Inhibitor SourceBook™ Second Edition

More documents

Recommendations

Info

Lipid Signaling Lipoxygenase (LOX) Inhibitors, continued Product Cat. No. Comments Size Price Eicosapentaenoic Acid 324875 (C20:5 w-3; 5,8,11,14,17-Eicosapentaenoic Acid; EPA) A fatty acid isolated from microscopic algae that acts as an antihyperlipoproteinenic agent. Inhibits 5-LOX and reduces thromboxane A2 production. ETYA 434741 (5,8,11,14-Eicosatetraynoic Acid) A cell-permeable inhibitor of COX (ID 50 = 8 mM), 5-LOX (ID 50 = 0 mM), 2-LOX (ID 50 = 300 nM), and 5-LOX (ID 50 = 200 nM) in whole cells. Also acts as a modulator of Ca 2+ entry into cells. Hinokitiol 377230 (4-Isopropyltropolone; b-Thujaplicin) A cell-permeable metal ion chelator that also acts as a reversible inhibitor of 2-LOX in platelets (IC 50 = 00 nM). Ketoconazole 420600 {cis-1-Acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3dioxolan-4-yl]methoxy]phenyl]piperazine; R-41400} An antifungal agent that acts as an inhibitor of 5-LOX (IC = 26 mM) and 50 thromboxane synthase. MK-886 475889 {3-[1-(p-Chlorobenzyl)-5-(isopropyl)-3-t-butylthioindol-2-yl]-2,2dimethylpropanoic Acid, Na} A cell-permeable, potent and specific inhibitor of leukotriene biosynthesis (IC = 02 nM). Prevents the activation of 5-LOX by binding to 5-LOX-activating 50 protein (FLAP); however, it does not affect 5-LOX activity in cell-free systems. NDGA, Larrea divaricata 479975 (Nordihydroguaiaretic Acid) An antioxidant and a selective LOX inhibitor (IC = 200 nM, 30 mM, and 30 mM 50 for 5-LOX, 2-LOX, and 5-LOX, respectively) over COX (IC = 00 mM). 50 Ro 06-9920 557550 A cell-permeable, irreversible inhibitor of IkBaee ubiquitination (IC = 2.3 mM) 50 that also inhibits the activity of 5-lipoxygenase (89% at 0 mM). SKF-86002 567305 {6-(4-Fluorophenyl)-2,3-dihydro-5-(4-pyridyl)imidazo[2,1-b]thiazole} A cytokine-suppressive anti-inflammatory drug that also acts as an inhibitor of both COX and 5-LOX. 25 mg $83 20 mg $203 50 mg $43 50 mg $75 5 mg $90 250 mg $46 92 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem mg 5 mg $72 $25 5 mg $ 23
Phospholipase Inhibitors Several signal transduction processes in cells utilize lipid-derived second messengers. These molecules are generated by the action of phospholipases on cellular lipids. Phospholipase A 2 (PLA 2 ) hydrolyzes the acyl group from the sn-2 position of glycerophospholipids. Two major types of PLA 2 are found in cells: the cytosolic form (cPLA 2 ) and the secretory form (sPLA 2 ). cPLA 2 , an 85 kDa enzyme, preferentially hydrolyzes phospholipids containing arachidonate at the sn-2 position and provides free arachidonic acid for the synthesis of eicosanoids. cPLA 2 is found in a variety of cells where it acts as a receptor-regulated enzyme that can mediate agonist-induced arachidonic acid release. It is activated by low levels of Ca 2+ . sPLA 2 , following its release from cells, plays an important role in inflammation and in antimicrobial defense. However, excessive activity of sPLA 2 has been shown to result in tissue damage and is linked to organ failure associated with critical illness. Phospholipase Inhibitors Calbiochem • Inhibitor SourceBook Lipid Signaling PLA 2 inhibitors are considered as desirable candidates for control and management of diseases related to eicosanoid production, such as allergy, inflammation, thrombosis, airway secretion, and cell proliferation. Phospholipase C (PLC) is another important member of the family that controls the production of inositol- 1,4,5- trisphosphate (IP 3 ). IP 3 is involved in cytosolic Ca 2+ release and diacylglycerol (DAG) production, both of which activate protein kinase C. Phospholipase D (PLD) catalyzes the hydrolysis of phosphatidylcholine to form phosphatidic acid (PA) and released choline headgroup. The PA can itself act as a signal molecule by activating a PA-activated kinase, or can be hydrolyzed to form DAG by the action of PA phosphohydrolase. Product Cat. No. Comments Size Price AACOCF 3 100109 (Arachidonyltrifluoromethyl Ketone) A cell-permeable trifluoromethyl ketone analog of arachidonic acid. Potent and selective slow-binding inhibitor of human cytosolic (85 kDa) PLA 2 . Causes a significant reduction in thromboxane B 2 production in thrombin-stimulated platelets. ACA 104550 [N-(p-Amylcinnamoyl)anthranilic Acid] Inhibits epinephrine-stimulated thromboxane production (86% at 3.5 mM) via inhibition of PLA 2 in human platelets. Possesses moderate leukotriene antagonist activity. Aristolochic Acid 182300 A : mixture of aristolochic acids I and II. Inhibits PLA 2 from various snake venoms as well as human platelet and synovial fluid PLA 2 . Also inhibits ionophore-stimulated PLA 2 activity (IC 50 = 40 mM) and Ca 2+ -dependent arachidonic acid released in human neutrophils. Exhibits greater inhibitory activity towards group II PLA 2 versus group I PLA 2 . D609, Potassium Salt 251400 (Tricyclodecan-9-yl-xanthogenate, K) Selective inhibitor of phosphatidylcholine-specific phospholipase C (Bacillus cereus, K i = 5– 0 mM). Does not inhibit (up to 50 mM) phosphatidylinositolspecific phospholipase C, PLA 2 , and PLD. Also inhibits the activity of sphingomyelinase. D609 Prodrug 251401 (S-Methyleneoxybutyryl D609) A cell-permeable prodrug form of D609 (Cat. No. 25 400) that displays reduced cytotoxicity towards normal cells, but enhanced potency in inducing apoptosis in tumor cells (LD 50 = 56.6 mM for U937 cells). ET- 8-OCH 3 341207 (Edelfosine; 1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphorylcholine) A selective inhibitor of phosphatidylinositol-specific PLC (IC 50 = 5 mM) but has no significant effect on phosphatidylcholine-specific PLC or PLD. Isotetrandrine 419650 A biscoclaurine alkaloid that inhibits G-protein activation of phospholipase A 2 but not phospholipase C or phospholipase D. Methyl Arachidonyl Fluorophosphonate More online... www.calbiochem.com/inhibitors/plipase 454565 (MAFP) A selective, active site-directed, irreversible inhibitor of both calcium-dependent and calcium-independent cytosolic (85 kDa) PLA 2 , but not secretory PLA 2 . 0 mg $87 25 mg $84 50 mg $50 5 mg $ 07 5 mg $ 63 5 mg $80 mg $77 mg $77 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 93
Page 1 and 2:
Inhibitor SourceBook Second Editio
Page 3 and 4:
Calbiochem • Inhibitor SourceBook
Page 5 and 6:
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 17 and 18:
Page 19 and 20:
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 35 and 36:
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 43 and 44: Calbiochem • Inhibitor SourceBook
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: Lipoxygenase (LOX) Inhibitors Lipox
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
Page 137 and 138: N Animal-Free Protease Inhibitor Co
Page 139 and 140: Proteasome and Ubiquitination Pathw
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 147 and 148:
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,
Page 157 and 158:
NF-kB Activation Inhibitors, contin
Page 159 and 160:
Phosphodiesterase (PDE) Inhibitors
Page 161 and 162:
Plasminogen Activator Inhibitors Ti
Page 163 and 164:
Protein Synthesis Inhibitors, conti
Page 165 and 166:
Sonic Hedgehog Signaling Inhibitors
Page 167 and 168:
Why can’t I make serial dilutions
Page 169 and 170:
Calpastatin, Human, Recombinant, Do
Page 171 and 172:
InSolution Microcystin-LR, Microcys
Page 173 and 174:
RNA Polymerase III Inhibitor ......
Page 175 and 176:
324875 ............................
Page 177 and 178:
Trademarks CALBIOCHEM®
Page 179 and 180:
Your #1 Resource for Inhibitors! We
show all

Inhibitor SourceBook™ Second Edition

Create successful ePaper yourself

Delete template?

Save as template?