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PLA2 Inhibitors
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ALX-340-001 Revised 28-Jul-06
Arachidonyl trifluoromethylketone
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SYNONYMS AACOCF3
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PLA2 Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-001-M005   5 mg 70.00 USD Add To Cart
ALX-340-001-M010   10 mg 110.00 USD Add To Cart
ALX-340-001-M050   50 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C21H31F3O
MW: 356.5
CAS NUMBER: 149301-79-1
PURITY: ≥98%
APPEARANCE: Clear to yellow oil.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Dissolve in solvent purged with nitrogen or argon. Store under nitrogen or argon in tightly sealed container. Solutions are stable for up to 1 month when stored under nitrogen or argon in tightly sealed container at -80°C.
HANDLING: PROTECT FROM AIR!
HAZARD: TOXIC.

Product Description
Selective inhibitor of both, Ca2+-dependent and Ca2+-independent phospholipase A2 (PLA2), but not secretory PLA2 (sPLA2). Also inhibits fatty acid amide hydrolase (FAAH) and anandamide amidase.
Product Specific Literature References
Inhibitors of arachidonoyl ethanolamide hydrolysis: B. Koutek, et al.; J. Biol. Chem. 269, 22937 (1994) Abstract; Full Text
Further Categories Containing This Product:
Fatty Acid Amide Hydrolase [FAAH] / Related Products
 
 
ALX-270-047 Revised 26-Sep-07
Aristolochic acid
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SYNONYMS 8-Methoxy-6-nitrophenanthrol(3,4-d)-1,3-dioxide-5-carboxylic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-047-M025   25 mg 25.00 USD Add To Cart
ALX-270-047-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C17H11NO7
MW: 341.3
CAS NUMBER: 313-67-7
MERCK INDEX: 14: 786
RTECS: CF3325000
SOURCE/HOST: Isolated from Aristolochia clematis.
PURITY: ≥97% (~1:1 mixture of aristolochic acids I (A) and II (B))
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: MAY BE CARCINOGENIC. TOXIC. MAY BE MUTAGENIC.

Product Description
Phospholipase A2 (PLA2) inhibitor active against the enzymes found in many snake venoms as well as those of human platelets and synovial fluids. Inhibits ionophore-stimulated PLA2 activity in human neutrophils. Has been shown to be nephropathic and carcinogenic.
Product Specific Literature References
Characterization of three edema-inducing phospholipase A2 enzymes from habu (Trimeresurus flavoviridis) venom and their interaction with the alkaloid aristolochic acid: B.S. Vishwanath, et al.; Toxicon 25, 501 (1987) Abstract
Interaction of aristolochic acid with Vipera russelli phospholipase A2: its effect on enzymatic and pathological activities: B.S. Vishwanath & T.V. Gowda; Toxicon 25, 929 (1987) Abstract
Interaction of phospholipase A2 from Vipera russelli venom with aristolochic acid: a circular dichroism study: B.S. Vishwanath, et al.; Toxicon 25, 939 (1987) Abstract
Edema-inducing activity of phospholipase A2 purified from human synovial fluid and inhibition by aristolochic acid: B.S. Vishwanath, et al.; Inflammation 12, 549 (1988) Abstract
Effects of aristolochic acid on phospholipase A2 activity and arachidonate metabolism of human neutrophils: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1001, 3 (1989) Abstract
Suramin alters phosphoinositide synthesis and inhibits growth factor receptor binding in HT-29 cells: R. Kopp & A. Pfeiffer; Cancer Res. 50, 6490 (1990) Abstract
The effects of the phospholipase A2 inhibitors aristolochic acid and PGBx on A23187-stimulated mobilization of arachidonate in human neutrophils are overcome by diacylglycerol or phorbol ester: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1126, 319 (1992) Abstract
Evidence for different mechanisms involved in the formation of lyso platelet-activating factor and the calcium-dependent release of arachidonic acid from human neutrophils: J.D. Winkler, et al.; Biochem. Pharmacol. 44, 2055 (1992) Abstract
Selective inhibition of group II phospholipase A2 by quercetin: M. Lindahl & C. Tagesson; Inflammation 17, 573 (1993) Abstract
Detection of DNA adducts formed by aristolochic acid in renal tissue from patients with Chinese herbs nephropathy: H.H. Schmeiser, et al.; Cancer Res. 56, 2025 (1996) Abstract
Aristolochic acid and ’Chinese herbs nephropathy’: a review of the evidence to date: J.P. Cosyns; Drug Saf. 26, 33 (2003), Review Abstract
Effect of aristolochic acid on intracellular calcium concentration and its links with apoptosis in renal tubular cells: Y.H. Hsin, et al.; Apoptosis 11, 2167 (2006) Abstract
Further Categories Containing This Product:
PLA2 Inhibitors • Carcinogens & Tumor Promoters Other Products • Natural Products - Other Tumor Promoters • Other Toxins • Alkaloids
 
 
ALX-270-195 Revised 14-Jan-08
Bromoenol lactone
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SYNONYMS BEL
(E)-6-(Bromomethylene)tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PLA2 Inhibitors
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ALX-270-195-M005   5 mg 136.00 USD Add To Cart
Product Specification
FORMULA: C16H13BrO2
MW: 317.2
CAS NUMBER: 88070-98-8
PURITY: 98%
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, acetonitrile, DMSO or dimethyl formamide.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Before use, product should be dissolved in an organic solvent miscible with water. Further dilutions in aqueous buffers should be made just prior to performing experiment. Store aqueous solutions on ice and use within 12 hours. Although the aqueous solutions may be stable for more than 12 hours, we strongly recommend using a fresh preparation each day.
HAZARD: IRRITANT.

Product Description
Potent, irreversible inhibitor of Ca2+-independent phospholipase A2 (iPLA2). Also inhibits the macrophage PLA2 in a concentration-dependent manner. Effective enzyme-activated irreversible inhibitor of chymotrypsin.
Product Specific Literature References
Haloenol lactones. Potent enzyme-activated irreversible inhibitors for alpha-chymotrypsin: S.B. Daniels, et al.; J. Biol. Chem. 258, 15046 (1983) Abstract; Full Text
Suicide inhibition of canine myocardial cytosolic calcium-independent phospholipase A2. Mechanism-based discrimination between calcium- dependent and -independent phospholipases A2: S.L. Hazen, et al.; J. Biol. Chem. 266, 7227 (1991) Abstract; Full Text
Inhibition of macrophage Ca(2+)-independent phospholipase A2 by bromoenol lactone and trifluoromethyl ketones: E.J. Ackermann, et al.; J. Biol. Chem. 270, 445 (1995) Abstract; Full Text
Inhibition of calcium-independent phospholipase A2 prevents arachidonic acid incorporation and phospholipid remodeling in P388D1 macrophages: J. Balsinde, et al.; PNAS 92, 8527 (1995) Abstract
 
 
ALX-270-171 Revised 30-Jun-08
Chlorpromazine . hydrochloride
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SYNONYMS 2-Chloro-10-(3-dimethylaminopropyl)phenothiazine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-270-171-G001   1 g 22.00 USD Add To Cart
ALX-270-171-G005   5 g 66.00 USD Add To Cart
Product Specification
FORMULA: C17H19ClN2S . HCl
MW: 318.9 . 36.5
CAS NUMBER: 69-09-0
MERCK INDEX: 14: 2185
RTECS: SO1750000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Not stable in aqueous solution. We strongly recommend always to use freshly prepared solutions.
HANDLING: Protect from light.
HAZARD: VERY TOXIC.

Product Description
Inhibits calmodulin stimulation of cyclic nucleotide phosphodiesterase. Dopamine antagonist. D2 antagonist. H1 antagonist. Inhibits TNF-α production. Potent PLA2 inhibitor. Inhibits nitric oxide synthase (NOS) in mouse brain and prevents lipopolysaccharide induction of NOS in mouse lung. Antipsychotic.
Product Specific Literature References
Chlorpromazine as a substitute for ortho-dianisidine and ortho-tolidine in the determination of chlorine, hemoglobin, and peroxidase activity: H.B. Collier; Clin. Biochem. 7, 331 (1974) Abstract
Drug-protein interactions: binding of chlorpromazine to calmodulin, calmodulin fragments, and related calcium binding proteins: D.R. Marshak, et al.; Biochemistry 24, 144 (1985) Abstract
Selective inhibition of group II phospholipase A2 by quercetin: M. Lindahl & C. Tagesson; Inflammation 17, 573 (1993) Abstract
Chlorpromazine inhibits both the constitutive nitric oxide synthase and the induction of nitric oxide synthase after LPS challenge: M. Palacios, et al.; BBRC 196, 280 (1993) Abstract
Protective effect of calmodulin inhibitors against acute cyanide- induced lethality and convulsions in mice: H. Yamamoto; Toxicol. Lett. 66, 73 (1993) Abstract
Pharmacologic inhibitors of tumor necrosis factor production exert differential effects in lethal endotoxemia and in infection with live microorganisms in mice: M.G. Netea, et al.; J. Infect. Dis. 171, 393 (1995) Abstract
Pharmacological regulation of mitochondrial nitric oxide synthase: A. Boveris, et al.; Methods Enzymol. 359, 328 (2002) Abstract
Brain mitochondrial nitric oxide synthase: in vitro and in vivo inhibition by chlorpromazine: S. Lores-Arnaiz, et al.; Arch. Biochem. Biophys. 430, 170 (2004) Abstract
Further Categories Containing This Product:
Phosphodiesterases / Related Products • TNF-alpha & TNF Receptors Other Products • Chemopreventive Agents Other Products • NOS Inhibitors (NOS Induction & Enzyme Activity) • PLA2 Inhibitors • Dopaminergics & Dopamine Receptors / Related Products
 
 
ALX-340-008 Revised 22-May-07
7,7-Dimethyleicosadienoic acid
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SYNONYMS DEDA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PLA2 Inhibitors
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ALX-340-008-M010   10 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C22H40O2
MW: 336.6
CAS NUMBER: 89560-01-0
PURITY: ≥99%
APPEARANCE: Colorless oil.
SOLUBILITY: Soluble in 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions are stable for up to 6 months when stored at –20°C.

Product Description
Potent inhibitor of snake venom phospholipase A2 (PLA2) and weak inhibitor of 5-lipoxygenase. Inhibits human recombinant synovial phospholipase A2 (sPLA2) selectively over cytosolic phospholipase A2 (cPLA2).
Product Specific Literature References
Analogs of arachidonic acid methylated at C-7 and C-10 as inhibitors of leukotriene biosynthesis: N. Cohen, et al.; Prostaglandins 27, 553 (1984) Abstract
A.F. Welton, et al.; Prostaglandins 28, 649 (1984)
Inhibition studies on the membrane-associated phospholipase A2 in vitro and prostaglandin E2 production in vivo of the macrophage-like P388D1 cell. Effects of manoalide, 7,7-dimethyl-5,8-eicosadienoic acid, and p- bromophenacyl bromide: M.D. Lister, et al.; J. Biol. Chem. 264, 8520 (1989) Abstract; Full Text
Effect of the phospholipase A2 inhibitors quinacrine and 7,7- dimethyleicosadienoic acid in isolated globally ischemic rat hearts: C.A. Sargent, et al.; J. Pharmacol. Exp. Ther. 262, 1161 (1992) Abstract
Secretory phospholipase A2 inhibitors and calmodulin antagonists as inhibitors of cytosolic phospholipase A2: W.C. Hope, et al.; Agents Actions 39, C39 (1993) Abstract
Further Categories Containing This Product:
Lipoxygenases / Related Products
 
 
ALX-340-010 Revised 28-Feb-07
ETYA
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SYNONYMS 5,8,11,14-Eicosatetraynoic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Lipoxygenases / Related Products
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ALX-340-010-M005   5 mg 40.00 USD Add To Cart
ALX-340-010-M025   25 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C20H24O2
MW: 296.5
CAS NUMBER: 1191-85-1
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO, acetone or acetonitrile.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: We do not recommend storing the solutions for more than one day.
HANDLING: Protect from light and oxygen.
HAZARD: TOXIC.

Product Description
Inhibits arachidonic acid uptake. Inhibitor of lipoxygenases, cyclooxygenases (COX), phospholipase A2 and cytochrome P450. Modulates Ca2+ entry into cells. Stimulates luteinizing hormone release from cultured pituitary cells. PPAR agonist.
Product Specific Literature References
Structural requirements of acetylenic fatty acids for inhibition of soybean lipoxygenase and prostaglandin synthetase: D.T. Downing, et al.; Biochim. Biophys. Acta 280, 343 (1972) Abstract
The effect of 5,8,11,14-eicosatetraynoic acid on lipid metabolism: L.D. Tobias & J.G. Hamilton; Lipids 14, 181 (1979) Abstract
An inhibitor of arachidonic acid metabolism stimulates luteinizing hormone (LH) release from cultured pituitary cells: P.M. Conn, et al.; Prostaglandins 19, 873 (1980) Abstract
Evidence for inhibition of leukotriene A4 synthesis by 5,8,11,14-eicosatetraynoic acid in guinea pig polymorphonuclear leukocytes: G.M. Bokoch & P.W. Reed; J. Biol. Chem. 256, 4156 (1981) Abstract; Full Text
Phospholipase A2-induced rat mast cell secretion. Role of arachidonic acid metabolites: E.Y. Chi, et al.; Lab. Invest. 47, 579 (1982) Abstract
Epoxyeicosatrienoic acids stimulate glucagon and insulin release from isolated rat pancreatic islets: J.R. Falck, et al.; BBRC 114, 743 (1983) Abstract
The mechanism of inactivation of lipoxygenases by acetylenic fatty acids: H. Kühn, et al.; Eur. J. Biochem. 139, 577 (1984) Abstract
Comparative effects of indomethacin, acetylenic acids, 15-HETE, nordihydroguaiaretic acid and BW755C on the metabolism of arachidonic acid in human leukocytes and platelets: H. Salari, et al.; Prostagl. Leukotr. Med. 13, 53 (1984) Abstract
Incorporation of 5,8,11,14-eicosatetraynoic acid (ETYA) into cell lipids: competition with arachidonic acid for esterification: A.S. Taylor, et al.; Prostaglandins 29, 449 (1985) Abstract
Inhibition of U937 eicosanoid and DNA synthesis by 5,8,11,14- eicosatetraynoic acid, an inhibitor of arachidonic acid metabolism and its partial reversal by leukotriene C4: F. Ondrey, et al.; Cancer Res. 49, 1138 (1989) Abstract
Effects of 5,8,11,14-eicosatetraynoic acid on thapsigargin-induced calcium entry, and intracellular pH in thyroid FRTL-5 cells: E. Ekokoski & K. Tornquist; Biochim. Biophys. Acta 1223, 274 (1994) Abstract
Further Categories Containing This Product:
Cytochrome P450 [CYP450] / Related Products • PPAR Agonists • PLA2 Inhibitors • Ca2+ Modulators • COX Inhibitors
 
 
ALX-420-043 Revised 03-Sep-08
FTY720
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SYNONYMS 2-Amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol . HCl
Fingolimod . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Sphingolipids & Glycosphingolipids Other Products
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ALX-420-043-M001   1 mg 40.00 USD Add To Cart
ALX-420-043-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C19H33NO2 . HCl
MW: 307.5 . 36.5
CAS NUMBER: 162359-56-0
PURITY: ≥98%
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: 20mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; sparingly soluble in aqueous buffers.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: We do not recommend storing aqueous solutions for more than one day.

Product Description
Analog of myriocin (Prod. No. ALX-350-274). Novel immune modulator that alters migration and homing of lymphocytes. Acts as a potent agonist of sphingosine 1-phosphate receptors (S1P) after phosphorylation by sphingosine kinase. Also inhibits cytosolic phospholipase A2 independently of sphingosine 1-phosphate receptors.
Product Specific Literature References
The immune modulator FTY720 targets sphingosine 1-phosphate receptors: V. Brinkmann, et al.; J. Biol. Chem. 277, 21453 (2002) Abstract; Full Text
The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2 independently of sphingosine-1-phosphate receptors: S.G. Payne, et al.; Blood 109, 1077 (2007) Abstract
FTY720, a new alternative for treating blast crisis chronic myelogenous leukemia and Philadelphia chromosome-positive acute lymphocytic leukemia: P. Neviani, et al.; J. Clin. Invest. 117, 2408 (2007) Abstract; Full Text
Related Products
Further Categories Containing This Product:
PLA2 Inhibitors • Immunomodulators Other Products
 
 
ALX-350-138 Revised 05-Dec-06
Hexaprenylhydroquinone
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SYNONYMS HPH
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antiviral / anti-HIV Agents
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ALX-350-138-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C36H54O2
MW: 518.8
CAS NUMBER: 119980-00-6
SOURCE/HOST: Isolated from Sarcotragus sp.
PURITY: ≥97% (HPLC)
APPEARANCE: Off-white to brown solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by MS, 1H-NMR.

Product Description
Potent inhibitor of HIV reverse transcriptase and cellular DNA polymerase. Inhibitor of CDC25A. Similar compounds have shown inhibitory effects on phospholipase A2.
Product Specific Literature References
Three new heptaprenylhydroquinone derivatives from the sponge Ircinia fasciculata: Y. Venkateswarlu and M. Venkata Rami Reddy; J. Nat. Prod. 57, 1286 (1994)
Biological effects of prenylated hydroquinones: structure-activity relationship studies in antimicrobial, brine shrimp, and fish lethality assays: S. De Rosa, et al.; J. Nat. Prod. 57, 1711 (1994) Abstract
Mode of inhibition of HIV reverse transcriptase by 2-hexaprenylhydroquinone, a novel general inhibitor of RNA-and DNA-directed DNA polymerases: S. Loya, et al.; Biochem. J. 324, 721 (1997) Abstract; Full Text
Polyprenyl-hydroquinones and -furans from three marine sponges inhibit the cell cycle regulating phosphatase CDC25A: I. Erdogan-Orhan, et al.; Nat. Prod. Res. 18, 1 (2004) Abstract
General Literature References
Effects of marine 2-polyprenyl-1,4-hydroquinones on phospholipase A2 activity and some inflammatory responses: B. Gil, et al.; Eur. J. Pharmacol. 285, 281 (1995) Abstract
Further Categories Containing This Product:
PLA2 Inhibitors • Natural Products - DNA Replication Inhibitors • Marine Natural Products • HIV / AIDS / Related Products
 
 
ALX-350-035 Revised 14-Nov-07
Isotetrandrine
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SYNONYMS Berbamine methyl ether
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-035-M001   1 mg 65.00 USD Add To Cart
Product Specification
FORMULA: C38H42N2O6
MW: 622.8
CAS NUMBER: 477-57-6
RTECS: NX7285000
PURITY: ≥98%
APPEARANCE: