Inhibitor SourceBook™ Second Edition

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Proteases Matrix Metalloproteinase Inhibitors, continued Product Cat. No. Comments Size Price MMP-9 Inhibitor I 444278 A potent and selective inhibitor of MMP-9 (IC 50 = 5 nM). Inhibits MMP- (IC 50 = .05 mM) and MMP- 3 (IC 50 = 3 nM) only at much higher concentrations MMP-9/MMP- 3 Inhibitor I 444252 [N-Hydroxy-1-(4-methoxyphenyl)sulfonyl-4-(4-biphenylcarbonyl)piperaz ine-2-carboxamide] A highly-potent, piperazine-based inhibitor of MMP-9 and MMP- 3 (IC 50 = 900 pM). Inhibits MMP- and MMP-3 at much higher concentrations (IC 50 = 43 nM and 23 nM, respectively). Also acts as an inhibitor of MMP-7 (IC 50 = 930 nM). MMP-9/MMP- 3 Inhibitor II 444253 [N-Hydroxy-1-(4-methoxyphenyl)sulfonyl-4-benzyloxycarbonylpiperazine- 2-carboxamide] A highly-potent, piperazine-based potent inhibitor of MMP-9 (IC 50 = .9 nM) and MMP- 3 (IC 50 = .3 nM). Inhibits MMP- and MMP-3 at higher concentrations (IC 50 = 24 nM and 8 nM, respectively). Also acts as a weak inhibitor of MMP-7 (IC 50 = 230 nM). N MMP- 3 Inhibitor 444283 [Pyrimidine-4,6-dicarboxylic acid, bis-(4-fluoro-3-methyl-benzylamide)] A pyrimidine dicarboxamide compound that potently inhibits MMP- 3 activity (IC 50 = 8 nM) with expected selectivity over MMP- , -2, -3, -7, -8, -9, - 0, - 2, - 4, and - 6 as determined by conformational structure analysis. Shown to bind to the MMP- 3 catalytic domain and act as a non-zinc-chelating inhibitor. DL-Thiorphan 598510 {N-[(RS)-2-Benzyl-3-mercaptopropanoyl]-glycine} A thiol containing amido-acid that selectively binds to the active site zinc of metalloproteinases and blocks their activity (IC 50 = 2. nM for neutral endopeptidase-NEP). Although it is shown to inhibit the activity for Ab peptide degrading enzyme neprilysin in vitro, it has no effect on the secretion of Ab peptide or amyloid b precursor protein (APP). Also inhibits the activity of angiotensin-converting enzyme (ACE) at much higher concentrations (IC 50 = 4 mM); however, it does not affect the activity of endothelin-converting enzyme. XG076 682300 7-Aza-2-phenylbenzisothizol-3-one An isothiazolone derivative that inhibits the activation of pro-MMPs but does not affect the activity of active MMPs. Related Products MMP-1 ELISA Kit The MMP- ELISA is a non-isotopic colorimetric assay kit for the in vitro quantification of human MMP- protein in tissue culture medium and serum. Not available for sale in Japan. Cat. No. QIA55 1 kit $412 MMP-2 ELISA Kit A non-isotopic colorimetric assay for the in vitro assay of human MMP-2 protein in tissue culture media, serum, or plasma. Not available for sale in Japan. Cat. No. QIA63 1 kit $412 MMP-9 ELISA Kit A sandwich ELISA based kit designed specifically for assay of MMP-9 in human cell lines in suspension or adherent cells. Not available for sale in Japan. Cat. No. QIA56 1 kit $424 MMP-3 ELISA Kit 500 mg $96 mg $87 mg $ 02 mg $93 0 mg $ 95 5 mg $ 27 A sandwich ELISA based kit that can be used to assay of MMP-3 in cells in suspension and in adherent cells. Not available for sale in Japan. Cat. No. QIA73 1 kit $412 MMP-13 ELISA Kit A highly sensitive and specific kit for detection of active MMP- 3 from human samples, including serum, synovial fluid, and cell culture supernatant. Does not recognize MMP- , MMP-2, MMP-3, MMP-8, MMP-9, or the latent form of MMP- 3. Cat. No. QIA130 1 kit $525 InnoZyme Gelatinase Activity Assay Kit, Fluorogenic A sensitive fluorogenic assay (Ex. max: ~325 nm; Em. max.: ~393 nm) for the measurement of gelatinases (MMP-2 and MMP-9). Also useful for the screening of gelatinase inhibitors. Cat. No. CBA003 1 kit $375 22 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
Tissue Inhibitors of Matrix Metalloproteinases (TIMPs) Tissue inhibitors of metalloproteinases (TIMPs) are a family of ubiquitous, endogenous inhibitors that regulate the activation and activity of matrix metalloproteinases (MMPs). They have been shown in animal models to be capable of the inhibition of tumor cell invasion and metastasis. They may also be involved in other diseases such as arthritis and periodontal disease. TIMP-1 is a 184 amino acid glycoprotein of 28.5 kDa. TIMP-1 preferentially binds and inhibits MMP-9 and MMP- 1 through interaction with their catalytic domains. TIMP-2 is a 194 amino acid, non-glycosylated protein of 21 kDa with 43% and 44% homology to TIMP-1 and TIMP-3, respectively. It inhibits the activity of all active MMPs and regulates MMP-2 expression by binding to the C-terminal region of pro-MMP-2 (K d ~5 nM). As with TIMP-1, TIMP-2 has been shown to have erythroidpotentiating activity and cell growth-promoting Tissue Inhibitors of Matrix Metalloproteinases Calbiochem • Inhibitor SourceBook Proteases activity. TIMP-3 is present in the eye. It is tightly bound to the extracellular matrix and has been shown to inhibit TNF-a converting enzyme (TACE). A mutation in TIMP-3 is found in Sorsby's fundus dystrophy, a dominantly-inherited form of blindness. TIMP-4 blocks the activities of several (MMPs) implicated in the arthritic cartilage erosion. References: Visse, R., and Nagase, H. 2003. Cir. Res. 92, 827. Cheung, P.Y., et al. 200 . Proc. West Pharmacol. Soc. 44, 97. Mannello, F., and Gazzanelli, G. 200 . Apoptosis 6, 479. Herbst, H., et al. 997. Am. J. Pathol. 150, 647. Jung, K., et al. 997. Int. J. Cancer 74, 220. Rivera, S., et al. 997. J. Neurosci. 17, 4223. Vallon, R., et al. 997. Eur. J. Biochem. 244, 8 . Cottam, D.W., et al. 993. Intl. J. Oncol. 2, 86 . Stetler-Stevenson, W.G. et al. 993. FASEB J. 7, 434. Product Cat. No. Comments Size Price TIMP- , Recombinant, Bovine PF020 (Tissue Inhibitor of Metalloproteinase-1) A CHO cell-derived protein. Shown to inhibit MMP- (IC 50 = –5 nM). Not available for sale in Japan. TIMP- , Human Neutrophil Granulocyte 612080 (Tissue Inhibitor of Metalloproteinase-1) A 28 kDa glycoprotein that forms a non-covalent stochiometric complex with latent and active MMPs. Binds to pro-MMP-9 and MMP-9 via their C-terminal domains. TIMP- , Recombinant, Human PF019 (Tissue Inhibitor of Metalloproteinase-1) A 28 kDa glycoprotein that is expressed by a variety of cell types. It forms a non-covalent, stoichiometric complex with both latent and active MMPs. TIMP- preferentially binds and inhibits MMP-9. Not available for sale in Japan. TIMP-2, Human Rheumatoid Synovial Fibroblast More online... www.calbiochem.com/inhibitors/TIMPs 612084 (Tissue Inhibitor of Metalloproteinase-2) Forms a non-covalent stoichiometric complex with latent and active MMPs. Shown to inhibit the activities of MMP- , MMP-2, MMP- 2, and transin. TIMP-2, Human, Recombinant PF021 (Tissue Inhibitor of Metalloproteinase 2) A 2 kDa (nonreduced) or a 24 kDa (reduced) protein expressed by a variety of cell types. Forms a non-covalent, stoichiometric complex with both latent and active MMPs. TIMP-2 preferentially binds and inhibits MMP-2. Not available for sale in Japan. TIMP-2, Mouse, Recombinant PF098 (Tissue Inhibitor of Metalloproteinase-2) A 94 amino acid non-glycosylated protein with 43% and 44% homology to TIMP- and TIMP-3, respectively. Inhibits the activity of all MMPs and regulates MMP-2 expression by binding to the C-terminal region of pro-MMP-2. TIMP-2 is constitutively produced by most cell types in culture, along with MMP-2. TIMP-3, Human, Recombinant PF095 (Tissue Inhibitor of metalloproteinase-3) Constitutively produced by many cell types. Differs from the other TIMPs in its localization to the extracellular matrix. TIMP-3 is more basic than the other TIMPs, and the basic residues are thought to help anchor TIMP-3 into the ECM. 3 mg $ 53 5 mg $225 3 mg $ 53 5 mg $225 3 mg $ 53 5 mg $276 5 mg $276 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 23
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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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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
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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
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
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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 121 and 122: Matrix Metalloproteinase (MMP) Inhi
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Page 141 and 142: Transmembrane receptors of various
Page 143 and 144: Angiotensin-Converting Enzyme (ACE)
Page 145 and 146: ATPase Inhibitors, continued Calbio
Page 149 and 150: Inhibitors of Glycoprotein Processi
Page 151 and 152: Heat Shock Protein Inhibitors Heat
Page 153 and 154: Inhibitors of Mitochondrial Functio
Page 155 and 156: NF-kB Activation Inhibitors NF-kB,
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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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Trademarks CALBIOCHEM®
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Your #1 Resource for Inhibitors! We
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