Inhibitor SourceBook™ Second Edition

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Phosphorylation/Dephosphorylation Protein Kinase C (PKC) Inhibitors, continued Product Cat. No. Comments Size Price Chelerythrine Chloride 220285 Naturally occurring alkaloid. Cell-permeable, selective inhibitor of PKC (IC 50 = 660 nM). Acts on the catalytic domain irrespective of the attachment of the regulatory domain. A competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, Dihydrochloride (Cat. No. 37 955). Dequalinium Chloride 263225 (DECA) An antitumor agent and PKC inhibitor. When exposed to UV light, DECA covalently and irreversibly inhibits PKC a or PKC b (IC 50 = 7- 8 mM). Ellagic Acid, Dihydrate 324683 (4,4´,5,5´,6,6´-Hexahydroxydiphenic Acid 2,6,2´,6´-Dilactone) A potent antioxidant with anti-mutagenic and anti-carcinogenic properties. Inhibits DNA topoisomerases I and II (IC 50 = .8 mM and 2. mM, respectively). Acts as a potent inhibitor of PKA catalytic subunit and PKC (IC 50 = 2 mM and 8 mM respectively). Gö 6976 365250 [12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a) pyrrolo (3,4-c)-carbazole; Go 6976] An inhibitor of PKC (IC 50 = 7.9 nM for rat brain). Selectively inhibits Ca 2+ -dependent PKC a-isozyme (IC 50 = 2.3 nM) and PKC bI (IC 50 = 6.2 nM). Does not affect the kinase activity of the Ca 2+ -independent PKC d , PKC e , and PKC z isoenzymes even at micromolar levels. InSolution Gö 6976 365253 [12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a) pyrrolo (3,4-c)-carbazole; Go 6976, Solution] A 500 mg/ml solution of Gö 6976 (Cat. No. 365250) in anhydrous DMSO. Gö 6983 365251 {2-[1-(3-Dimethylaminopropyl)-5-methoxyindol-3-yl]-3-(1H-indol-3-yl) maleimide; Go 6983} A potent inhibitor of PKC that has been shown to selectively inhibit several PKC isozymes (IC 50 = 7 nM for PKC a and PKC b ; 6 nM for PKC g ; 0 nM for PKC d ; 60 nM for PKC z ). Gö 6983 does not effectively inhibit PKC m (IC 50 = 20 mM) and can thus be used to differentiate PKC m from other PKC isozymes. Gö 7874, Hydrochloride 365252 A potent and selective inhibitor of rat brain PKC (IC 50 = 4 nM) versus MLCK (IC 50 = 20 nM), PKA (IC 50 = 50 nM), and PKG (IC 50 = 4.8 mM). H-7, Dihydrochloride 371955 [1-(5-Isoquinolinesulfonyl)-2-methylpiperazine, 2HCl] A broad based serine-threonine kinase inhibitor. Potent inhibitor of MLCK (K i = 97 mM), PKA (K i = 3 mM), PKC (K i = 6 mM), and PKG (K i = 5.8 mM). Not available for sale in Japan. Iso-H-7, Dihydrochloride 371956 [1-(5-Isoquinolinesulfonyl)-3-methylpiperazine, 2HCl] Less potent than H-7 in inhibiting rat brain PKC isoforms (IC 50 = 50 mM). Also inhibits other cyclic-nucleotide-dependent protein kinases. HBDDE 372770 (2,2´,3,3´,4,4´-Hexahydroxy-1,1´-biphenyl-6,6´-dimethanol Dimethyl Ether) An inhibitor of PKC that selectively inhibits PKC a (IC 50 = 43 mM) and PKC g (IC 50 = 50 mM) over PKC d , PKC bI , and PKC bII isozymes. Hispidin 377980 [6-(3,4-Dihydroxystyrl)-4-hydroxy-2-pyrone] A potent inhibitor of PKC b isoform (IC 50 = 2 mM). Hypericin 400076 A polycyclic dione that inhibits PKC (IC 50 = 3.3 mM). Also known to inhibit the protein tyrosine kinase activities of the insulin receptor (IC 50 = 20 - 29 nM), EGFR (IC 50 = 35 nM), casein kinase II (IC 50 = 6 nM), and MAP kinase (IC 50 = 4 nM). Useful probe for PKC due to its bright red fluorescence emission and photostability. K-252a, Nocardiopsis sp. InSolution K-252a, Nocardiopsis sp. K-252b, Nocardiopsis sp. 420298 A cell-permeable protein kinase inhibitor that inhibits CaM kinase II (K i = .8 nM), MLCK (K i = 7 nM), PKA (K i = 8 nM), PKC (K i = 25 nM), and PKG (K i = 20 nM). 5 mg $97 500 mg $57 500 mg $57 500 mg $ 22 ml $ 36 500 mg $89 500 mg $ 00 38 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem mg 5 mg $84 $327 mg $87 mg $ 38 2 mg $ 44 mg $ 05 00 mg $ 33 420297 A mM ( 00 mg/2 4 ml) solution of K-252a (Cat. No. 420298) in anhydrous DMSO. 00 mg $ 28 420319 A non-selective inhibitor of MLCK (K i = 47 nM), PKA (K i = 90 nM), PKC (K i = 20 nM), and PKG (K i = 00 nM). K-252c 420305 Inhibits PKA (IC 50 = 25.7 mM) and PKC (IC 50 = 2.45 mM). mg $ 50 Melittin 444605 A 26-residue polypeptide from bee venom that binds calmodulin in a Ca 2+ -dependent manner. Activates phospholipase A 2 and inhibits protein kinase C (IC 50 = 5-7 mM) by binding to the catalytic domain in a Mg 2+ -ATP sensitive manner. Has also been used for affinity purification of several Ca 2+ -binding proteins. A stimulator of G i a and G a activity that is reported to inhibit adenylate cyclase activity in synaptic membranes. 50 mg 00 mg $76 $ 33 250 mg $67
Protein Kinase C (PKC) Inhibitors, continued Calbiochem • Inhibitor SourceBook Phosphorylation/Dephosphorylation Product Cat. No. Comments Size Price NGIC-I 481500 (Non-glycosidic Indolocarbazole I) A potent and selective inhibitor of PKC (IC 50 = 75 nM) versus PKA (IC 50 > 0 mM) and PKG (IC 50 = 320 nM). Phloretin 524488 (2´,4´,6´-Trihydroxy-3-p-hydroxyphenylpropiophenone) A flavonoid that prevents the activation of PKC. Piceatannol 527948 (trans-3,3´,4,5´-Tetrahydroxystilbene) A plant metabolite that preferentially inhibits the activity of p72 Syk (IC 50 ~ 0 mM). Also acts as an inhibitor of the rat liver PKA catalytic subunit (cAK) (IC 50 = 3 mM), PKC (IC 50 = 8 mM), MLCK (IC 50 = 2 mM), and wheat embryo Ca 2+ -dependent protein kinase (CDPK) (IC 50 = 9 mM). N PKC b Inhibitor 539654 [3-(1-(3-Imidazol-1-ylpropyl)-1H-indol-3-yl)-4-anilino-1H-pyrrole-2,5-dione] A potent, ATP-competitive inhibitor of PKC b isozymes (IC 50 = 5 nM and 2 nM for human PKC bII and bI ). Displays greater selectivity over PKC a , PKC g , and PKC e (IC 50 = 33 nM, > mM, and 2.8 mM, respectively). N PKC bII /EGFR Inhibitor 539652 A cell-permeable symmetrical phthalimide compound that acts as a potent and ATPcompetitive inhibitor of EGFR and PKC isozymes a, bI, and bII (IC 50 = 0.7, .9, 3.8, and 0.4 mM, respectively), while exhibiting little or much weaker activity towards a panel of 6 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulinstimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro, and exhibit antitumor activity in mice in vivo. Polymyxin B Sulfate 5291 (Aerosporin) An antibiotic that inhibits phospholipid sensitive Ca 2+ -dependent protein kinase. Mixture of polymyxin B sulfate and polymyxin B 2 sulfate. Protein Kinase C Inhibitor 20-28, Cell-Permeable, Myristoylated Protein Kinase C Inhibitor, EGF-R Fragment 65 -658, Myristoylated Protein Kinase C Inhibitor Peptide 9-3 Protein Kinase C Inhibitor Peptide 9-36 Protein Kinase C h Pseudosubstrate Inhibitor, Myristoylated Protein Kinase C z Pseudosubstrate Inhibitor Protein Kinase C z Pseudosubstrate Inhibitor, Myristoylated Protein Kinase C θ Pseudosubstrate Inhibitor Protein Kinase C θ Pseudosubstrate Inhibitor, Myristoylated 476480 (Myr-N-FARKGALRQ-NH 2 ; Myristoylated Protein Kinase C Inhibitor 20-28, Cell-Permeable) Pseudosubstrate sequence from PKC a and PKC b . N-terminal myristoylated to allow membrane permeability. Highly specific inhibitor of TPA activation of MARCKS phosphorylation in fibroblast primary cultures (IC 50 = 8 mM). Exhibits 98% inhibition at 00 mM. 476475 [Myr-N-RKRTLRRL-OH; Myristoylated EGF-R Fragment (651-658), PKC Inhibitor] Epidermal growth-factor receptor (EGF-R) conserved sequence that is identical to verbB (95- 02). An N-terminal myristoylated membrane-permeable inhibitor that inhibits PKC (IC 50 = 5 mM) in intact cells. 05-23- 4904 (PKC 19-31; RFARKGALRQKNV) More potent inhibitor of PKC (IC = 00 nM) than Protein Kinase C Inhibitor Peptide 50 9-36 (Cat. No. 539560). 539560 (PKC 19-36; RFARKGALRQKNVHEVKN) Acts as a pseudo substrate by binding to the active sites of protein kinases. Potent inhibitor of PKC (K i = 47 nM) but not of PKA (IC 50 = 423 mM). 539604 (Myr-TRKRQRAMRRRVHQING-NH 2 ) A cell-permeable myristoylated PKC h pseudosubstrate inhibitor of protein kinase C h isozyme. Useful for studies of PKC h function in intact cells. 539610 (SIYRRGARRWRKL) A non-cell-permeable PKC z pseudosubstrate sequence peptide that can be used as a competitive inhibitor PKC z in in vitro kinase assays. 539624 (Myr-SIYRRGARRWRKL-OH) A cell-permeable myristoylated form of PKC z pseudosubstrate peptide (Cat. No. 5396 0) that includes amino acids 3– 25 of the pseudosubstrate region. Useful for inhibition studies of PKC z in intact cells. 539634 (LHQRRGAIKQAKVHHVKC-NH 2 ) A selective and competitive inhibitor of protein kinase C θ isozyme that includes amino acids 3– 25 of the pseudosubstrate sequence. 539636 (Myr-LHQRRGAIKQAKVHHVKC-NH 2 ) A cell-permeable myristoylated PKC θ pseudosubstrate sequence peptide (Cat. No. 539634). Useful for studies of PKC θ function in intact cells. 500 mg $ 30 200 mg $8 mg $4 500 mg $ 26 2 mg $ 3 500 mg g 5 g $3 $50 $208 500 mg $ 03 500 mg $ 04 mg 5 mg 500 mg mg $98 $372 $ 33 $238 500 mg $ 64 500 mg $ 7 500 mg $ 45 500 mg $ 23 500 mg $ 69 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 39
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: Isozyme Specificities of Selected P
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
Page 93 and 94:
Lipoxygenase (LOX) Inhibitors Lipox
Page 95 and 96:
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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