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DNA Regulation / Transcription
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ALX-350-095 Revised 03-Apr-08
Apicidin
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SYNONYMS cyclo-L-(2-Amino-8-oxodecanoyl)-L-(N-methoxy-tryptophan)-L-isoleucyl-D-pipecolinyl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-095-M001   1 mg 50.00 USD Add To Cart
ALX-350-095-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C34H49N5O6
MW: 623.8
CAS NUMBER: 183506-66-3
SOURCE/HOST: Isolated from Fusarium sp.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC.

Product Description
Potent inhibitor of histone deacetylase (HDAC). Inhibits proliferation. Induces cell cycle arrest. Stimulates apoptosis of cancer cells. Antiprotozoal.
Product Specific Literature References
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase: S.J. Darkin-Rattray, et al.; PNAS 93, 13143 (1996) Abstract
Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin: J.W. Han, et al.; Cancer Res. 60, 6068 (2000) Abstract
Transcriptional activation of p21(WAF1/CIP1) by apicidin, a novel histone deacetylase inhibitor: J.S. Kim, et al.; BBRC 281, 866 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 107 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 113 (2001) Abstract
Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities: S.B. Singh, et al.; J. Org. Chem. 67, 815 (2002) Abstract
Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells: J. Hong, et al.; Cancer Lett. 189, 197 (2003) Abstract
Activation of NF-kappaB by HDAC inhibitor apicidin through Sp1-dependent de novo protein synthesis: its implication for resistance to apoptosis: Y.K. Kim, et al.; Cell Death Differ. 13, 2033 (2006) Abstract
Apicidin, a novel histone deacetylase inhibitor, has profound anti-growth activity in human endometrial and ovarian cancer cells: T. Ueda, et al.; Int. J. Mol. Med. 19, 301 (2007) Abstract
 
 
ALX-350-097 Revised 16-Jun-08
Hyperforin . dicyclohexylammonium salt (high purity)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-350-097-C500   500 µg 130.00 USD Add To Cart
ALX-350-097-M001   1 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C35H51O4 . C12H24N
MW: 535.8 . 182.3
CAS NUMBER: 11079-53-1 (non-salt form)
SOURCE/HOST: Isolated from St. John's wort (Hypericum perforatum).
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
PURITY DETAIL: Contains <3% adhyperforin.
SOLUBILITY: Soluble in DMSO, methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Major constituent of St. John’s wort, a herbal remedy widely used for the treatment of depression. Inhibits the reuptake of neurotransmitters in synapses. Activator of the pregnane X receptor (PXR), which serves as a key regulator of CYP3A4 transcription, a member of the cytochrome (CYP) P450 enzyme system. Specifically activates TRPC6 channels. Represents an interesting lead-structure for a new class of antidepressants. Displays several other biological properties of potential pharmacological interest, including antibacterial, anti-inflammational, antitumoral and anti-angiogenic effects. Induces apoptosis in various cancer cells.
Product Specific Literature References
Hyperforin as a possible antidepressant component of hypericum extracts: S.S. Chatterjee, et al.; Life Sci. 63, 499 (1998) Abstract
Hyperforin attenuates various ionic conductance mechanisms in the isolated hippocampal neurons of rat: S. Chatterjee, et al.; Life Sci. 65, 2395 (1999) Abstract
Antibacterial activity of hyperforin from St John's wort, against multiresistant Staphylococcus aureus and gram-positive bacteria: C.M. Schempp, et al.; Lancet 353, 2129 (1999) Abstract
Hyperforin, a major antidepressant constituent of St. John's Wort, inhibits serotonin uptake by elevating free intracellular Na+1: A. Singer, et al.; J. Pharmacol. Exp. Ther. 290, 1363 (1999) Abstract
St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor: L.B. Moore, et al.; PNAS 97, 7500 (2000) Abstract
Inhibition of human cytochrome P450 enzymes by constituents of St. John's Wort, an herbal preparation used in the treatment of depression: R.S. Obach; J. Pharmacol. Exp. Ther. 294, 88 (2000) Abstract
St John's wort, a herbal antidepressant, activates the steroid X receptor: J.M. Wentworth, et al.; J. Endocrinol. 166, R11 (2000) Abstract
St John's wort (Hypericum perforatum L.): a review of its chemistry, pharmacology and clinical properties: J. Barnes, et al.; J. Pharm. Pharmacol. 53, 583 (2001), (Review) Abstract
St John's wort: Prozac from the plant kingdom: G. Di Carlo, et al.; TIPS 22, 292 (2001), (Review) Abstract
Effect of St. John's wort on free radical production: E.J. Hunt, et al.; Life Sci. 69, 181 (2001) Abstract
Hypericum perforatum (St John's Wort): a non-selective reuptake inhibitor? A review of the recent advances in its pharmacology: P.J. Nathan; J. Psychopharmacol. 15, 47 (2001), (Review) Abstract
Aristoforin, a novel stable derivative of hyperforin, is a potent anticancer agent: M. Gartner, et al.; Chembiochem 6, 171 (2005) Abstract
Hyperforin, a new lead compound against the progression of cancer and leukemia?: C. Quiney, et al.; Leukemia 20, 1519 (2006), (Review) Abstract
Hyperforin a key constituent of St. John’s wort specifically activates TRPC6 channels: K. Leuner, et al.; FASEB J. 21, 4101 (2007) Abstract
 
 
ALX-350-098 Revised 05-Apr-08
Ferutinin (high purity)
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SYNONYMS Tefestrol (high purity)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-098-M001   1 mg 35.00 USD Add To Cart
ALX-350-098-M005   5 mg 100.00 USD Add To Cart
ALX-350-098-M010   10 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C22H30O4
MW: 358.5
SOURCE/HOST: Semisynthetic.
PURITY: ≥98%
SOLUBILITY: Soluble in acetone, dichloromethane, DMSO or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent, naturally occuring non-steroid estrogenic compound. Agonist for estrogen receptor (ER) α and agonist/antagonist for ERβ with higher binding affinity than tamoxifen (Prod. No. ALX-550-095) for both ERs. Electrogenic Ca2+ ionophore inducing mitochondrial depolarisation which can be completely blocked by cyclosporin A (Prod. No. ALX-380-002), suggesting that ferutinin opens the mitochondrial permeability transition pore (mPTP). In a concentration range of 1-50µM ferutinin increases the permeability of thymocytes, mitochondria, sarcoplasmic reticulum, liposomes and bilayer lipid membranes for Ca2+.
Product Specific Literature References
Ferutinine structure: A.I. Saidkhodjaev, et al.; Chem. Nat. Comp. 1, 28 (1973)
Ionophoretic properties of ferutinin: M.V. Zamaraeva, et al.; Cell Calcium 22, 235 (1997) Abstract
Influence of plant terpenoids on the permeability of mitochondria and lipid bilayers: A.Y. Abramov, et al.; Biochim. Biophys. Acta 1512, 98 (2001) Abstract
Daucane phytoestrogens: a structure-activity study: G. Appendino, et al.; J. Nat. Prod. 65, 1612 (2002) Abstract
Terpenoids found in the umbelliferae family act as agonists/antagonists for ER(alpha) and ERbeta: differential transcription activity between ferutinine-liganded ER(alpha) and ERbeta: K. Ikeda, et al.; BBRC 291, 354 (2002) Abstract
Actions of ionomycin, 4-BrA23187 and a novel electrogenic Ca2+ ionophore on mitochondria in intact cells: A.Y. Abramov & M.R. Duchen; Cell Calcium 33, 101 (2003) 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-350-246 Revised 07-Oct-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol. Specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
 
 
ALX-350-247 Revised 21-May-08
Genistin
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SYNONYMS Genistein-7-O-glucoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-247-M010   10 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C21H20O10
MW: 432.4
CAS NUMBER: 529-59-9
MERCK INDEX: 14: 4391
PURITY: ≥98%
APPEARANCE: Off-white to light yellow powder.
SOLUBILITY: Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Glucoside of genistein (Prod. No. ALX-350-006) found in soy beans. Useful as a negative control for genistein and other tyrosine kinase inhibitors. Selective inhibitor of terminal deoxyribonucleotidyltransferase (TdT). Displays antioxidant and anticarcinogenic properties.
Product Specific Literature References
Soybean isoflavones, genistein and genistin, inhibit rat myoblast proliferation, fusion and myotube protein synthesis: S. Ji, et al.; J. Nutr. 129, 1291 (1999) Abstract
Daidzein and genistein but not their glucosides are absorbed from the rat stomach: M.K. Piskula, et al.; FEBS Lett. 447, 287 (1999) Abstract
Inhibition of CYP1A1 enzyme activity in mouse hepatoma cell culture by soybean isoflavones: H.G. Shertzer, et al.; Chem. Biol. Interact. 123, 31 (1999) Abstract
Selective inhibitors of terminal deoxyribonucleotidyltransferase (TdT): baicalin and genistin: Y. Uchiyama, et al.; Biochim. Biophys. Acta 1725, 298 (2005) Abstract
Genistin inhibits UV light-induced plasmid DNA damage and cell growth in human melanoma cells: A. Russo, et al.; J. Nutr. Biochem. 17, 103 (2006) Abstract
Pro-apoptotic effect and cytotoxicity of genistein and genistin in human ovarian cancer SK-OV-3 cells: E.J. Choi, et al.; Life Sci. 80, 1403 (2007) Abstract
 
 
ALX-350-254 Revised 10-Mar-08
Epoxomicin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome / Ubiquitin Modulators
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ALX-350-254-C050   50 µg 132.00 USD Add To Cart
Product Specification
FORMULA: C28H50N4O7
MW: 554.7
CAS NUMBER: 134381-21-8
MERCK INDEX: 14: 3630
SOURCE/HOST: Synthetic.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (15mg/ml); insoluble in water.
ACTIVITY: kobs/[I] = 25’000M-1s-1 versus 20S proteasome.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles. Protect from light.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Cell permeable, potent and selective proteasome inhibitor originally isolated from Actinomycetes strain based on its potent in vivo antitumor activity. More potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin. Effectively inhibits NF-κB activation in vitro and potently blocks inflammation in vivo in the mouse ear edema assay.
Product Specific Literature References
Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. (Tokyo) 45, 1746 (1992) Abstract
Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency: K.B. Kim, et al.; Bioorg. Med. Chem. Lett. 9, 3335 (1999) Abstract
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999) Abstract
Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology: N. Sin, et al.; Bioorg. Med. Chem. Lett. 9, 2283 (1999) Abstract
The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses: K. Schwarz, et al.; J. Immunol. 164, 6147 (2000) Abstract
Establishment and some characteristics of epoxomicin (a proteasome inhibitor) resistant variants of the human squamous cell carcinoma cell line, A431: K. Ohkawa, et al.; Int. J. Oncol. 24, 425 (2004) Abstract
 
 
ALX-350-258 Revised 08-Apr-08
Parthenolide
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SYNONYMS (1aR-[1aR*,4E,7aS*,-10aS*,-10bR*])-2,3-6,7,7a,8,10a,10b-Octahydro-1a,5-dimethyl-8-methyleneoxireno[9,10]cyclo deca[1,2-b]furan-9(1aH)-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-258-M005   5 mg 15.00 USD Add To Cart
ALX-350-258-M025   25 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C15H20O3
MW: 248.3
CAS NUMBER: 20554-84-1
MERCK INDEX: 14: 7048
RTECS: LY4220000
SOURCE/HOST: Isolated from feverfew leaves.
PURITY: ≥99% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (100mg/ml), dichloromethane (50mg/ml) or 100% ethanol (20mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Sesquiterpene lactone. Anti-inflammatory compound. Specifically inhibits activation of NF-κB by preventing the degradation of IκBα and IκBβ. Inhibits activation of MAP kinase (MAPK/ERK) and generation of leukotriene B4 and thromboxane B2. Potent anticancer agent. Induces apoptosis in various cancer cell lines. Specifically inhibits histone deacetylase 1 (HDAC1) without affecting other class I/II HDACs. Inhibits tubulin carboxypeptidase (TCP) activity.

Product Specific Literature References
A comparison of the effects of an extract of feverfew and parthenolide, a component of feverfew, on human platelet activity in-vitro: W.A. Groenewegen & S. Heptinstall; J. Pharm. Pharmacol. 42, 553 (1990) Abstract
Feverfew extracts and parthenolide irreversibly inhibit vascular responses of the rabbit aorta: R.W. Barsby, et al.; J. Pharm. Pharmacol. 44, 737 (1992) Abstract
Inhibition of 5-lipoxygenase and cyclo-oxygenase in leukocytes by feverfew. Involvement of sesquiterpene lactones and other components: H. Sumner, et al.; Biochem. Pharmacol. 43, 2313 (1992) Abstract
Inhibition of the expression of inducible cyclooxygenase and proinflammatory cytokines by sesquiterpene lactones in macrophages correlates with the inhibition of MAP kinases: D. Hwang, et al.; BBRC 226, 810 (1996) Abstract
Sesquiterpene lactones specifically inhibit activation of NF-kappa B by preventing the degradation of I kappa B-alpha and I kappa B-beta: S.P. Hehner, et al.; J. Biol. Chem. 273, 1288 (1998) Abstract
Sesquiterpene lactones inhibit inducible nitric oxide synthase gene expression in cultured rat aortic smooth muscle cells: H.R. Wong & I.Y. Menendez; BBRC 262, 375 (1999) Abstract
The antiinflammatory sesquiterpene lactone parthenolide inhibits NF- kappa B by targeting the I kappa B kinase complex: S.P. Hehner, et al.;