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NF-kB Pathway
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ALX-430-096 Revised 24-Feb-05
A77 1726
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SYNONYMS N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-096-M005   5 mg 45.00 USD Add To Cart
ALX-430-096-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C12H9F3N2O2
MW: 270.2
CAS NUMBER: 108605-62-5
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No. ALX-430-095). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2) in vitro and in vivo.
Product Specific Literature References
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms: R.T. Elder, et al.; J. Immunol. 159, 22 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression: S.K. Manna & B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract
Further Categories Containing This Product:
NF-kB Pathway InhibitorsCOX InhibitorsImmunomodulators Other Products
 
 
ALX-350-310 Revised 03-Apr-08
3-O-Acetyl-11-keto-β-boswellic acid
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SYNONYMS AKβBA
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-310-M005   5 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C32H48O5
MW: 512.7
CAS NUMBER: 67416-61-9
SOURCE/HOST: Isolated from Boswellia serrata.
PURITY: ≥99% (HPLC, NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetone, dichloromethane, diethyl ether or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Shows antitumor and anti-inflammatory activities. Potent non-redox, noncompetitive 5-lipoxygenase and topoisomerase I and IIa inhibitor leading to apoptosis. 10-times more potent than 3-O-acetyl-β-boswellic acid (Prod. No. ALX-350-308). Exhibits in vivo efficacy in tumor growth and inhibition.
Product Specific Literature References
Acetyl-11-keto-beta-boswellic acid induces apoptosis in HL-60 and CCRF-CEM cells and inhibits topoisomerase I: R.F. Hoernlein, et al.; J. Pharmacol. Exp. Ther. 288, 613 (1999) Abstract; Full Text
Boswellic acids activate p42(MAPK) and p38 MAPK and stimulate Ca(2+) mobilization: A. Altmann, et al.; BBRC 290, 185 (2002) Abstract
Coupling of boswellic acid-induced Ca2+ mobilisation and MAPK activation to lipid metabolism and peroxide formation in human leucocytes: A. Altmann, et al.; Br. J. Pharmacol. 141, 223 (2004) Abstract; Full Text
Inhibition of IkappaB kinase activity by acetyl-boswellic acids promotes apoptosis in androgen-independent PC-3 prostate cancer cells in vitro and in vivo: T. Syrovets, et al.; J. Biol. Chem. 280, 6170 (2005) Abstract; Full Text
Boswellic acids: biological actions and molecular targets: D. Poeckel & O. Werz; Curr. Med. Chem. 13, 3359 (2006), Review Abstract
Mechanisms underlying the anti-inflammatory actions of boswellic acid derivatives in experimental colitis: C. Anthoni, et al.; Am. J. Physiol. Gastrointest. Liver Physiol. 290, G1131 (2006) Abstract
Potentiation of antinociceptive effect of NSAIDs by a specific lipooxygenase inhibitor, acetyl 11-keto-beta boswellic acid: M. Bishnoi, et al.; Indian J. Exp. Biol. 44, 128 (2006) Abstract
 
 
ALX-480-021 Revised 16-Dec-04
Adenosine 5'-triphosphate . disodium salt
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SYNONYMS ATP . 2Na
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Adenosine Derivatives Other Products
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ALX-480-021-G001   1 g 15.00 USD Add To Cart
ALX-480-021-G005   5 g 45.00 USD Add To Cart
Product Specification
FORMULA: C10H14N5O13P3. 2Na
MW: 505.2 . 46.0
CAS NUMBER: 51963-61-2
MERCK INDEX: 14: 155
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from moisture. Keep cool and dry.

Further Categories Containing This Product:
Inflammasome
 
 
ALX-430-110 Revised 16-Jan-08
5-Aminosalicylic acid
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SYNONYMS 5-ASA
Mesalamine
5-Amino-2-hydroxybenzoic acid
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY NF-kB Pathway Inhibitors
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ALX-430-110-G005   5 g 20.00 USD Add To Cart
Product Specification
FORMULA: C7H7NO3
MW: 153.1
CAS NUMBER: 89-57-6
MERCK INDEX: 14: 5904
PURITY: ≥98%
SOLUBILITY: Soluble in 1 M hydrochloric acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
Product Description
Inhibits TNF-α regulated IκB degradation and NF-κB activation.
Product Specific Literature References
Inhibition of nuclear factor kappa B and induction of apoptosis in T-lymphocytes by sulfasalazine: S. Liptay, et al.; Br. J. Pharmacol. 128, 1361 (1999) Abstract
Aminosalicylic acid inhibits IkappaB kinase alpha phosphorylation of IkappaBalpha in mouse intestinal epithelial cells: F. Yan & D.B. Polk; J. Biol. Chem. 274, 36631 (1999) Abstract; Full Text
Further Categories Containing This Product:
Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
 
 
ALX-340-029 Revised 08-Jul-08
Anandamide
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SYNONYMS AEA
N-Arachidonoylethanolamine
(all-Z)-N-(2-Hydroxyethyl)-5,8,11,14-eicosatetraenamide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Anandamide & Anandamide Analogs
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-029-M005   5 mg 51.00 USD Add To Cart
Product Specification
FORMULA: C22H37NO2
MW: 347.5
CAS NUMBER: 94421-68-8
MERCK INDEX: 14: 624
RTECS: JX3842500
CONCENTRATION: 50mg/ml 
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: 10mg/ml soluble in DMSO or dimethyl formamide.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. Stable for at least 6 months in other organic solvents when stored at -20°C.
HANDLING: Protect from light and oxygen.

Product Description
Endogenous [1] ligand for the CB1 receptor (CB1: Ki=52nm; CB2: Ki=1930nm [2]) and TRPV1 (Ki=5.78µM [3,4]). Inhibits NF-κB activation through direct binding to IKKβ [5] and induces apoptosis independently of cannabinoid or vanilloid receptors [6]. Activates the MAP kinase (MAPK/ERK) signalling pathway [7].
Product Specific Literature References
[1] Isolation and structure of a brain constituent that binds to the cannabinoid receptor: W.A. Devane, et al.; Science 258, 1946 (1992) Abstract
[2] Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability: S. Lin, et al.; J. Med. Chem. 41, 5353 (1998) Abstract
[3] Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide: P.M. Zygmunt, et al.; Nature 400, 452 (1999) Abstract
[4] Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens: R.A. Ross, et al.; Br. J. Pharmacol. 132, 631 (2001) Abstract
[5] Anandamide inhibits nuclear factor-kappaB activation through a cannabinoid receptor-independent pathway: R. Sancho, et al.; Mol. Pharmacol. 63, 429 (2003) Abstract
[6] Anandamide induces cell death independently of cannabinoid receptors or vanilloid receptor 1: possible involvement of lipid rafts: K.P. Sarker, et al.; Cell Mol. Life Sci. 60, 1200 (2003) Abstract
[7] The MAP kinase signal transduction pathway is activated by the endogenous cannabinoid anandamide: M. Wartmann, et al.; FEBS Lett. 359, 133 (1995) Abstract
Biochemistry and pharmacology of arachidonylethanolamide, a putative endogenous cannabinoid: C.J. Hillard & W.B. Campbell; J. Lipid Res. 38, 2383 (1997), (Review) Abstract
The endogenous cannabinoid anandamide inhibits human breast cancer cell proliferation: L. De Petrocellis, et al.; PNAS 95, 8375 (1998) Abstract
Cannabinoid receptors and their endogenous agonist, anandamide: J. Axelrod & C.C. Felder; Neurochem. Res. 23, 575 (1998), (Review) Abstract
Endocannabinoids: endogenous cannabinoid receptor ligands with neuromodulatory action: V. Di Marzo, et al.; TINS 21, 521 (1998), (Review) Abstract
Endocannabinoids: a new class of vasoactive substances: M.D. Randall & D.A. Kendall; TIPS 19, 55 (1998), (Review) Abstract
Metabolism of anandamide and 2-arachidonoylglycerol: an historical overview and some recent developments: V. Di Marzo, et al.; Lipids 34, S319 (1999), (Review) Abstract
Anandamide: a candidate neurotransmitter heads for the big leagues: D.W. Self; Nat. Neurosci. 2, 303 (1999), (Review) Abstract
New perspectives on enigmatic vanilloid receptors: A. Szallasi & V. Di Marzo; TINS 23, 491 (2000), (Review) Abstract
Anandamide: some like it hot: V. Di Marzo, et al.; TIPS 22, 346 (2001), (Review) Abstract
Anandamide is an endogenous inhibitor for the migration of tumor cells and T lymphocytes: J. Joseph, et al.; Cancer Immunol. Immunother. 53, 723 (2004) Abstract
Anandamide-induced cell death in primary neuronal cultures: role of calpain and caspase pathways: V.A. Movsesyan, et al.; Cell Death Differ. 11, 1121 (2004) Abstract
Arachidonylethanolamide induces apoptosis of human glioma cells through vanilloid receptor-1: E. Contassot, et al.; J. Neuropathol. Exp. Neurol. 63, 956 (2004) Abstract
Preferred conformations of endogenous cannabinoid ligand anandamide: J.Z. Chen, et al.; Life Sci. 76, 2053 (2005) Abstract
The cardiovascular actions of anandamide: more targets?: M.D. Randall; Br. J. Pharmacol. 145, 565 (2005) Abstract; Full Text
Accumulation of anandamide: Evidence for cellular diversity: C.J. Hillard and A. Jarrahian; Neuropharmacology 48, 1072 (2005) Abstract
Anandamide as an intracellular messenger regulating ion channel activity: M. van der Stelt and V. Di Marzo; Prostaglandins Other Lipid Mediat. 77, 111 (2005) Abstract
Anandamide reduces infarct size in rat isolated hearts subjected to ischaemia-reperfusion by a novel cannabinoid mechanism: N.J. Underdown, et al.; Br. J. Pharmacol. 146, 809 (2005) Abstract
Anandamide inhibits adhesion and migration of breast cancer cells: C. Grimaldi, et al.; Exp. Cell Res. 312, 363 (2006) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
 
 
ALX-840-602 Revised 24-Nov-05
Positive Control (Cell Lysate) for Antibodies to Asc (human)
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SYNONYMS Positive Control (Cell Lysate) for Antibodies to Pycard (human)
PRODUCT LINE Immunology
PRODUCT CATEGORY Positive Controls (Cell Lysates & Extracts)
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ALX-840-602-R100   100 µl 70.00 USD Add To Cart
Product Specification
SOURCE/HOST: Whole cell lysate of HEK 293T cells transfected with an expression plasmid for human Asc (aa 1-195) fused at the C-terminus to a FLAG®-tag.
QUANTITY: 100µl corresponding to 2x105 cells.
FORMULATION: Liquid. In 5x sample buffer (312.5mM TRIS, pH 6.8, containing 10% SDS, 6% glycerol, 0.075% bromophenol blue, 10% β-mercaptoethanol and 10mM DTT).
APPLICATION: Positive control in Western blot for PAb to Asc (human) (AL177) (Prod. No. ALX-210-905). Add 13µl sterile water and 2µl DTT (100mM) to 5µl of cell lysate.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: After opening, prepare aliquots and store at -20°C. Avoid freeze/thaw cycles.
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General Information
BACKGROUND/TECHNICAL INFORMATION FLAG is a registered trademark of Sigma-Aldrich Co.
MANUFACTURER Manufactured by Apotech Corporation.
Further Categories Containing This Product:
Caspase Recruitment Domain [CARD] Proteins / Related ProductsInflammasome
 
 
ALX-430-115 Revised 14-Aug-08
Aspirin
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SYNONYMS Acetylsalicylic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-430-115-G005   5 g 10.00 USD Add To Cart
Product Specification
FORMULA: C9H8O4
MW: 180.2
CAS NUMBER: 50-78-2
MERCK INDEX: 14: 851
RTECS: VO0700000
PURITY: ≥99%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol (80mg/ml), DMSO (41mg/ml) or dimethyl formamide (30mg/ml); slightly soluble in PBS, pH 7.2 (2.7mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Stable for at least 2 years when stored at room temperature. Keep aqueous solutions on ice and use within 30 minutes. Unstable in basic solutions pH>7.4.
HAZARD: HARMFUL.

Product Specific Literature References
Inhibition of NF-kappa B by sodium salicylate and aspirin: E. Kopp & S. Ghosh; Science 265, 956 (1994) Abstract
Neuroprotection by aspirin and sodium salicylate through blockade of NF- kappaB activation: M. Grilli, et al.; Science 274, 1383 (1996) Abstract
The anti-inflammatory agents aspirin and salicylate inhibit the activity of I(kappa)B kinase-beta: M.J. Yin, et al.; Nature 396, 77 (1998) Abstract
The pleiotropic functions of aspirin: mechanisms of action: A.R. Amin, et al.; Cell Mol. Life Sci. 56, 305 (1999) Abstract
 
 
ALX-270-219 Revised 15-May-07
BAY 11-7082
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SYNONYMS (E)-3-(4-Methylphenylsulfonyl)-2-propenenenitrile
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY NF-kB Pathway Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-219-M010   10 mg 45.00 USD Add To Cart
ALX-270-219-M050   50 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C10H9NO2S
MW: 207.3
CAS NUMBER: 195462-67-7
PURITY: ≥99%
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol or methylene dichloride; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Inhibitor of cytokine induced IκBα phosphorylation resulting thereby in a decreased expression of NF-κB and adhesion molecules. Potential anti-inflammatory agent.
Product Specific Literature References
Novel inhibitor of cytokine-induced IkBa phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo: J.W. Pierce, et al.; J. Biol. Chem. 272, 21096 (1997) Abstract; Full Text
Inhibition of NF-kappaB induces apoptosis of KSHV-infected primary effusion lymphoma cells: S.A. Keller, et al.; Blood 96, 2537 (2000) Abstract
Insulin-like growth factor-I protects colon cancer cells from death factor-induced apoptosis by potentiating tumor necrosis factor alpha- induced mitogen-activated protein kinase and nuclear factor kappaB signaling pathways: M.M. Remacle-Bonnet, et al.; Cancer Res. 60, 2007 (2000) Abstract
Up-regulation of multidrug resistance P-glycoprotein via nuclear factor- kappaB activation protects kidney proximal tubule cells from cadmium- and reactive oxygen species-induced apoptosis: F. Thevenod, et al.; J. Biol. Chem. 275, 1887 (2000) Abstract; Full Text
Neuronal injury-induced expression and release of apolipoprotein E in mixed neuron/glia co-cultures: nuclear factor kappaB inhibitors reduce basal and lesion-induced secretion of apolipoprotein E: V. Petegnief, et al.; Neuroscience 104, 223 (2001) Abstract
Poly(ADP-ribose) polymerase-1 promotes microglial activation, proliferation, and matrix metalloproteinase-9-mediated neuron death: T.M. Kauppinen & R.A. Swanson; J. Immunol. 174, 2288 (2005) Abstract; Full Text
Further Categories Containing This Product:
Anti-inflammatory Agents Other Products
 
 
ALX-270-220 Revised 04-Nov-05
BAY 11-7085
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SYNONYMS (E)-3-(t-Butylphenylsulfonyl)-2-propenenitrile
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY NF-kB Pathway Inhibitors
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ALX-270-220-M010   10 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C13H15NO2S
MW: 249.3
CAS NUMBER: 196309-76-9
PURITY: ≥98%
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in DMSO or ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Has biological properties very similar to those of BAY 11-7082 (Prod. No. ALX-270-219). In addition, the product exhibits potent anti-inflammatory properties in vivo.
Product Specific Literature References
Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo: J.W. Pierce, et al.; J. Biol. Chem. 272, 21096 (1997) Abstract; Full Text
Pharmacologic interference with NF-kappaB activation attenuates central nervous system complications in experime