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ALX-270-089 Revised 25-May-07
D609 . potassium salt
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SYNONYMS Tricyclodecan-9-yl xanthogenate . K
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipase C/Related Products
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ALX-270-089-M001   1 mg 25.00 USD Add To Cart
ALX-270-089-M005   5 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C11H15OS2 . K
MW: 227.4 . 39.1
CAS NUMBER: 83373-60-8
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: We recommend to prepare fresh solutions each day.

Product Description
Selective inhibitor of phosphatidylcholine-specific phospholipase C. Has been used to study the coupling of phosphatidylcholine-specific phospholipase C with sphingomyelinase. Shows antitumor and antiviral activity. Inhibits basement membrane collagen synthesis, which is the last step in the development of a new blood vessel. Inhibits induction of nitric oxide synthases (NOS). Induces apoptosis.
Product Specific Literature References
DNA and RNA virus species are inhibited by xanthates, a class of antiviral compounds with unique properties: G. Sauer, et al.; PNAS 81, 3263 (1984) Abstract
Interruption of growth signal transduction by an antiviral and antitumoral xanthate compound: K. Muller-Decker, et al.; Exp. Cell. Res. 177, 295 (1988) Abstract
Interruption of TPA-induced signals by an antiviral and antitumoral xanthate compound: inhibition of a phospholipase C-type reaction: K. Muller-Decker; BBRC 162, 198 (1989) Abstract
TNF activates NF-kappa B by phosphatidylcholine-specific phospholipase C-induced "acidic" sphingomyelin breakdown: S. Schütze, et al.; Cell 71, 765 (1992) Abstract
Inhibitors of basement membrane collagen synthesis prevent endothelial cell alignment in matrigel in vitro and angiogenesis in vivo: G.C. Haralabopoulos, et al.; Lab. Invest. 71, 575 (1994) Abstract
Induction of nitric oxide synthase activity in phagocytic cells inhibited by tricyclodecan-9-yl-xanthogenate (D609): K. Tschaikowsky, et al.; Br. J. Pharmacol. 113, 664 (1994) Abstract
Prevention of experimental allergic encephalomyelitis by targeting nitric oxide and peroxynitrite: implications for the treatment of multiple sclerosis: D.C. Hooper, et al.; PNAS 94, 2528 (1997) Abstract; Full Text
The antiviral xanthate compound D609 inhibits herpes simplex virus type 1 replication and protein phosphorylation: D.G. Walro & K.S. Rosenthal; Antiviral. Res. 36, 63 (1997) Abstract
Induction of apoptosis and potentiation of TNF- and Fas-mediated apoptosis in U937 cells by the xanthogenate compound D609: M.I. Porn-Ares, et al.; Exp. Cell Res. 235, 48 (1997) Abstract
Phosphatidylcholine-specific phospholipase inhibitor D609 differentially affects MAP kinases and immediate-early genes in PC12 cells: P.J. Kahle, et al.; Cell Signal. 10, 321 (1998) Abstract
Stimulation of DNA synthesis in untransformed cells by the antiviral and antitumoral compound tricyclodecan-9-yl-xanthogenate (D609): Z. Kiss, et al.; Biochem. Pharmacol. 55, 915 (1998) Abstract
A phosphatidylcholine phospholipase C inhibitor, D609, blocks interleukin-3 (IL-3)-induced bcl-2 expression but not c-myc expression in human IL-3-dependent cells: R.A. Mufson, et al.; Exp. Cell Res. 240, 228 (1998) Abstract
D609-phosphatidylcholine-specific phospholipase C inhibitor attenuates thapsigargin-induced sodium influx in human lymphocytes: J.R. Nofer, et al.; Cell Signal. 12, 289 (2000) Abstract
D609 inhibits ionizing radiation-induced oxidative damage by acting as a potent antioxidant: D. Zhou, et al.; J. Pharmacol. Exp. Ther. 298, 103 (2001) Abstract; Full Text
D609-sensitive tyrosine phosphorylation is involved in Fas-mediated phospholipase D activation: J.G. Kim, et al.; Exp. Mol. Med. 33, 303 (2001) Abstract; Full Text
Synthesis and phospholipase C inhibitory activity of D609 diastereomers: A. Gonzalez-Roura, et al.; Lipids 37, 401 (2002) Abstract
Sphingomyelin synthase as a potential target for D609-induced apoptosis in U937 human monocytic leukemia cells: A. Meng, et al.; Exp. Cell Res. 292, 385 (2004) Abstract
Protective effect of the xanthate, D609, on Alzheimer´s amyloid beta-peptide (1-42)-induced oxidative stress in primary neuronal cells: R. Sultana, et al.; Free Radic. Res. 38, 449 (2004) Abstract
Two distinct Fas-activated signaling pathways revealed by an antitumor drug D609: L. Zhang, et al.; Oncogene 24, 2954 (2005) Abstract
Protection against amyloid beta-peptide (1-42)-induced loss of phospholipid asymmetry in synaptosomal membranes by tricyclodecan-9-xanthogenate (D609) and ferulic acid ethyl ester: implications for Alzheimer´s disease: H. Mohmmad Abdul & D.A. Butterfield; Biochim. Biophys. Acta 1741, 140 (2005) Abstract
D609 blocks cell survival and induces apoptosis in neural stem cells: N. Wang, et al.; Bioorg. Med. Chem. Lett 16, 4780 (2006) Abstract
Further Categories Containing This Product:
NOS Inhibitors (NOS Induction & Enzyme Activity) • Angiogenesis Modulators Other Products • Antitumor Agents (Enzyme Inhibitors) • Antiviral Agents Other Products
 
 
ALX-270-277 Revised 07-Dec-04
Tyrphostin AG 1433
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SYNONYMS SU 1433
2-(3,4-Dihydroxyphenyl)-6,7-dimethylquinoxaline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
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ALX-270-277-M001   1 mg 35.00 USD Add To Cart
ALX-270-277-M005   5 mg 100.00 USD Add To Cart
Product Specification
FORMULA: C16H14N2O2
MW: 266.3
PURITY: ≥95%
APPEARANCE: Pale yellow solid.
SOLUBILITY: Soluble in DMSO. Further dilute with aqueous buffers just before use. Use fresh solutions.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Store tightly sealed in the dark.

Product Description
Potent and specific inhibitor of PDGF-β receptor kinase (IC50= 5.0µM) and VEGFR-1 (Flk-1/KDR) (IC50= 9.3µM). Also acts as an angiogenesis inhibitor.
Product Specific Literature References
Flk-1 as a target for tumor growth inhibition: L.M. Strawn, et al.; Cancer Res. 56, 3540 (1996) Abstract
The vascular endothelial growth factor receptor KDR activates multiple signal transduction pathways in porcine aortic endothelial cells: J. Kroll & J. Waltenberger; J. Biol. Chem. 272, 32521 (1997) Abstract; Full Text
Further Categories Containing This Product:
Angiogenesis Modulators Other Products
 
 
ALX-270-283 Revised 06-May-08
DL-α-Difluoromethylornithine . hydrochloride . monohydrate
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SYNONYMS DFMO . HCl . H2O
Eflornithine . HCl . H2O
RMI-71782
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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ALX-270-283-M010   10 mg 25.00 USD Add To Cart
ALX-270-283-M050   50 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C6H12F2N2O2 . HCl . H2O
MW: 182.2 . 36.5 . 18.0
CAS NUMBER: 96020-91-6
MERCK INDEX: 14: 3522
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: HARMFUL.

Product Description
Specific, irreversible inhibitor of ornithine decarboxylase (ODC), the rate-limiting enzyme in polyamine biosynthesis. Potent chemopreventive agent. Induces apoptosis. Arginase activity inhibitor.
Product Specific Literature References
Effect of alpha-difluoromethylornithine, an enzyme-activated irreversible inhibitor of ornithine decarboxylase, on L1210 leukemia in mice: N.J. Prakash, et al.; Cancer Res. 38, 3059 (1978) Abstract
Inhibition of cell proliferation by DL-alpha-difluoromethylornithine, a catalytic irreversible inhibitor of ornithine decarboxylase: S. Oredsson, et al.; Acta Chem. Scand. B 34, 457 (1980) Abstract
Kinetics of alpha-difluoromethylornithine: an irreversible inhibitor of ornithine decarboxylase: K.D. Haegele, et al.; Clin. Pharmacol. Ther. 30, 210 (1981) Abstract
The competitive inhibition of tissue transglutaminase by alpha-difluoromethylornithine: J.G. Delcros, et al.; FEBS Lett. 171, 221 (1984) Abstract
The effect of alpha-difluoromethylornithine, an inhibitor of polyamine biosynthesis, on mitogen-induced interleukin 2 production: T.L. Bowlin, et al.; Immunopharmacology 13, 143 (1987) Abstract
The enzyme-activated irreversible inhibitor of ornithine decarboxylase, DL-alpha-difluoromethylornithine: a chemopreventive agent: A.K. Verma; Prev. Med. 18, 646 (1989) Abstract
Inhibition of tumor promotion by DL-alpha-difluoromethylornithine, a specific irreversible inhibitor of ornithine decarboxylase: A.K. Verma; Basic Life Sci. 52, 195 (1990), (Review) Abstract
The polyamine synthesis inhibitor alpha-difluoromethylornithine blocks NMDA-induced neurotoxicity: M.A. Markwell, et al.; Eur. J. Pharmacol. 182, 607 (1990) Abstract
Difluoromethylornithine (DFMO), an inhibitor of nitrite production by macrophages?: D.M. Morgan; Biochem. Soc. Trans. 22, 389S (1994) Abstract
Alpha-difluoromethylornithine (DFMO) as a potent arginase activity inhibitor in human colon carcinoma cells: M. Selamnia, et al.; Biochem. Pharmacol. 55, 1241 (1998) Abstract
Development of difluoromethylornithine (DFMO) as a chemoprevention agent: F.L. Meyskens, Jr. & E.W. Gerner; Clin. Cancer Res. 5, 945 (1999), (Review) Abstract; Full Text
alpha-difluoromethylornithine induces apoptosis as well as anti-angiogenesis in the inhibition of tumor growth and metastasis in a human gastric cancer model: Y. Takahashi, et al.; Int. J. Cancer 85, 243 (2000) Abstract
Further Categories Containing This Product:
Arginine & Arginases/Related Products • Angiogenesis Modulators Other Products • Chemopreventive Agents Other Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-270-325 Revised 20-Nov-07
SB220025
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SYNONYMS 5-(2-Amino-4-pyrimidinyl)-4-(4-fluorophenyl)-1-(4-piperidinyl)imidazole
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY MAPK Pathway Inhibitors
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ALX-270-325-C500   500 µg 200.00 USD Add To Cart
Product Specification
FORMULA: C18H19FN6
MW: 338.4
CAS NUMBER: 165806-53-1
PURITY: ≥97% (HPLC)
APPEARANCE: White to pale yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Hygroscopic. Packaged under inert gas.

Product Description
Potent and specific inhibitor of human p38 (SAPK2a; IC50=60nM). Exhibits over 2000-fold greater selectivity for p38 over ERK (MAPK), 500-fold over cAMP-dependent protein kinase (PKA), 50-fold over protein kinase C (PKC), and >1000-fold over EGFR. Acts as a potent inhibitor of angiogenesis and as an inhibitor of TNF-α production.
Product Specific Literature References
Structural basis of inhibitor selectivity in MAP kinases: Z. Wang, et al.; Structure 6, 1117 (1998) Abstract
Pharmacological effects of SB 220025, a selective inhibitor of P38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models: J.R. Jackson, et al.; J. Pharmacol. Exp. Ther. 284, 687 (1998) Abstract
Further Categories Containing This Product:
Angiogenesis Modulators Other Products
 
 
ALX-306-009 Revised 17-Jan-06
D-erythro-Sphingosine, N,N-Dimethyl-
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SYNONYMS N,N-Dimethyl-D-erythro-sphingosine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Ceramides/Cerebrosides/Sphingolipids/Related Products
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ALX-306-009-M005   5 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C20H41NO2
MW: 327.6
CAS NUMBER: 119567-63-4
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent and specific inhibitor of sphingosine kinase (IC50=5µM) which blocks conversion of sphingosine to sphingosine-1-phosphate (Prod. No. ALX-306-010). Inhibitor of protein kinase C (PKC) which also stimulates Src-kinase. May affect expression of cell surface selectins, which in turn mediate leukocyte or tumor cell adhesion to endothelial cells and platelets. Induces apoptosis.
Product Specific Literature References
A specific enhancing effect of N,N-dimethylsphingosine on epidermal growth factor receptor autophosphorylation. Demonstration of its endogenous occurrence (and the virtual absence of unsubstituted sphingosine) in human epidermoid carcinoma A431 cells: Y. Igarashi, et al.; J. Biol. Chem. 265, 5385 (1990) Abstract; Full Text
Downregulation of GMP-140 (CD62 or PADGEM) expression on platelets by N,N-dimethyl and N,N,N-trimethyl derivatives of sphingosine: K. Handa, et al.; Biochemistry 30, 11682 (1991) Abstract
Effect of sphingosine and its N-methyl derivatives on oxidative burst, phagokinetic activity, and trans-endothelial migration of human neutrophils: S. Kimura, et al.; Biochem. Pharmacol. 44, 1585 (1992) Abstract
Induction of apoptosis by sphingosine in human leukemic HL-60 cells: a possible endogenous modulator of apoptotic DNA fragmentation occurring during phorbol ester-induced differentiation: H. Ohta, et al.; Cancer Res. 55, 691 (1995) Abstract
N,N-Dimethylsphingosine is a potent competitive inhibitor of sphingosine kinase but not of protein kinase C: modulation of cellular levels of sphingosine 1-phosphate and ceramide: L.C. Edsall, et al.; Biochemistry 37, 12892 (1998) Abstract
D-erythro-N,N-dimethylsphingosine inhibits bFGF-induced proliferation of cerebral, aortic and coronary smooth muscle cells: C.B. Xu, et al.; Atherosclerosis 164, 237 (2002) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products • Angiogenesis Modulators Other Products • PKC Inhibitors
 
 
ALX-306-010 Revised 31-Jan-07
D-erythro-Sphingosine 1-phosphate (high purity)
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SYNONYMS 1-SPP
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Ceramides/Cerebrosides/Sphingolipids/Related Products
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ALX-306-010-M001   1 mg 80.00 USD Add To Cart
ALX-306-010-M005   5 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C18H38NO5P
MW: 379.5
CAS NUMBER: 26993-30-6
SOURCE/HOST: Synthetic.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Sparingly soluble in 1:1 ethanol:water. Addition of small amounts of acetic acid may help to dissolve this product.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Packaged under inert gas. Hygroscopic.
HAZARD: IRRITANT.

Product Description
Sphingosine 1-phosphate (1-SPP) regulates a variety of cellular responses, including survival, cytoskeletal remodeling, chemotaxis etc. via the activation of cell surface EDG receptors. 1-SPP also promotes angiogenesis.
Product Specific Literature References
Sphingosine-1-phosphate in cell growth and cell death: S. Spiegel, et al.; Ann. NY Acad. Sci. 845, 11 (1998) Abstract
Roles of sphingosine-1-phosphate in cell growth, differentiation, and death: S. Spiegel, et al.; Biochemistry 63, 69 (1998) Abstract
Extracellular actions of sphingosine I-phosphate through endothelial differentiation gene products in mammalian cells: role in regulating proliferation and apoptosis: S. Pyne, et al.; Biochem. Soc. Trans. 27, 404 (1999) Abstract
Sphingosine 1-phosphate signalling in mammalian cells: S. Pyne & N.J. Pyne; Biochem. J. 349, 385 (2000) Abstract
Sphingosine-1-phosphate: signaling inside and out: S. Spiegel & S. Milstien; FEBS Lett. 476, 55 (2000) Abstract
Further Categories Containing This Product:
Angiogenesis Modulators Other Products
 
 
ALX-420-039 Revised 14-Aug-08
Imiquimod
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SYNONYMS 1-(2-Methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine
R-837
PRODUCT LINE Inflammation
PRODUCT CATEGORY TLR Agonists Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-420-039-M100   100 mg 55.00 USD Add To Cart
ALX-420-039-M250   250 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C14H16N4
MW: 240.3
CAS NUMBER: 99011-02-6
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (3mg/ml) or dimethyl formamide; slightly soluble in water (warm to 37°C, vortex); insoluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for up to 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C.

Product Description
Topical immune response modifier that inhibits angiogenesis. Up-regulates IL-18 and down-regulates MMP-9 through recognition of Toll-like receptor 7 (TLR7) and subsequent activation of MyD88-dependent pathway.
Product Specific Literature References
Imiquimod applied topically: a novel immune response modifier and new class of drug: R.L. Miller, et al.; Int. J. Immunopharmacol. 21, 1 (1999) Abstract
Small anti-viral compounds activate immune cells via the TLR7 MyD88-dependent signaling pathway: H. Hemmi, et al.; Nat. Immunol. 3, 196 (2002) Abstract
In vivo and in situ modulation of the expression of genes involved in metastasis and angiogenesis in a patient treated with topical imiquimod for melanoma skin metastases: C. Hesling, et al.; Br. J. Dermatol. 150, 761 (2004) Abstract
Imiquimod as an antiangiogenic agent: V.W. Li, et al.; J. Drugs Dermatol. 4, 708 (2005) Abstract
Imiquimod is a strong inhibitor of tumor cell-induced angiogenesis: S. Majewski, et al.; Int. J. Dermatol. 44, 14 (2005) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Stimulation of TLR7 can be achieved with 1-10µg/ml of the compound for 6 to 24 hours.

Related Products:
- ddWater (endotoxin-free) (Prod. No. ALX-505-008)
- PBS (endotoxin-free) (Prod. No. ALX-505-007)
Related Products
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Angiogenesis Modulators Other Products • MMPs Other Products • Inflammasome
 
 
ALX-550-409 Revised 18-May-06
Tranilast
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SYNONYMS N-(3’,4’-Dimethoxycinnamoyl)anthranilic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Anti-inflammatory Agents Other Products
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ALX-550-409-M010   10 mg 70.00 USD Add To Cart
ALX-550-409-M050   50 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C18H17NO5
MW: 327.3
CAS NUMBER: 53902-12-8
MERCK INDEX: 14: 9570
RTECS: DG8731000
PURITY: ≥95% (HPLC)
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description

Anti-inflammatory and anti-angiogenic agent. Exerts its effects by inhibiting the expression of mediators such as MCP-1,  TGF-β, TNF-α induced vascular cell adhesion molecule-1 (VCAM-1), intracellular adhesion molecule-1 (ICAM-1) and E-selectin.
Product Specific Literature References
Inhibitory action of tranilast, an anti-allergic drug, on the release of cytokines and PGE2 from human monocytes-macrophages: H. Suzawa, et al.; Jpn. J. Pharmacol. 60, 85 (1992) Abstract
Tranilast, a selective inhibitor of collagen synthesis in human skin fibroblasts: H. Yamada, et al.; J. Biochem. 116, 892 (1994) Abstract
Tranilast inhibits interleukin-1beta-induced monocyte chemoattractant protein-1 expression in rat mesangial cells: A. Chikaraishi, et al.; Eur. J. Pharmacol. 427, 151 (2001) Abstract
Tranilast inhibits cytokine-induced nuclear factor kappaB activation in vascular endothelial cells: M. Spiecker, et al.; Mol. Pharmacol. 62, 856 (2002) Abstract; Full Text
Tranilast: a novel weapon against insulin resistance: M.R. Namazi & J. Soma; Med. Hypotheses 64, 1135 (2005) Abstract
Further Categories Containing This Product:
Angiogenesis Modulators Other Products • Antitumor Reagents Other Products
 
 
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