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PLA2 Inhibitors
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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
 
 
ALX-270-105 Revised 05-Dec-04
OBAA
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SYNONYMS 3-(4-Octadecyl)-benzoylacrylic acid
4-(4-Octadecylphenyl)-4-oxobutenoic acid
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PLA2 Inhibitors
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ALX-270-105-M005   5 mg 35.00 USD Add To Cart
Product Specification
FORMULA: C28H44O3
MW: 428.6
CAS NUMBER: 134531-42-3
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Potent inhibitor of phospholipase A2.
Product Specific Literature References
Phospholipase A2 inhibition by alkylbenzoylacrylic acids: T. Köhler, et al.; Agents Actions 32, 70 (1991) Abstract
Allergen-induced bronchospasm in passively sensitized guinea pigs: influence of new substances in comparison to reference compounds: S. Madi, et al.; Agents Actions 32, 144 (1991) Abstract
Phospholipase A2 inhibition by alkylbenzoylacrylic acids: T. Köhler, et al.; Biochem. Pharmacol. 44, 805 (1992) Abstract
 
 
ALX-270-115 Revised 08-Dec-05
ONO-RS-082
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SYNONYMS 2-(p-Amylcinnamoyl)amino-4-chlorobenzoic acid
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PLA2 Inhibitors
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ALX-270-115-M005   5 mg 40.00 USD Add To Cart
ALX-270-115-M025   25 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C21H22ClNO3
MW: 371.9
CAS NUMBER: 99754-06-0
PURITY: ≥98%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions are stable for 3 months when stored at -20°C.
HANDLING: Do not freeze. Protect from light.

Product Description
Phospholipase A2 inhibitor. Inhibits epinephrine-stimulated thromboxane production in human platelets. Also blocks insulin secretion in pancreatic islets in response to glucose.
Product Specific Literature References
Activation of phospholipases A and C in human platelets exposed to epinephrine: role of glycoproteins IIb/IIIa and dual role of epinephrine: H.S. Banga, et al.; PNAS 83, 9197 (1986) Abstract
Inhibition of phospholipase A2 and insulin secretion in pancreatic islets: R.J. Konrad, et al.; Biochim. Biophys. Acta 1135, 215 (1992) 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. Hantagonist. 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
 
 
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-300-142 Revised 09-Dec-04
Thioetheramide PC
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SYNONYMS 1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphocholine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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ALX-300-142-M005   5 mg 101.00 USD Add To Cart
ALX-300-142-M010   10 mg 177.00 USD Add To Cart
Product Specification
FORMULA: C40H83N2O5PS
MW: 735.1
CAS NUMBER: 116457-99-9
PURITY: ≥98%
APPEARANCE: Lyophilized powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from moisture.

Product Description
Inhibitor of snake venom phospholipase A2 (PLA2).
Product Specific Literature References
The interaction of phospholipase A2 with phospholipid analogues and inhibitors: L. Yu, et al.; J. Biol. Chem. 265, 2657 (1990) Abstract; Full Text
Further Categories Containing This Product:
PLA2 Inhibitors
 
 
ALX-300-145 Revised 18-Dec-07
MJ33
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SYNONYMS 1-Hexadecyl-3-(trifluoroethyl)-sn-glycero-2-phosphomethanol . Li
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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ALX-300-145-M005   5 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C22H43F3O6P . Li
MW: 491.6 . 6.9
PURITY: ≥93%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.

Product Description
Active site-directed, specific, competitive, and reversible inhibitor of phospholipase A2 (PLA2). Shows high specificity for type I (pancreatic) and bee venom PLA2, but has relatively poor affinity for type II human synovial PLA2.
Product Specific Literature References
Active-site-directed specific competitive inhibitors of phospholipase A2: novel transition state analogues: M.K. Jain, et al.; Biochemistry 30, 10256 (1991) Abstract
A competitive inhibitor of phospholipase A2 decreases surfactant phosphatidylcholine degradation by the rat lung: A.B. Fisher, et al.; Biochem. J. 288, 407 (1992) Abstract
Inhibition of lung calcium-independent phospholipase A2 by surfactant protein A: A.B. Fisher, et al.; Am. J. Physiol. 267, L335 (1994) Abstract
Purification and characterization of a calcium-independent acidic acid phospholipase A2 from rat lung: R. Wang, et al.; Biochem. J. 304, 131 (1994) Abstract
Role of acidic Ca2+-independent phospholipase A2 in synthesis of lung dipalmitoyl phosphatidylcholine: A.B. Fisher, et al.; Am. J. Physiol. 272, L238 (1997) Abstract
Identification of a human cDNA clone for lysosomal type Ca2+-independent phospholipase A2 and properties of the expressed protein: T.S. Kim, et al.; J. Biol. Chem. 272, 2542 (1997) Abstract; Full Text
Crystal structure of the complex of bovine pancreatic phospholipase A2 with the inhibitor 1-hexadecyl-3-(trifluoroethyl)-sn-glycero-2-phosphomethanol: K. Sekar, et al.; Biochemistry 36, 14186 (1997) Abstract
Cloning and expression of rat lung acidic Ca2+-independent PLA2 and its organ distribution: T.S. Kim, et al.; Am. J. Physiol. 274, L750 (1998) Abstract
Role of phospholipase A2 (group I secreted) in the genesis of basal tone in the internal anal sphincter smooth muscle: M.A. de Godoy & S. Rattan; Am. J. Physiol. Gastrointest. Liver. Physiol. 293, G979 (2007) Abstract
Further Categories Containing This Product:
PLA2 Inhibitors
 
 
ALX-306-008 Revised 07-Feb-05
D-erythro-Sphingosine, Dihydro-
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SYNONYMS D-erythro-Dihydrosphingosine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Ceramides / Cerebrosides / Sphingolipids / Related Products
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ALX-306-008-M010   10 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C18H39NO2
MW: 301.5
CAS NUMBER: 3102-56-5
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of protein kinase C (PKC). Blocks phospholipases A2 (PLA2) and the D-sphingosine precursor.
Product Specific Literature References
Structural requirements for long-chain (sphingoid) base inhibition of protein kinase C in vitro and for the cellular effects of these compounds: A.H. Merrill, Jr., et al.; Biochemistry 28, 3138 (1989) Abstract
Sphingolipid metabolism and signal transduction: inhibition of in vitro phospholipase activity by sphingosine: R.C. Franson, et al.; Biochim. Biophys. Acta 1136, 169 (1992) Abstract
Glucocorticoid stimulation of amnion cell prostaglandin synthesis: suppression by protein kinase C inhibitors and independence of phorbol ester-sensitive protein kinase C: T. Zakar, et al.; Biochim. Biophys. Acta 1136, 161 (1992) Abstract
Sphinganine potentiation of dimethyl sulfoxide-induced granulocyte differentiation, increase of alkaline phosphatase activity and decrease of protein kinase C activity in a human leukemia cell line (HL-60): B.Y. Yung, et al.; BBRC 199, 888 (1994) Abstract
Further Categories Containing This Product:
PKC InhibitorsPLA2 Inhibitors
 
 
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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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-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-340-0