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NF-kB Pathway Inhibitors
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ALX-385-016 Revised 02-Jun-08
Morin
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SYNONYMS 2’,3,4’,5,7-Pentahydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonols
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-385-016-G001   1 g 16.00 USD Add To Cart
Product Specification
FORMULA: C15H10O7
MW: 302.2
CAS NUMBER: 480-16-0
MERCK INDEX: 14: 6269
RTECS: LK8749000
PURITY: ≥85%
APPEARANCE: White to brown powder.
SOLUBILITY: Soluble in methanol or 100% ethanol; slightly soluble in ether or acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: IRRITANT.

Product Description
Antioxidant flavonoid. Shows anti-proliferative and antitumor properties. Induces apoptosis. Induces cell cycle arrest at the G2/M phase. Anti-inflammatory compound. Suppresses NF-κB activation. Induces lipid peroxidation and DNA strand breaks.
Product Specific Literature References
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Lipid peroxidation and DNA damage induced by morin and naringenin in isolated rat liver nuclei: S. C. Sahu & G. C. Gray; Food Chem. Toxicol. 35, 443 (1997) Abstract
Morin inhibits the growth of human leukemia HL-60 cells via cell cycle arrest and induction of apoptosis through mitochondria dependent pathway: H.M. Kuo, et al.; Anticancer Res. 27, 395 (2007) Abstract
Morin (3,5,7,2’,4’-Pentahydroxyflavone) abolishes nuclear factor-kappaB activation induced by various carcinogens and inflammatory stimuli, leading to suppression of nuclear factor-kappaB-regulated gene expression and up-regulation of apoptosi: S.K. Manna, et al.; Clin. Cancer Res. 13, 2290 (2007) Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents • Antitumor Agents (Anti-proliferative) • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Antitumor Reagents • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antioxidants • Cell Cycle Blockers & Inhibitors / Related Products • Natural Products for Cell Cycle Research • Lipid Peroxidation
 
 
ALX-400-002 Revised 15-May-08
Pyrrolidinedithiocarbamic acid . ammonium salt
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SYNONYMS Ammoniumpyrrolidinedithiocarbamate
Ammoniumtetramethylenedithiocarbamate
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY NF-kB Pathway Inhibitors
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ALX-400-002-G005   5 g 29.00 USD Add To Cart
ALX-400-002-G025   25 g 55.00 USD Add To Cart
Product Specification
FORMULA: C5H8NS2 . NH4
MW: 146.3 . 18.0
CAS NUMBER: 5108-96-3
PURITY: ≥98%
APPEARANCE: White to-off white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: IRRITANT.

Product Description
Inhibitor of NF-κB activation (induced by either PMA or TNF-α) in various cell types.
Product Specific Literature References
Dithiocarbamates as potent inhibitors of nuclear factor kappa B activation in intact cells: R. Schreck, et al.; J. Exp. Med. 175, 1181 (1992) Abstract
Pyrrolidine dithiocarbamate inhibits NF-kappa B mobilization and TNF production in human monocytes: H.W. Ziegler-Heitbrock, et al.; J. Immunol. 151, 6986 (1993) Abstract
Pyrrolidine dithiocarbamate inhibits induction of nitric oxide synthase activity in rat alveolar macrophages: M.P. Sherman, et al.; BBRC 191, 1301 (1993) Abstract
Pyrrolidine dithiocarbamate differentially affects interleukin 1 beta- and cAMP-induced nitric oxide synthase expression in rat renal mesangial cells: W. Eberhardt, et al.; BBRC 200, 163 (1994) Abstract
In vivo antioxidant treatment suppresses nuclear factor-kappa B activation and neutrophilic lung inflammation: T.S. Blackwell, et al.; Immunol. 157, 1630 (1996) Abstract
In vivo inhibition of nuclear factor-kappa B activation prevents inducible nitric oxide synthase expression and systemic hypotension in a rat model of septic shock: S.F. Liu, et al.; J. Immunol. 159, 3976 (1997) Abstract
Zinc is required in pyrrolidine dithiocarbamate inhibition of NF-kappaB activation: C.H. Kim, et al.; FEBS Lett. 449, 28 (1999) Abstract
Dual activity of pyrrolidine dithiocarbamate on kappa B-dependent gene expression in U937 cells: I. Regulation by the phorbol ester TPA: K. Watanabe, et al.; Cell Signal 11, 479 (1999) Abstract
Inhibition of NF-kappaB activation by pyrrolidine dithiocarbamate prevents In vivo expression of proinflammatory genes: S.F. Liu, et al.; Circulation 100, 1330 (1999) Abstract
Dual activity of pyrrolidine dithiocarbamate on kappaB-dependent gene expression in U937 cells: II. Regulation by tumour necrosis factor- alpha: K. Watanabe, et al.; Cell Signal 11, 371 (1999) Abstract
Pyrrolidine dithiocarbamate inhibits TNF-alpha-dependent activation of NF-kappaB by increasing intracellular copper level in human aortic smooth muscle cells: A. Iseki, et al.; Biochem Biophys Res Commun 276, 88 (2000) Abstract
 
 
ALX-400-003 Revised 25-May-07
Diethyldithiocarbamic acid . sodium salt . trihydrate (high purity)
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SYNONYMS DETC . 3H2O (high purity)
Diethyldithiocarbamate . 3H2O (high purity)
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Spin Traps, Spin Probes & Spin Labels
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ALX-400-003-G005   5 g 17.00 USD Add To Cart
ALX-400-003-G025   25 g 27.00 USD Add To Cart
Product Specification
FORMULA: C5H10NS2 . Na . 3H2O
MW: 148.3 . 23.0 . 54.0
CAS NUMBER: 20624-25-3
MERCK INDEX: 14: 3378
RTECS: EZ6550000
PURITY: ≥99%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: HARMFUL.

Product Description
Nitric oxide (NO) spin-trapping reagent. Thiol and iron chelator. Inhibits induction of macrophage nitric oxide synthase (NOS). Has been shown to be an inhibitor of the nuclear transcription factor κB (NF-κB).
Product Specific Literature References
On-line detection of nitric oxide formation in liquid aqueous phase by electron paramagnetic resonance spectroscopy: P. Mordvintcev, et al.; Anal. Biochem. 199, 142 (1991) Abstract
NO accounts completely for the oxygenated nitrogen species generated by enzymic L-arginine oxygenation: A. Mülsch, et al.; Biochem. J. 288, 597 (1992) Abstract
Iron diethyldithiocarbamate as spin trap for nitric oxide detection: A.F. Vanin; Methods Enzymol. 301, 269 (1999), Review Abstract
Diethyldithiocarbamate inhibits induction of macrophage NO synthase: A. Mülsch, et al.; FEBS Lett. 321, 215 (1993) Abstract
The relationship between L-arginine-dependent nitric oxide synthesis, nitrite release and dinitrosyl-iron complex formation by activated macrophages: A. Vanin, et al.; Biochim. Biophys. Acta 1177, 37 (1993) Abstract
Dithiocarbamates as potent inhibitors of nuclear factor kappa B activation in intact cells: R. Schreck, et al.; J. Exp. Med. 175, 1181 (1992) Abstract
In vivo spin trapping of nitric oxide generated in the small intestine, liver, and kidney during the development of endotoxemia: a time-course study: G. Wallis, et al.; Shock 6, 274 (1996) Abstract
Epr evidence of nitric oxide production by the regenerating rat liver: M. Obolenskaya, et al.; BBRC 202, 571 (1994) Abstract
EPR and laser flash photolysis studies of the reaction of nitric oxide with water soluble NO trap Fe(II)-proline-dithiocarbamate complex: S.V. Paschenko, et al.; BBRC 225, 577 (1996) Abstract
Complexes of Fe2+ with diethyldithiocarbamate or N-methyl-D-glucamine dithiocarbamate as traps of nitric oxide in animal tissues: comparative investigations: V.D. Mikoyan, et al.; Biochim. Biophys. Acta 1336, 225 (1997) Abstract
NO-dependent mechanisms of adaptation to hypoxia: I.Y. Malyshev, et al.; Nitric Oxide 3, 105 (1999) Abstract
Ex vivo EPR detection of nitric oxide in brain tissue: H. Fujii & L.J. Berliner; Magn. Reson. Med. 42, 599 (1999) Abstract
EPR spectroscopy of common nitric oxide - spin trap complexes: S. Nedeianu & T. Pali; Cell Mol. Biol. Lett. 7, 142 (2002) Abstract
EPR quantification of vascular nitric oxide production in genetically modified mouse models: J.P. Khoo, et al.; Nitric Oxide 10, 156 (2004) Abstract
Evaluation of lipid-based carrier systems and inclusion complexes of diethyldithiocarbamate-iron to trap nitric oxide in biological systems: N. Charlier, et al.; Magn. Reson. Med. 55, 215 (2006) Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • NOS Inhibitors (NOS Induction & Enzyme Activity)
 
 
ALX-430-095 Revised 23-Jan-08
Leflunomide
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SYNONYMS HWA486
5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide)
N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
PRODUCT LINE Immunology
PRODUCT CATEGORY Immunomodulators Other Products
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ALX-430-095-M010   10 mg 15.00 USD Add To Cart
ALX-430-095-M050   50 mg 40.00 USD Add To Cart
ALX-430-095-G001   1 g 380.00 USD Add To Cart
Product Specification
FORMULA: C12H9F3N2O2
MW: 270.2
CAS NUMBER: 75706-12-6
MERCK INDEX: 14: 5432
RTECS: NY2354200
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep under inert gas. Protect from light.
HAZARD: HARMFUL.

Product Description
Immunosuppressive drug that inhibits T and B cell responses in vivo. Inhibitor of tyrosine phosphorylation (tyrosine kinase inhibitor), of dihydroorotate dehydrogenase, an enzyme for de novo pyrimidine synthesis, of TNF-dependent NF-κB activation, and of COX-2. The physiological activity of leflunomide is attributed mainly to its metabolite A77 1726 (Prod. No. ALX-430-096).
Product Specific Literature References
Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity-I. Disease modifying action on adjuvant arthritis of the rat: R.R. Bartlett & R. Schleyerbach; Int. J. Immunopharmacol. 7, 7 (1985) Abstract
Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection: R.R. Bartlett, et al.; Agents Actions 32, 10 (1991) Abstract
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
Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide: T.R. Brazelton & R.E. Morris; Curr. Opin. Immunol. 8, 710 (1996) Abstract
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Regulation of B cell function by the immunosuppressive agent leflunomide: K.F. Siemasko, et al.; Transplantation 61, 635 (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
Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti- inflammatory drugs: A.P. Curnock, et al.; J. Pharmacol. Exp. Ther. 282, 339 (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
Leflunomide, a novel immunomodulating agent, prevents the development of allergic sensitization in an animal model of allergic asthma: E. Eber, et al.; Clin. Exp. Allergy 28, 376 (1998) Abstract
Species-related inhibition of human and rat dihydroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives: W. Knecht & M. Löffler; Biochem. Pharmacol. 56, 1259 (1998) Abstract
Inhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in IgG1 production: K.F. Siemasko, et al.; J. Immunol. 160, 1581 (1998) Abstract
In vivo activity of leflunomide: pharmacokinetic analyses and mechanism of immunosuppression: A.S. Chong, et al.; Transplantation 68, 100 (1999) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF- dependent nuclear factor-kappa B activation and gene expression: S.K. Manna and 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
Leflunomide: mode of action in the treatment of rheumatoid arthritis: F.C. Breedveld & J.M. Dayer; Ann. Rheum. Dis. 59, 841 (2000) Abstract
General Literature References
Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis: M.M. Goldenberg; Clin. Ther. 21, 1837 (1999), (Review) Abstract
Leflunomide, mycophenolic acid and matrix metalloproteinase inhibitors: D.E. Furst; Rheumatology (Oxford) 38 Suppl 2, 14 (1999), (Review) Abstract
Leflunomide and methotrexate: R.F. Laan, et al.; Curr. Opin. Rheumatol. 13, 159 (2001), (Review) Abstract
Experiences with leflunomide in solid organ transplantation: J.W. Williams, et al.; Transplantation 73, 358 (2002), (Review) Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • Tyrosine Kinase Inhibitors • COX Inhibitors
 
 
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
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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 Inhibitors • COX Inhibitors • Immunomodulators Other Products
 
 
ALX-430-105 Revised 10-Dec-04
Sulindac
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SYNONYMS MK-231
(1Z)-5-Fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-1H-indene-3-acetic acid
cis-5-Fluoro-2-methyl-1-[p-(methylsulfinyl)benzylidene]-indene-3-acetic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-430-105-G001   1 g 10.00 USD Add To Cart
Product Specification
FORMULA: C20H17FO3S
MW: 356.4
CAS NUMBER: 38194-50-2
MERCK INDEX: 14: 8982
RTECS: NK8226000
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or aqueous bases.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Inhibits the NF-κB pathway. Non-steroidal anti-inflammatory drug. Reduces the level and activity of several cyclin-dependent kinases (CDKs) and induces apoptosis. For the active metabolite sulindac sulfide see Prod. No. ALX-430-106.
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • Apoptosis Inducers & Inhibitors Other Products • COX Inhibitors
 
 
ALX-430-106 Revised 31-Aug-04
Sulindac sulfide
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-430-106-M005   5 mg 32.00 USD Add To Cart
ALX-430-106-M025   25 mg 85.00 USD Add To Cart
Product Specification
FORMULA: C20H17FO2S
MW: 340.4
CAS NUMBER: 32004-67-4
PURITY: ≥98%
APPEARANCE: Yellow-orange solid.
SOLUBILITY: Soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Active metabolite of sulindac (Prod. Nr. ALX-430-105). NF-κB inhibitor. Induces apoptosis. Inhibits Ras signaling. Also inhibits cyclooxygenase (COX).
Product Specific Literature References
Antineoplastic drugs sulindac sulfide and sulfone inhibit cell growth by inducing apoptosis: G.A. Piazza, et al.; Cancer Res. 55, 3110 (1995) Abstract
Sulindac sulfide inhibits Ras signaling: C. Herrmann, et al.; Oncogene 17, 1769 (1998) Abstract
Sulindac inhibits activation of the NF-kappaB pathway: Y. Yamamoto, et al.; J. Biol. Chem. 274, 27307 (1999) Abstract; Full Text
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • COX Inhibitors • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-430-107 Revised 20-Aug-08
Sulindac sulfone
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-430-107-M005   5 mg 30.00 USD Add To Cart
ALX-430-107-M050   50 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C20H17FO4S
MW: 372.4
CAS NUMBER: 59864-04-9
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol (warm).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Metabolite of sulindac (Prod. No. ALX-430-105).
Product Specific Literature References
Sulindac inhibits activation of the NF-kappaB pathway: Y. Yamamoto, et al.; J. Biol. Chem. 274, 27307 (1999) Abstract; Full Text
Further Categories Containing This Product:
COX Inhibitors • NF-kB Pathway Inhibitors
 
 
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</