Inhibitor SourceBook™ Second Edition

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Cell Division/Cell Cycle/Cell Adhesion Did you know Calbiochem carries a wide range of convenient ready-to-use Insolution Inhibitors? Ready-to-use, InSolution Protein Kinase Inhibitors Name Cat. No. Comments Size Price InSolution AMPK Inhibitor, Compound C 7 26 Supplied as a 0 mM ( mg/250 ml) solution of AMPK Inhibitor, Compound C (Cat. No. 7 260) in DMSO. Purity: ≥95% by HPLC. M.W. 399.5 InSolution Casein Kinase I Inhibitor, D4476 2 8705 Supplied as a 0 mM ( mg/25 ml) solution of Casein Kinase I Inhibitor, D4476 (Cat. No. 2 8696) in DMSO. Purity: ≥95% by HPLC. M.W. 398.4 InSolution Casein Kinase II Inhibitor, DMAT 2 8706 Supplied as a 0 mM (5 mg/ .05 ml) solution of Casein Kinase II Inhibitor, DMAT (Cat. No. 2 8699), in DMSO. Purity: ≥95% by HPLC. M.W. 476.8 InSolution GSK-3b Inhibitor VIII 36 557 Supplied as a 25 mM (5 mg/649 ml) solution of GSK-3b Inhibitor VIII (Cat. No. 36 549) in DMSO. Purity: ≥95% by HPLC. M.W. 308.3 InSolution JAK Inhibitor I 420097 Supplied as a 0 mM (500 mg/ 62 ml) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO. Purity: ≥98% by HPLC. M.W. 309.3 InSolution p38 MAP Kinase Inhibitor III 506 48 Supplied as a 0 mM ( mg/247 ml) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506 2 ) in DMSO. Purity: ≥98% by HPLC. M.W. 404.5 InSolution PD 58780 5 3036 Supplied as a 0 mM (500 mg/ 5 ml) solution of PD 58780 (Cat. No. 5 3035) in DMSO. Purity: ≥95% by HPLC. M.W. 330.2 InSolution Rapamycin 5532 Supplied as a 5 mM (500 mg/ 09 ml) solution of Rapamycin (Cat. No. 5532 0) in DMSO. Purity: ≥98% by TLC. M.W.9 4.2 InSolution Rho Kinase Inhibitor 555552 Supplied as a 0 mM (500 mg/ 28 ml) solution of Rho Kinase Inhibitor (Cat. No. 555550) in H 2 O. Purity: ≥95% by HPLC. M.W. 392.3 InSolution VEGF Receptor 2 Kinase Inhibitor III 676498 Supplied as a 0 mM (500 mg/2 0 ml) solution of VEGF Receptor 2 Kinase Inhibitor III (Cat. No. 676487) in DMSO. Purity: ≥95% by HPLC. M.W. 238.3 More online... www.calbiochem.com/insolution mg $72 mg $ 2 5 mg $90 5 mg $84 500 mg $83 mg $ 2 500 mg $ 07 500 mg $95 500 mg $90 500 mg $73 84 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
Lipid Signaling Acetyl-CoA Carboxylase (ACC) Inhibitors Cyclooxygenases (COX) are bifunctional hemoproteins that catalyze both the bisoxygenation of arachidonic acid to form PGG 2 and the peroxidative reduction of PGG 2 to form PGH 2 . Hence, COX has two different active sites. On one side, it has the cyclooxygenase active site, and on the opposite side is an entirely separate peroxidase site, which is required to activate the heme groups that participate in the cyclooxygenase reaction. The enzyme complex is a dimer of identical subunits, two cyclooxygenase active sites and two peroxidase active sites. COX-1 is a constitutive enzyme associated with the endoplasmic reticulum. It is responsible for maintaining normal physiologic function and is considered as a “housekeeping” enzyme. COX-2 is an inducible enzyme mainly associated with the nuclear envelope and is primarily associated with inflammation. Several cytokines and growth factors increase the expression of COX-2, mainly at inflammatory sites, producing prostaglandins, which mediate inflammation, pain, and fever. Increased expression of COX-2 has been associated with increased incidence of colon and breast cancers. Inflammatory Non-steroidal anti-inflammatory Signaling drugs (NSAIDs) exert antiinflammatory and analgesic effects through the inhibition of prostaglandin synthesis by blocking COX activity. Traditional NSAIDs inhibit prostaglandin formation through the inhibition of both COX-1 and COX-2. Inhibition of COX-1 is not necessary for anti- Calbiochem • Inhibitor SourceBook Lipid Signaling Product Cat. No. Comments Size Price CoEnzyme A, Trilithium Salt 234101 A reversible inhibitor of acetyl-CoA (IC 50 = 40 nM). 00 mg $ 27 TOFA 613450 5-(Tetradecyloxy)-2-furoic acid A cell-permeable furoic acid compound that acts as a potent, reversible, and competitive inhibitor of acetyl-CoA carboxylase (ACC), a key enzyme involved in the fatty acid biosynthesis. Inhibits cellular fatty acid synthesis in a dosedependent manner (IC 50 = 4 mM in human breast cancer cell line MCF7). TOFAinduced reduction in malonyl-CoA is reported to offset the effect of C75 (Cat. No. 34 325) on food intake in fasted mice and on apoptosis in tumor cells. Cyclooxygenase (COX) Inhibitors inflammatory and analgesic effects but is thought to account for much of the toxicity of traditional NSAIDs. Based on structural differences in the active sites of these two isozymes, several new drugs have been developed that specifically inhibit only COX-2 activity. COX-2 selective inhibitors have the potential to provide the traditional benefits of NSAID with significantly reduced incidence of endoscopic ulcers. The selective COX-2 inhibitors have great clinical significance because they can allow the preservation of COX-1 activity, which is essential in maintaining prostaglandins that are important for normal platelet function and protection of the gastrointestinal mucosa, and still inhibit COX-2 to reduce inflammation and other pathologic processes. Due to the consideration of “inflammation as a factor” there has been an upsurge of interest in COX-2 inhibitors as possible candidates for the treatment of Alzheimer's disease. NSAIDs are believed to inhibit human Ab aggregation in vitro and reverse the b-sheet conformation of preformed (continued…) PLA2 Activation COX COX PGG 2 Arachidonic Acid Prostaglandins Thromboxane Inflammation Pain Fever Hypertension 5 mg $2 0 Platelet Aggregation Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 85
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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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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
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: Topoisomerase Related Inhibitors, c
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 •
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
Page 131 and 132: Protease Inhibitors, continued Calb
Page 133 and 134: Protease Inhibitors, continued Sele
Page 135 and 136: 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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