactive Pathways at: www.calbiochem.com/pkc A cell-permeable, dimeric indolo-phenol compound that acts as a selective, reversible, non-toxic, and mixed type inhibitor of polo-like kinase (Plk ; IC 50 = 2.0 mM) and PKC bI (IC 50 = 3.4 mM) and exhibits anti-proliferative and anti-inflammatory properties. Also inhibits several other cell cycle regulatory kinases, and PKC bII (IC 50 = .2 mM, .4 mM, 3.0 mM, and 2.7 mM for Myt , Chk , Cdk /B, and PKC bII ). At higher concentrations, affects the activities of PKA and Tie2 (IC 50 > 0 mM). Cat. No. 565715 1 mg $98 $ 43 $302 5 mg $97 0 mg $ 23 00 mg $34 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 4
Page 1 and 2: Inhibitor SourceBook Second Editio
Page 3 and 4: Calbiochem • Inhibitor SourceBook
Page 7 and 8: Akt (Protein Kinase B) Inhibitors,
Page 9 and 10: Calmodulin-Dependent Protein Kinase
Page 11 and 12: Casein Kinase (CK) Inhibitors Casei
Page 13 and 14: Checkpoint Kinase Inhibitors Eukary
Page 15 and 16: Cyclin-Dependent Kinase (Cdk) Inhib
Page 21 and 22: Glycogen Synthase Kinase-3 (GSK-3)
Page 23 and 24: Glycogen Synthase Kinase Inhibitors
Page 25 and 26: c-Jun N-Terminal Kinase (JNK/SAP Ki
Page 27 and 28: Mitogen-Activated Protein (MAP) Kin
Page 29 and 30: MAP Kinase Inhibitors, continued Ca
Page 31 and 32: Myosin Light Chain Kinase (MLCK) In
Page 33 and 34: Phosphatidylinositol 3-Kinase (PI 3
Page 37 and 38: Protein Kinase A (PKA; cAMP-Depende
Page 39 and 40: Isozyme Specificities of Selected P
Page 41: 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
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
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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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Secretase Inhibitors Calbiochem •
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Calbiochem • Inhibitor SourceBook
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Glutathione S-Transferase (GST) Inh
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Guanylate Cyclase Inhibitors, conti
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Characteristics of various forms of
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Nitric Oxide Synthase (NOS) Inhibit
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Proteases Anthrax Lethal Factor (LF
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the ratio of active (76 kDa) to ina
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Collagenase Inhibitors (Also see Ma
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Matrix Metalloproteinase (MMP) Inhi
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Matrix Metalloproteinase Inhibitors
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Tissue Inhibitors of Matrix Metallo
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Protease Inhibitors The proper func
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Protease Inhibitors, continued Calb
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Protease Inhibitors, continued Calb
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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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Calbiochem • Inhibitor SourceBook
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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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