Inhibitor SourceBook™ Second Edition

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Phosphorylation/Dephosphorylation Calmodulin-Dependent Protein Kinase (CaM Kinase) Inhibitors Many effects of Ca 2+ are mediated by Ca 2+ / calmodulin(CaM)-dependent protein kinases (CaM kinases). CaM kinases constitute a family of structurally related enzymes that include phosphorylase kinase, myosin light chain kinase, and CaM kinases I-IV. CaM kinase II, one of the best-studied multifunctional enzymes, is found in high concentrations in neuronal synapses, and in some regions of the brain it may constitute up to 2% of the total protein content. Activation of CaM kinase II has been linked to memory and learning processes in the vertebrate nervous system. CaM kinase II is a complex of about 12 subunits that exist in four differentially expressed forms (a, b, g, and d). In the inactive state there is a strong interaction between the inhibitory and catalytic domains of the enzyme. The binding of Ca 2+ /CaM allows the catalytic domain to phosphorylate the inhibitory domain. Once activated, CaM kinase II retains significant activity even after the withdrawal of Ca 2+ , thereby prolonging the duration of kinase activity. Several synthetic and naturally occurring compounds have been shown to bind CaM in a Ca 2+ -dependent manner and block the activation of CaM-dependent enzymes. These compounds have been extensively used in investigating the mechanism of Ca 2+ -binding and activation in biological systems. References: Fujisawa, H. 2000. J. Biochem. (Tokyo) 129, 93. Rokolya, A., and Singer, H.A. 2000. Am. J. Physiol. 278, C537. Fukunaga, K., and Miyamoto, E. 999. Jap. J. Pharmacol. 79, 7. Kemp, B.E., et al. 994. In Protein Kinases (Woodgett, J.R., ed.), Oxford Univ. Press, N.Y. pp 30-67. ADP ATP More online... www.calbiochem.com/inhibitors/CAMK 6 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
Calmodulin-Dependent Protein Kinase (CaM Kinase) Inhibitors Calbiochem • Inhibitor SourceBook Phosphorylation/Dephosphorylation Product Cat. No. Comments Size Price Autocamtide-2 Related Inhibitory Peptide Autocamtide-2 Related Inhibitory Peptide II Autocamtide-2 Related Inhibitory Peptide II, Cell-permeable Autocamtide-2 Related Inhibitory Peptide, Myristoylated Calmodulin Binding Domain Ca 2+ /Calmodulin Kinase II Inhibitor 28 -309 [Ala 286 ]-Ca 2+ / Calmodulin Kinase II Inhibitor 28 -30 Calmodulin Kinase IINtide Calmodulin Kinase IINtide, Myristoylated 189480 [(Ala 9 )-Autocamtide-2; AIP; KKALRRQEAVDAL] Non-phosphorylatable analog of Autocamtide-2 (Cat. No. 89475) that is a highly specific and potent inhibitor of CaM kinase II (IC 50 = 40 nM). 189484 (A3K/V10F-AIP; AIP-II; KKKLRRQEAFDAL) An AIP-related peptide where Ala 3 and Val 0 are replaced with Lys and Phe. Highly specific and potent inhibitor of CaM kinase II (IC 50 = 4. nM). 189485 (Ac-RQIKIWFQNRRMKWKKKKKLRRQEAFDAL-OH; Ant-A3K/V10F-AIP; Ant-AIP-II) A highly specific, potent, cell-permeable inhibitor of CaM kinase II. Contains the Antennapedia transport peptide sequence fused to the N-terminus of AIP-II (Cat. No. 89484). 189482 (Myr-N-KKALRRQGAVDAL-OH; Myristoylated AIP) This peptide corresponds to AIP (Cat. No. 89480) which has been myristoylated at the N-terminus, enhancing its cell-permeability. 208734 (Calmodulin antagonist; CaM kinase II 290-309) A potent calmodulin antagonist that inhibits the activation of CaM kinase II (IC 50 = 52 nM). 208711 (CaM Kinase II Inhibitor 281-309; MHRQETVDCLKKFNARRKLKGAILTTMLA-OH) A synthetic peptide containing the CaM-binding domain (290-309) and the autophosphorylation site (Thr 286 ) of CaM kinase II. Inhibits CaM kinase II by blocking Ca 2+ / calmodulin activation (IC 50 = 80 nM) and enzyme-active site (IC 50 = 2 mM). 208710 (CaM Kinase II Inhibitor 281-301; MHRQEAVDCLKKFNARRKLKG-NH 2 ) A synthetic peptide corresponding to residues 28 -30 of the a subunit of CaM kinase II that acts as a potent inhibitor (IC 50 = 2 mM) of CaM kinase II catalytic fragment. Inhibition is competitive with respect to ATP and in a non-competitive manner with respect to peptide substrate. 208920 (KRPPKLGQIGRAKRVVIEDDRIDDVLK-OH) A potent and specific inhibitor of CaM kinase II (IC 50 = 50 nM). Does not affect the activity of CaM kinase I, IV, CaM KK, PKA, or PKC. 208921 (Myr-N-GGGKRPPKLGQIGRAKRVVIEDDRIDDVLK-OH) The myristoylated, cell–permeable form of CaM Kinase IINtide (Cat. No. 208920). H-89, Dihydrochloride 371963 {N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl} A cell-permeable, selective and potent inhibitor of protein kinase A (K i = 48 nM). Inhibits other kinases at higher concentrations: MLCK (K i = 28.3 mM), CaM kinase II (K i = 29.7 mM), PKC (K i = 3 .7 mM), casein kinase I (K i = 38.3 mM), and Rho Kinase II (IC 50 = 270 nM). Not available for sale in Japan. HA 004, Dihydrochloride K-252a, Nocardiopsis sp. InSolution K-252a, Nocardiopsis sp. 371964 [N-(2-Guanidinoethyl)-5-isoquinolinesulfonamide, 2HCl] An inhibitor of CaM kinase II (K i = 3 mM), MLCK (K i = 50 mM), PKA (K i = 2.3 mM), PKC (K i = 40 mM), and PKG (K i = .3 mM). Not available for sale in Japan. 420298 A cell-permeable inhibitor of CaM kinase II (K i = .8 nM), MLCK (K i = 7 nM), protein kinase A (K i = 8 nM), protein kinase C (K i = 25 nM), and protein kinase G (K i = 20 nM). 500 mg $ 9 mg $ 06 mg $2 7 500 mg $ 5 mg $ 07 500 mg $ 6 500 mg $208 mg $ 07 mg $ 7 mg $84 mg $57 00 mg $ 33 420297 A mM ( 00 mg/2 4 ml) solution of K-252a (Cat. No. 420298) in anhydrous DMSO. 00 mg $ 28 KN-62 422706 {1-[N,O-bis-(5-Isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine} A cell-permeable, selective inhibitor of CaM kinase II (K i = 900 nM) that binds directly to the CaM-binding site of the enzyme. Not available for sale in Japan. KN-92 422709 {2-[N-(4-Methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine, Phosphate} Useful as a negative control for KN-93 (Cat. No. 422708), a CaM kinase II inhibitor. KN-93 422708 {2-[N-(2-hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)- N-methylbenzylamine)} A cell-permeable, competitive inhibitor of rat brain CaM kinase II (K i = 370 nM). Selectively binds to the CaM-binding site of the enzyme and prevents the association of CaM with CaM kinase II. mg $ 03 mg $ 03 KN-93, Water-Soluble 422711 A water-soluble form of the CaM kinase II inhibitor KN-93 (Cat. No. 422708). mg $ 03 InSolution KN-93 422712 A 5 mM ( mg/399 ml) solution of KN-93 Inhibitor (Cat. No. 422708) in DMSO. mg $ 09 mg 5 mg $ 03 $36 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 7
Page 1 and 2: Inhibitor SourceBook Second Editio
Page 3 and 4: Calbiochem • Inhibitor SourceBook
Page 7: Akt (Protein Kinase B) Inhibitors,
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 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
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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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Calbiochem • Inhibitor SourceBook
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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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Secretase Inhibitors Calbiochem •
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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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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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