Inhibitor SourceBook™ Second Edition

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Phosphorylation/Dephosphorylation Calmodulin-Dependent Protein Kinase (CaM Kinase) Inhibitors, continued Product Cat. No. Comments Size Price Lavendustin C 234450 [Compound 5; 5-(N-2´,5´-Dihydroxybenzyl)aminosalicylic Acid] Potent inhibitor of CaM kinase II (IC 50 = 200 nM) and pp60 c-src (IC 50 = 200 nM). N PP Analog II, NM-PP 529581 A cell-permeable PP analog (Cat. No. 529579) that acts as a potent and selective ATPcompetitive inhibitor of a variety of mutant kinases over wild-type (IC 50 = 3.2 nM for T339G, c-Fyn-as vs. .0 mM for c-Fyn; 4.3 nM for I338G, v-src-as vs. 28 mM for v-src; 5 nM for F80G, CDK2-as vs. 29 mM for CDK2; 8 nM for F89G, CAMK IIa-as vs. 24 mM for CAMKII; 20 nM for T3 5A, c-Abl-as2 vs. 3.4 mM for c-Abl). Shown to activate mutants of Ire , a transmembrane kinase. STO-609 570250 A cell-permeable, highly selective, potent, ATP-competitive inhibitor of CaM kinase kinase (CaM-KK) (IC 50 = 320 nM and 06 nM for CaM-KKa and CaM-KKb isoforms, respectively). Binds to the catalytic domain of CaM-KK, and inhibits autophosphorylation. TX-1918 A cell-permeable, potent inhibitor for eEF2 kinase (IC 50 = 440 nM). Inhibits other kinases at much higher concentrations (IC 50 = 4.4, 44, 44, and 440 mM for Src, PKA, PKC, and EGFR kinase, respectively). Cat. No. 655203 10 mg $90 Including Oncogene Research Products mg $62 mg $82 5 mg $ 73 Featuring 50 NEW products 8 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
Casein Kinase (CK) Inhibitors Casein kinases I and II (CKI and CKII) are highly conserved, ubiquitous serine/threonine protein kinases that play a significant role in neoplasia and cell survival. CKI can be found in the nucleus and the cytosol and is bound to the cytoskeleton and membranes. The CKI family consists of several isoforms (CKIa, b, g1, g2, g3, d, and e) encoded by seven distinct genes. It plays a significant role in the regulation of circadian rhythm, intracellular trafficking and also acts as a regulator of Wnt signaling, nuclear import, and the progression of Casein Kinase (CK) Inhibitors Calbiochem • Inhibitor SourceBook Phosphorylation/Dephosphorylation Alzheimer’s disease. CKII has traditionally been classified as a messenger-independent protein serine/threonine kinase and consists of two catalytic and two regulatory subunits. It plays an important role in the progression of the cell cycle and in maintenance of cell viability. It is highly conserved and is known to phosphorylate about 300 different proteins. CKII activity is required at transition points of the cell cycle. Excessive activity of CKII has been linked to oncogenic transformation and the development of primary and metastatic tumors. Product Cat. No. Comments Size Price A3, Hydrochloride 100122 [N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide, HCl] A shorter alkyl chain derivative of W-7 (Cat. No. 68 629) that inhibits CKI (K i = 80 mM), CKII (K i = 5. mM), MLCK (K i = 7.4 mM), PKA (K i = 4.3 mM), PKC (K i = 47 mM), and PKG (K i = 3.8 mM). N Casein Kinase I Inhibitor, D4476 N InSolution Casein Kinase I Inhibitor, D4476 Casein Kinase II Inhibitor I N InSolution Casein Kinase II Inhibitor I N Casein Kinase II Inhibitor II, DMAT N InSolution Casein Kinase II Inhibitor, DMAT 218696 {CKI Inhibitor; 4-(4-(2,3-Dihydrobenzo[1,4]dioxin-6-yl)-5-pyridin-2-yl-1H-imidazol- 2-yl)benzamide} A cell-permeable, potent, and relatively specific ATP-competitive inhibitor of CKI (IC 50 = 200 nM from S. pombe; 300 nM for CKId). Shown to be ~ 0-fold more potent than IC26 (Cat. No. 400090; IC 50 = 2.5 mM for CKI). 218705 A 0 mM ( mg/25 ml) solution of Casein Kinase I Inhibitor, D4476 (Cat. No. 2 8696) in DMSO. 218697 (CKII Inhibitor; TBB; TBBt; 4,5,6,7-Tetrabromo-2-azabenzimidazole; 4,5,6,7- Tetrabromobenzotriazole) A cell-permeable, highly selective, ATP/GTP-competitive CKII inhibitor (IC 50 = 900 nM and .6 mM for rat liver and human recombinant CKII, respectively and DYRK (IC 50 < mM for DYRK a). 218708 A 0 mM (5 mg/ . 5 ml) solution of Casein Kinase II Inhibitor I (Cat. No. 2 8697) in DMSO. 218699 (CKII Inhibitor II, DMAT; 2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole) A cell-permeable, potent, high affinity and ATP-competitive inhibitor of CKII (IC 50 = 40 nM rat liver; K i = 40 nM). Displays ~ 300 fold greater selectivity over CKI (IC 50 > 200 mM) and is superior to CKII inhibitor, TBB (Cat. No. 2 8697). 218706 A 0 mM (5 mg/ .05 ml) solution of Casein Kinase II Inhibitor, DMAT (Cat. No. 2 8699), in DMSO. Daidzein 251600 (4´,7-Dihydroxyisoflavone) Inactive analog of Genistein that is reported to inhibit casein kinase II activity. 5,6-Dichloro- -b-Dribofuranosylbenz– imidazole 287891 (5,6-Dichlorobenzimidazole Riboside; DRB) Potent and specific inhibitor of casein kinase II (IC 50 = 6 mM). Ellagic Acid, Dihydrate 324683 4,4′,5,5′,6,6′-Hexahydroxydiphenic Acid 2,6,2′,6′-Dilactone A cell-permeable, potent, selective and ATP-competitive inhibitor of CKII (IC 50 = 40 nM). H-89, Dihydrochloride 371963 {N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl} A cell-permeable, selective and potent inhibitor of PKA (K i = 48 nM). At higher concentrations it also inhibits MLCK (K i = 28.3 mM), CaM kinase II (K i = 29.7 mM), PKC (K i = 3 .7 mM), CKI (K i = 38.3 mM), and Rho kinase II (IC 50 = 270 nM). Not available for sale in Japan. InSolution H-89, Dihydrochloride More online... www.calbiochem.com/inhibitors/CK 371962 N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl A 0 mM ( mg/ 93 µl) solution of H-89, Dihydrochloride (Cat. No. 37 963) in DMSO. Not available for sale in Japan. Key: CKI: Casein kinase I; CKII: Casein kinase II; MLCK: Myosin light chain kinase; PKA: Protein kinase A; PKC: Protein kinase C 0 mg $90 mg $ 2 mg $ 2 0 mg $73 5 mg $53 5 mg $90 5 mg $90 25 mg $47 50 mg $90 500 mg $57 mg $84 mg $84 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 9
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: Calmodulin-Dependent Protein Kinase
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
Page 59 and 60: 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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