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Antitumor Agents (Enzyme Activators & Inducers)
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Items 11 of 11
ALX-350-005 Revised 02-Oct-07
Bryostatin 1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-005-C010   10 µg 85.00 USD Add To Cart
Product Specification
FORMULA: C47H68O17
MW: 905.0
CAS NUMBER: 83314-01-6
MERCK INDEX: 14: 1457
PURITY: ≥97%
APPEARANCE: Colorless oil.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Store tightly sealed. Binds to glass and plastic surfaces in aqueous solutions.

Product Description
Binds to and activates protein kinase C (PKC). Antineoplastic.
Product Specific Literature References
Isolation and structure of Bryostatin 1: G.R. Pettit, et al.; J. Am. Chem. Soc. 104, 6846 (1982)
Bryostatin 1: differentiating agent from the depths: R.M. Stone; Leuk. Res. 21, 399 (1997) Abstract
Chemistry and clinical biology of the bryostatins: R. Mutter & M. Wills; Bioorg. Med. Chem. 8, 1841 (2000), (Review) Abstract
The clinical development of the bryostatins: A. Clamp and G.C. Jayson; Anticancer Drugs 13, 673 (2002) Abstract
The chemistry and biology of the bryostatin antitumour macrolides: K.J. Hale, et al.; Nat. Prod. Rep. 19, 413 (2002), Review Abstract
Bryostatin-1: pharmacology and therapeutic potential as a CNS drug: M.K. Sun & D.L. Alkon; CNS Drug Rev. 12, 1 (2006), Review Abstract
 
 
ALX-270-286 Revised 18-Sep-07
C75
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SYNONYMS trans-4-Carboxy-5-octyl-3-methylene-butyrolactone
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Fatty Acid Synthase [FAS]/Related Products
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ALX-270-286-M001   1 mg 65.00 USD Add To Cart
ALX-270-286-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C14H22O4
MW: 254.3
CAS NUMBER: 191282-48-1
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in dichloromethane, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Inhibitor of fatty acid synthase (FAS) reducing food intake and body weight in mice. Exhibits irreversible slow-binding biphasic inactivation of fatty acid synthase. Downregulates neuropeptide Y and Agouti-related protein expression. Has been proposed to activate CPT-1 activity in liver and adipose tissue, leading to increased fatty acid oxidation and energy production. Shows significant in vivo antitumor activity in human breast cancer cells. Suppresses DNA replication and induces apoptosis. FAS inhibition by C75 leads to a dramatic accumulation of the CDK inhibitor p27KIP1 from cytosol to cell nuclei.
Product Specific Literature References
Pharmacological inhibitors of mammalian fatty acid synthase suppress DNA replication and induce apoptosis in tumor cell lines: E.S. Pizer, et al.; Cancer Res. 58, 4611 (1998) Abstract
Synthesis and antitumor activity of an inhibitor of fatty acid synthase: F.P. Kuhajda, et al.; PNAS 97, 3450 (2000) Abstract
Reduced food intake and body weight in mice treated with fatty acid synthase inhibitors: T.M. Loftus, et al.; Science 288, 2379 (2000) Abstract
Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts: E.S. Pizer, et al.; Cancer Res. 60, 213 (2000) Abstract
Increased fatty acid synthase is a therapeutic target in mesothelioma: E.W. Gabrielson, et al.; Clin. Cancer Res. 7, 153 (2001) Abstract
Pharmacological inhibition of fatty acid synthase activity produces both cytostatic and cytotoxic effects modulated by p53: J.N. Li, et al.; Cancer Res. 61, 1493 (2001) Abstract
Green tea epigallocatechin gallate: a natural inhibitor of fatty-acid synthase: X. Wang & W. Tian; BBRC 288, 1200 (2001) Abstract
Comparison of central and peripheral administration of c75 on food intake, body weight, and conditioned taste aversion: D.J. Clegg, et al.; Diabetes 51, 3196 (2002) Abstract
Expression of FAS within hypothalamic neurons: a model for decreased food intake after C75 treatment: E.K. Kim, et al.; Am. J. Physiol. Endocrinol. Metab. 283, E867 (2002) Abstract
Differential effects of a centrally acting fatty acid synthase inhibitor in lean and obese mice: M.V. Kumar, et al.; PNAS 99, 1921 (2002) Abstract; Full Text
Effect of a fatty acid synthase inhibitor on food intake and expression of hypothalamic neuropeptides: T. Shimokawa, et al.; PNAS 99, 66 (2002) Abstract
C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity: J.N. Thupari, et al.; PNAS 99, 9498 (2002) Abstract
Effect of the anorectic fatty acid synthase inhibitor C75 on neuronal activity in the hypothalamus and brainstem: S. Gao and M.D. Lane; PNAS 100, 10 (2003) Abstract
Hypothalamic malonyl-CoA as a mediator of feeding behavior: Z. Hu, et al.; PNAS 100, 12624 (2003) Abstract
C75 inhibits food intake by increasing CNS glucose metabolism: M.D. Wortman, et al.; Nat. Med. 9, 483 (2003) Abstract
Fatty Acid Synthase Inhibition Triggers Apoptosis during S Phase in Human Cancer Cells: W. Zhou, et al.; Cancer Res. 63, 7330 (2003) Abstract
Long-term effects of a fatty acid synthase inhibitor on obese mice: food intake, hypothalamic neuropeptides, and UCP3: S.H. Cha, et al.; BBRC 317, 301 (2004) Abstract
C75, a fatty acid synthase inhibitor, modulates AMP-activated protein kinase to alter neuronal energy metabolism: L.E. Landree, et al.; J. Biol. Chem. 279, 3817 (2004) Abstract
Inhibition of tumor-associated fatty acid synthase activity antagonizes estradiol- and tamoxifen-induced agonist transactivation of estrogen receptor (ER) in human endometrial adenocarcinoma cells: J.A. Menendez, et al.; Oncogene 23, 4945 (2004) Abstract
C75 activates malonyl-CoA sensitive and insensitive components of the CPT system: C. Nicot, et al.; BBRC 325, 660 (2004) Abstract
The anorexigenic fatty acid synthase inhibitor, C75, is a non-specific neuronal activator: K.A. Takahashi, et al.; Endocrinology 145, 184 (2004) Abstract
 
 
ALX-270-262 Revised 13-Feb-08
Ellagic acid . dihydrate
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SYNONYMS 4,4',5,5',6,6'-Hexahydroxydiphenic acid 2,6,2',6'-dilactone . 2H2O
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-270-262-M100   100 mg 12.00 USD Add To Cart
Product Specification
FORMULA: C14H6O8 . 2H2O
MW: 302.2 . 36.0
CAS NUMBER: 476-66-4
MERCK INDEX: 14: 3547
RTECS: DJ2620000
SOURCE/HOST: Isolated from chestnut bark.
PURITY: ≥97%
APPEARANCE: Grey to green solid.
SOLUBILITY: Soluble in 1M sodium hydroxide (10mg/ml) or pyridine.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep under inert gas. Protect from light.
HAZARD: IRRITANT.
IDENTITY: Determined by MS and NMR.

Product Description
Polyphenol antioxidant with antitumor properties. Inhibitor of topoisomerases. Inhibits VEGF-induced phosphorylation of VEGFR-2 and PDGF-induced phosphorylation of PDGFR. Induces apoptosis.
Product Specific Literature References
The dietary anticancer agent ellagic acid is a potent inhibitor of DNA topoisomerases in vitro: A. Constantinou, et al.; Nutr. Cancer 23, 121 (1995) Abstract
Novel inhibitors of 3-phosphoglycerate kinase: M.J. Hickey, et al.; Biochem. Soc. Trans. 23, 607S (1995) Abstract
Inhibitory actions of ellagic acid on growth and arylamide N-acetyltransferase activity in strains of Heliobacter pylori from peptic ulcer patients: J.G. Chung; Microbios 93, 115 (1998) Abstract
Polyphenols inhibit promotional phase of tumorigenesis: relevance of superoxide radicals: A. Kaul & K.L. Khanduja; Nutr. Cancer 32, 81 (1998) Abstract
Inhibition of eukaryote serine/threonine-specific protein kinases by piceatannol: B.H. Wang, et al.; Planta Med. 64, 195 (1998) Abstract
p53/p21 (WAF1CIP1) expression and its possible role in G1 arrest and apoptosis in ellagic acid treated cancer cells: B.A. Narayanan, et al.; Cancer Lett. 136, 215 (1999) Abstract
Combined inhibition of PDGF and VEGF receptors by ellagic acid, a dietary-derived phenolic compound: L. Labrecque, et al.; Carcinogenesis 26, 821 (2005) Abstract
Antioxidant and apoptosis-inducing activities of ellagic acid: D.H. Han, et al.; Anticancer Res. 26, 3601 (2006) Abstract
The efficacy of protective effects of tannic acid, gallic acid, ellagic acid, and propyl gallate against hydrogen peroxide-induced oxidative stress and DNA damages in IMR-90 cells: C.H. Chen, et al.; Mol. Nutr. Food Res. 51, 962 (2007) Abstract
Ellagic acid, a natural polyphenol protects rat peripheral blood lymphocytes against nicotine-induced cellular and DNA damage in vitro: with the comparison of N-acetylcysteine: A.R. Sudheer, et al.; Toxicology 230, 11 (2007) Abstract
 
 
ALX-350-223 Revised 07-Apr-08
Kahweol
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-223-M010   10 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C20H26O3
MW: 314.2
CAS NUMBER: 6894-43-5
SOURCE/HOST: Natural product isolated from the unsaponifiable fraction of petroleum ether extract of coffee beans.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in ethyl acetate, acetone or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Induces glutathione S-transferase. Has anti-cancer, chemoprotective, anti-inflammatory and anti-atherosclerotic properties.
Product Specific Literature References
R.O. Bengis & R.J. Anderson; J. Biol. Chem. 47, 99 (1932)
Isolation and identification of kahweol palmitate and cafestol palmitate as active constituents of green coffee beans that enhance glutathione S-transferase activity in the mouse: L.K. Lam, et al.; Cancer Res. 42, 1193 (1982) Abstract
Effects of derivatives of kahweol and cafestol on the activity of glutathione S-transferase in mice: L.K. Lam, et al.; J. Med. Chem. 30, 1399 (1987) Abstract
Placental glutathione S-transferase (GST-P) induction as a potential mechanism for the anti-carcinogenic effect of the coffee-specific components cafestol and kahweol: B. Schilter, et al.; Carcinogenesis 17, 2377 (1996) Abstract
Chemoprotection against the formation of colon DNA adducts from the food-borne carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in the rat: W.W. Huber, et al.; Mutat. Res. 376, 115 (1997) Abstract
The coffee-specific diterpenes cafestol and kahweol protect against aflatoxin B1-induced genotoxicity through a dual mechanism: C. Cavin, et al.; Carcinogenesis 19, 1369 (1998) Abstract
Cafestol and kahweol, two coffee specific diterpenes with anticarcinogenic activity: C. Cavin, et al.; Food Chem. Toxicol. 40, 1155 (2002) Abstract
The coffee diterpene kahweol inhibits tumor necrosis factor-alpha-induced expression of cell adhesion molecules in human endothelial cells: H.G. Kim, et al.; Toxicol. Appl. Pharmacol. 217, 332 (2006) Abstract
 
 
ALX-350-227 Revised 28-Apr-08
Myristicin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-227-M100   100 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C11H12O3
MW: 192.2
CAS NUMBER: 607-91-0
MERCK INDEX: 14: 6334
SOURCE/HOST: Isolated from Petroselinium hortense Hoffmann.
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless to slightly yellow liquid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Natural product isolated from parsley oil. Inducer of glutathione S-transferases. Also inhibits chemical carcinogenesis. Induces rat and human cytochrome P450 enzymes. Has very potent hepatoprotective activity. Induces apoptosis.
Product Specific Literature References
Myristicin: a potential cancer chemopreventive agent from parsley leaf oil: G.-Q. Zheng, et al.; J. Agri. Food Chem. 40, 107 (1992)
Inhibition of benzo[a]pyrene-induced tumorigenesis by myristicin, a volatile aroma constituent of parsley leaf oil: G.-Q. Zheng, et al.; Carcinogenesis 13, 1921 (1992) Abstract
Induction of rat hepatic cytochrome P450 enzymes by myristicin: H.G. Jeong & C.H. Yun; BBRC 217, 966 (1995) Abstract
Toxicological evaluation of myristicin: H. Hallstrom & A. Thuvander; Nat. Toxins 5, 186 (1997), Review Abstract
Roles of human liver cytochrome P450 3A4 and 1A2 enzymes in the oxidation of myristicin: C.H. Yun, et al.; Toxicol. Lett. 137, 143 (2003) Abstract
Hepatoprotective effect of myristicin from nutmeg (Myristica fragrans) on lipopolysaccharide/ d-galactosamine-induced liver injury: T. Morita, et al.; J. Agric. Food Chem. 51, 1560 (2003) Abstract
Myristicin-induced neurotoxicity in human neuroblastoma SK-N-SH cells: B.K. Lee, et al.; Toxicol. Lett. 157, 49 (2005) Abstract
 
 
ALX-350-222 Revised 28-Mar-08
Dihydromyristicin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-222-M100   100 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C11H14O3
MW: 194.2
CAS NUMBER: 52811-28-6
PURITY: ≥98% (TLC)
APPEARANCE: Colorless liquid.
SOLUBILITY: Soluble in 100% ethanol or ethyl acetate; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Hydrogenated product of myristicin (Prod. No. ALX-350-227), a natural constituent of parsley. Inducer of glutathione S-transferases.
Product Specific Literature References
Myristicin: a potential cancer chemopreventive agent from parsley leaf oil: G.-Q. Zheng, et al.; J. Agri. Food Chem. 40, 107 (1992)
Inhibition of benzo[a]pyrene-induced tumorigenesis by myristicin, a volatile aroma constituent of parsley leaf oil: G.Q. Zheng, et al.; Carcinogenesis 13, 1921 (1992) Abstract
 
 
ALX-350-228 Revised 08-Jul-08
Nomilin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-228-M025   25 mg 105.00 USD Add To Cart
Product Specification
FORMULA: C28H34O9
MW: 514.6
CAS NUMBER: 1063-77-0
MERCK INDEX: 14: 6674
SOURCE/HOST: Isolated from grapefruit seed and citrus juice.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetone; slightly soluble in 100% ethanol, methanol, isopropanol or ethyl acetate; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Induces phase II detoxifying enzymes and inhibits chemically induced carcinogenesis. Exhibits immunomodulatory activity and also inhibits HIV-1 replication. Does not possess any inherent antioxidant capacity.
Product Specific Literature References
V.P. Maier, et al.; ACS Symposium Series 143, 63 (1980)
Inhibition of benzo[a]pyrene-induced forestomach neoplasia in mice by citrus limonoids: L.K.T. Lam & S. Hasegawa; Nutr. Cancer 12, 43 (1989) Abstract
The effect of citrus limonoids on hamster buccal pouch carcinogenesis: E.G. Miller, et al.; Carcinogenesis 10, 1535 (1989) Abstract
Effect of naturally occurring triterpenoids glycyrrhizic acid, ursolic acid, oleanolic acid and nomilin on the immune system: T.J. Raphael & G. Kuttan; Phytomedicine 10, 483 (2003) Abstract
Effect of limonin and nomilin on HIV-1 replication on infected human mononuclear cells: L. Battinelli, et al.; Planta Med. 69, 910 (2003) Abstract
Evaluation of the antioxidant capacity of limonin, nomilin, and limonin glucoside: A.P. Breksa, 3rd & G.D. Manners; J. Agric. Food Chem. 54, 3827 (2006) Abstract
 
 
ALX-350-229 Revised 24-Jul-08
Sedanolide
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SYNONYMS 3-Butyl-3a,4,5,6-tetrahydro-1(3H)-isobenzofuranone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-229-M100   100 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C12H18O2
MW: 194.1
CAS NUMBER: 6415-59-4
SOURCE/HOST: Isolated from Apium graveolens L.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol or ethyl acetate.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
MELTINGPOINT: 30-31°C

Product Description
Inducer of glutathione S-transferases and inhibitor of chemically induced carcinogenesis. Mosquitocidal, nematicidal and antifungal. Was shown to inhibit cyclooxygenase-1 and -2 (COX-1 and COX-2) as well as topoisomerase I and topoisomerase II.
Product Specific Literature References
Chemoprevention of benzo[a]pyrene-induced forestomach cancer in mice by natural phthalides from celery seed oil: G.-Q. Zheng, et al.; Nutr. Cancer 19, 77 (1993) Abstract
Mosquitocidal, nematicidal, and antifungal compounds from Apium graveolens L. seeds: R.A. Momin & M.G. Nair; J. Agric. Food Chem. 49, 142 (2001) Abstract
Sedanolide, a natural phthalide from celery seed oil: effect on hydrogen peroxide and tert-butyl hydroperoxide-induced toxicity in HepG2 and CaCo-2 human cell lines: J.A. Woods, et al.; In Vitr. Mol. Toxicol. 14, 233 (2001) Abstract
Antioxidant, cyclooxygenase and topoisomerase inhibitory compounds from Apium graveolens Linn. seeds: R.A. Momin & M.G. Nair; Phytomedicine 9, 312 (2002) Abstract
 
 
ALX-350-232 Revised 17-Jul-08
DL-Sulforaphane
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SYNONYMS R,S-Sulforaphane
1-Isothiocyanato-4-methylsulfinyl-butane
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-232-M025   25 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C6H11NOS2
MW: 177.3
CAS NUMBER: 142825-10-3; 4478-93-7 (unspecified stereo)
MERCK INDEX: 14: 8962
SOURCE/HOST: Synthetic.
PURITY: ≥98% (UPLC)
APPEARANCE: Slightly yellowish liquid.
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by 1H-NMR and MS.

Product Description
Potent, selective inducer of phase II detoxification enzymes. Inhibits chemically induced mammary tumor formation in rats. Inhibits LPS-induced HMGB1 (high mobility group box 1) secretion.
Product Specific Literature References
A major inducer of anticarcinogenic protective enzymes from broccoli: isolation and elucidation of structure: Y. Zhang, et al.; PNAS 89, 2399 (1992) Abstract; Full Text
Anticarcinogenic activities of sulforaphane and structurally related synthetic norbornyl isothiocyanates: Y. Zhang, et al.; PNAS 91, 3147 (1994) Abstract; Full Text
A novel mechanism of chemoprotection by sulforaphane: inhibition of histone deacetylase: M.C. Myzak, et al.; Cancer Res. 64, 5767 (2004) Abstract; Full Text
The phase 2 enzyme inducers ethacrynic acid, DL-sulforaphane, and oltipraz inhibit lipopolysaccharide-induced high-mobility group box 1 secretion by RAW 264.7 cells: M.E. Killeen, et al.; J. Pharmacol. Exp. Ther. 316, 1070 (2006)