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Natural Products - NF-kB Pathway Inhibitors
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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-350-277 Revised 03-Apr-08
Betulinic acid (high purity)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
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-350-277-M005   5 mg 32.00 USD Add To Cart
ALX-350-277-M025   25 mg 95.00 USD Add To Cart
ALX-350-277-M100   100 mg 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane) tree bark.
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: IRRITANT.

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
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
Induction of central signalling pathways and select functional effects in human platelets by beta-boswellic acid: D. Poeckel, et al.; Br. J. Pharmacol. 146, 514 (2005) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari and D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid and its derivatives, potent DNA topoisomerase II inhibitors, from the bark of Bischofia javanica: S. Wada & R. Tanaka; Chem. Biodivers. 2, 689 (2005) Abstract
Betulinic acid as new activator of NF-kappaB: molecular mechanisms and implications for cancer therapy: H. Kasperczyk, et al.; Oncogene 24, 6945 (2005) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract
 
 
ALX-350-298 Revised 03-Apr-08
Betulinic acid (~95%)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
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-350-298-M100   100 mg 55.00 USD Add To Cart
ALX-350-298-M500   500 mg 180.00 USD Add To Cart
ALX-350-298-G001   1 g 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane tree) bark.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection: R.H. Cichewicz & S.A. Kouzi; Med. Res. Rev. 24, 90 (2004), Review Abstract
Betulinic acid-induced apoptosis in leukemia cells: H. Ehrhardt, et al.; Leukemia 18, 1406 (2004) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari & D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid decreases expression of bcl-2 and cyclin D1, inhibits proliferation, migration and induces apoptosis in cancer cells: W. Rzeski, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 374, 11 (2006) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract
 
 
ALX-270-480 Revised 10-Mar-08
Caffeic acid ethyl ester
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SYNONYMS CAEE
Ethyl caffeate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-270-480-M050   50 mg 20.00 USD Add To Cart
ALX-270-480-M250   250 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C11H12O4
MW: 208.2
CAS NUMBER: 66648-50-8
SOURCE/HOST: Synthetic.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at -20°C.
HANDLING: Protect from light and moisture.

Product Description
Shows anti-carcinogenic, anti-inflammatory and immunomodulatory properties. Suppresses lipopolysaccharide (LPS)-induced nitric oxide (NO) production (IC50=5.5µg/ml). Potent and specific inhibitor of NF-κB and its downstream inflammatory mediators inducible nitric oxide synthase (iNOS; NOS II), prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2). Prevents DNA single-strand breaks caused by H2O2.
Product Specific Literature References
Inhibitory effects of caffeic acid ethyl ester on H2O2-induced cytotoxicity and DNA single-strand breaks in Chinese hamster V79 cells: T. Nakayama, et al.; Biosci. Biotechnol. Biochem. 60, 316 (1996) Abstract
Ethyl caffeate suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2, and PGE2 in vitro or in mouse skin: Y.M. Chiang, et al.; Br. J. Pharmacol. 146, 352 (2005) Abstract
Antitumor activity of some natural flavonoids and synthetic derivatives on various human and murine cancer cell lines: M. Cardenas, et al.; Bioorg. Med. Chem. 14, 2966 (2006) Abstract
Drastic effect of several caffeic acid derivatives on the induction of heme oxygenase-1 expression revealed by quantitative real-time RT-PCR: K. Suzuki, et al.; Biofactors 28, 151 (2006) Abstract
 
 
ALX-350-278 Revised 08-Apr-08
Caffeic acid n-octyl ester
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SYNONYMS n-Octylcaffeate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
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ALX-350-278-M005   5 mg 25.00 USD Add To Cart
ALX-350-278-M025   25 mg 100.00 USD Add To Cart
Product Specification
FORMULA: C17H24O4
MW: 292.2
PURITY: ≥99%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
More potent analog than CAPE (Prod. No. ALX-270-244). Suppressor of inducible nitric oxide synthase (iNOS; NOS II). Induces apoptosis.
Product Specific Literature References
Mechanism of toxicity of esters of caffeic and dihydrocaffeic acids: B. Etzenhouser, et al.; Bioorg. Med. Chem. 9, 199 (2001) Abstract
A novel antioxidant, octyl caffeate, suppression of LPS/IFN-gamma-induced inducible nitric oxide synthase gene expression in rat aortic smooth muscle cells: G. Hsiao, et al.; Biochem. Pharmacol. 65, 1383 (2003) Abstract
Caffeic acid derivatives: in vitro and in vivo anti-inflammatory properties: F.M. da Cunha, et al.; Free Radic. Res. 38, 1241 (2004) Abstract
Octylcaffeate induced apoptosis in human leukemia U937 cells: M. Ujibe, et al.; Biol. Pharm. Bull. 28, 2338 (2005) Abstract
General Information
Octylcaffeate significantly ameliorates circulatory failure of endotoxemia by suppression of iNOS (NOS II) expression through inactivation of mitogen-activated protein kinases.
 
 
ALX-270-244 Revised 03-Apr-08
Caffeic acid phenylethyl ester
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SYNONYMS CAPE
Phenethyl caffeiate
Caffeic acid phenethyl ester
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-244-M010   10 mg 20.00 USD Add To Cart
ALX-270-244-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C17H16O4
MW: 284.3
CAS NUMBER: 115610-29-2
SOURCE/HOST: Synthetic.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetone or acetonitrile; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at –20°C.
HANDLING: Protect from light and moisture.
HAZARD: IRRITANT.

Product Description
Active component of propolis from honeybee hives, known to have anti-mitogenic, anti-carcinogenic, anti-inflammatory, and immunomodulatory properties. Potent and specific inhibitor of NF-κB activation, induced by TNF-α (Prod. No. ALX-522-008 (human) or Prod. No. ALX-522-009 (mouse)), PMA (Prod. No. ALX-445-004) and other inflammatory agents. Exhibits inhibitory activity against HIV-1 integrase (IC50=7µM). Suppresses lipid peroxidation and inhibits ornithine decarboxylase, protein tyrosine kinase and lipoxygenase activities. Induces apoptosis.
Product Specific Literature References
Hydroxylated aromatic inhibitors of HIV-1 integrase: T.R. Burke Jr., et al.; J. Med. Chem. 38, 4171 (1995) Abstract
Apoptosis and altered redox state induced by caffeic acid phenethyl ester (CAPE) in transformed rat fibroblast cells: C. Chiao, et al.; Cancer Res. 55, 3576 (1995) Abstract
Caffeic acid phenethyl ester is a potent and specific inhibitor of activation of nuclear transcription factor NF-kappa B: K. Natarajan, et al.; PNAS 93, 9090 (1996) Abstract
Inhibitory effects of caffeic acid phenethyl ester on the activity and expression of cyclooxygenase-2 in human oral epithelial cells and in a rat model of inflammation: P. Michaluart, et al.; Cancer Res. 59, 2347 (1999) Abstract
Caffeic acid phenethyl ester induces leukocyte apoptosis, modulates nuclear factor-kappa B and suppresses acute inflammation: Z. Orban, et al.; Neuroimmunomodulation 7, 99 (2000) Abstract
Caffeic acid phenethyl ester inhibits T-cell activation by targeting both nuclear factor of activated T-cells and NF-kappaB transcription factors: N. Marquez, et al.; J. Pharmacol. Exp. Ther. 308, 993 (2004) Abstract
Caffeic acid derivatives: in vitro and in vivo anti-inflammatory properties: F.M. da Cunha, et al.; Free Radic. Res. 38, 1241 (2004) Abstract
Drastic effect of several caffeic acid derivatives on the induction of heme oxygenase-1 expression revealed by quantitative real-time RT-PCR: K. Suzuki, et al.; Biofactors 28, 151 (2006) Abstract
 
 
ALX-270-254 Revised 22-Sep-08
Carnosol
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SYNONYMS 1,3,4,9,10,10aS-Hexahydro-5,6-dihydroxy-1,1-dimethyl-7-isopropyl-2H-9S,4aR-(epoxymethano)phenanthren-12-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-254-M001   1 mg 60.00 USD Add To Cart
ALX-270-254-M005   5 mg 269.00 USD Add To Cart
Product Specification
FORMULA: C20H26O4
MW: 330.4
CAS NUMBER: 5957-80-2
SOURCE/HOST: Isolated from Rosmarinus officinalis.
PURITY: ≥96%
APPEARANCE: White to beige solid.
SOLUBILITY: Soluble in 100% ethanol (8mg/ml), DMSO (250mg/ml) or dimethyl formamide (35mg/ml); sparingly soluble in aqueous PBS, pH 7.2 (<30μg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.
HANDLING: Protect from light.

Product Description
Naturally occurring phenolic compound with antioxidant and anti-inflammatory properties. Suppresses nitric oxide (NO) production and inducible nitric oxide synthase (iNOS; NOS II) gene expression by inhibiting NF-κB activation. Inhibits lipid peroxidation. Antimicrobial. Anticarcinogenic. Inhibits cyclooxygenase-2 (COX-2).
Product Specific Literature References
Antioxidant and pro-oxidant properties of active rosemary constituents: carnosol and carnosic acid: O.I. Aruoma, et al.; Xenobiotica 22, 257 (1992) Abstract
Effects of three dietary phytochemicals from tea, rosemary and turmeric on inflammation-induced nitrite production: M.M. Chan, et al.; Cancer Lett. 96, 23 (1995) Abstract
Inhibition of lipid peroxidation and superoxide generation by diterpenoids from Rosmarinus officinalis: H. Haraguchi, et al.; Planta Med. 61, 333 (1995) Abstract
Inhibition by rosemary and carnosol of 7,12-dimethylbenz[a]anthracene (DMBA)-induced rat mammary tumorigenesis and in vivo DMBA-DNA adduct formation: K. Singletary, et al.; Cancer Lett. 104, 43 (1996) Abstract
Development of in vitro models for cellular and molecular studies in toxicology and chemoprevention: K. Macé, et al.; Arch. Toxicol. Suppl. 20, 227 (1998) Abstract
Carnosol, an antioxidant in rosemary, suppresses inducible nitric oxide synthase through down-regulating nuclear factor-kappaB in mouse macrophages: A.H. Lo, et al.; Carcinogenesis 23, 983 (2002) Abstract
Carnosic acid and carnosol, phenolic diterpene compounds of the labiate herbs rosemary and sage, are activators of the human peroxisome proliferator-activated receptor gamma: O. Rau, et al.; Planta Med. 72, 881 (2006) Abstract
Potentiation of antimicrobial activity of aminoglycosides by carnosol from Salvia officinalis: K. Horiuchi, et al.; Biol. Pharm. Bull. 30, 287 (2007) Abstract