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MDR Inhibitors
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ALX-270-109 Revised 14-Apr-08
Ophiobolin A
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SYNONYMS Cochliobolin A
Ophiobalin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-270-109-MC01   0.1 mg 50.00 USD Add To Cart
ALX-270-109-M001   1 mg 220.00 USD Add To Cart
Product Specification
FORMULA: C25H36O4
MW: 400.6
CAS NUMBER: 4611-05-6
RTECS: RL1576000
SOURCE/HOST: Isolated from Bipolaris leersia MST-FP107.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in dimethyl formamide, DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Cell permeable antagonist of calmodulin. Inhibits Ca2+/calmodulin-dependent phosphodiesterase. Inhibits P-glycoprotein-mediated transport. Exhibits antibacterial, antitumor and nematocidal activities. Phytotoxic.
Product Specific Literature References
The structure of ophiobolin, a C25 terpenoid having a novel skeleton: S. Nozoe, et al.; JACS 87, 4968 (1965) Abstract
The constitution of cochliobolin: L. Canonica, et al.; THL 7, 1211 (1966)
Ophiobolin A. A natural product inhibitor of calmodulin: P.C. Leung, et al.; J. Biol. Chem. 259, 2742 (1984) Abstract; Full Text
Role of Calmodulin Inhibition in the Mode of Action of Ophiobolin A: P.C. Leung, et al.; Plant Physiol. 77, 303 (1985) Abstract; Full Text
Characterization of the interaction of ophiobolin A and calmodulin: P.C. Leung, et al.; Int. J. Biochem. 20, 1351 (1988) Abstract
Microbial metabolites of ophiobolin A and antimicrobial evaluation of ophiobolins: E. Li, et al.; J. Nat. Prod. 58, 74 (1995) Abstract
The biology of ophiobolins: T.K. Au, et al.; Life Sci. 67, 733 (2000), Review Abstract
Calmodulin and lipid binding to synaptobrevin regulates calcium-dependent exocytosis: S. Quetglas, et al.; EMBO J. 21, 3970 (2002) Abstract; Full Text
Herbicidal potential of ophiobolins produced by Drechslera gigantea: A. Evidente, et al.; J. Agric. Food Chem. 54, 1779 (2006) Abstract
Inhibition of P-glycoprotein-mediated transport by terpenoids contained in herbal medicines and natural products: N. Yoshida, et al.; Food Chem. Toxicol. 44, 2033 (2006) Abstract
Further Categories Containing This Product:
Natural Products with Antibiotic Activity • P-glycoprotein [Pgp] / Related Products • Other Toxins • MDR Inhibitors • Calmodulin Inhibitors • Phosphodiesterases / Related Products • Natural Products - Antitumor Reagents
 
 
ALX-270-290 Revised 22-Apr-08
PGP-4008
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SYNONYMS N-(1-Benzyl-2,3-dihydro-1H-pyrrolo[2,3-b]quinolin-4-yl)-2-phenylacetamide
PRODUCT LINE Cancer
PRODUCT CATEGORY MDR Inhibitors
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ALX-270-290-M002   2 mg 96.00 USD Add To Cart
ALX-270-290-M010   10 mg 310.00 USD Add To Cart
Product Specification
FORMULA: C26H23N3O
MW: 393.5
PURITY: ≥98%
APPEARANCE: White to off white powder.
SOLUBILITY: Soluble in methanol, 100% ethanol (3mg/ml) or DMSO (20mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Selective P-glycoprotein (Pgp) inhibitor. Effectively reverses Pgp mediated drug resistance in NCI/ADR cells, but has no effect on the drug sensitivities of MCF-7/VP cells that overexpress MRP1.
Product Specific Literature References
Development of a syngeneic in vivo tumor model and its use in evaluating a novel P-glycoprotein modulator, PGP-4008: B.D. Lee, et al.; Oncol. Res. 14, 49 (2003) Abstract
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-: B.D. Lee, et al.; J. Med. Chem. 47, 1413 (2004) Abstract
 
 
ALX-270-360 Revised 21-May-08
Tryptanthrin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products for Inflammation Research
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ALX-270-360-M001   1 mg 50.00 USD Add To Cart
ALX-270-360-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C15H8N2O2
MW: 248.2
CAS NUMBER: 13220-57-0
SOURCE/HOST: Synthetic.
PURITY: ≥98% (1H-NMR, HPLC)
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO (8mg/ml) or methanol (0.3mg/ml); sparingly soluble in water (2.5µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years after receipt when stored at +4°C in the dark. Stock solutions made in DMSO must be stored in the dark no longer than one month.
HANDLING: Protect from light and moisture.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR, IR, MS and UV.

Product Description
Potent inhibitor of prostaglandin and leukotriene synthesis in various cell lines. Selective inhibitor of cyclooxygenase 2 (COX-2). Inhibitor of inducible nitric oxide synsthase (iNOS; NOS II) expression. Inhibits the production of IFN-γ and IL-2 after stimulation of Peyer’s patch lymphocytes with staphylococcal enterotoxin B (SEB). Inhibits P-glycoprotein (Pgp) (expressed by the MDR1 gene) and reverses doxorubicin (Prod. No. ALX-380-042) resistance on breast cancer cells.
Product Specific Literature References
H. Danz, et al.; Arch. Pharm. Suppl. I 333, 11 (2000)
Identification and isolation of the cyclooxygenase-2 inhibitory principle in Isatis tinctoria: H. Danz, et al.; Planta Med. 67, 411 (2001) Abstract
Inhibitory activity of tryptanthrin on prostaglandin and leukotriene synthesis: H. Danz, et al.; Planta Med. 68, 875 (2002) Abstract
Tryptanthrin inhibits nitric oxide and prostaglandin E(2) synthesis by murine macrophages: T. Ishihara, et al.; Eur. J. Pharmacol. 407, 197 (2000) Abstract
Tryptanthrin inhibits interferon-gamma production by Peyer’s patch lymphocytes derived from mice that had been orally administered staphylococcal enterotoxin: Y. Takei, et al.; Biol. Pharm. Bull. 26, 365 (2003) Abstract
Tryptanthrin inhibits MDR1 and reverses doxorubicin resistance in breast cancer cells: S.T. Yu, et al.; BBRC 358, 79 (2007) Abstract
General Information
Tryptanthrin occurs as a natural product in various plants, including Isatis tinctoria, I. indigotica, Polygonum tinctorium, Couroupita guianensis, Wrightia tinctoria and Calanthe discolor.
Further Categories Containing This Product:
Leukotrienes Other Products • Prostaglandins Other Products • P-glycoprotein [Pgp] / Related Products • NOS Inhibitors (NOS Induction & Enzyme Activity) • Natural Products - Nitric Oxide Pathway Modulators • MDR Inhibitors • COX Inhibitors
 
 
ALX-340-021 Revised 04-Jun-08
MK-571 . sodium salt
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Leukotrienes Other Products
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ALX-340-021-M005   5 mg 45.00 USD Add To Cart
ALX-340-021-M025   25 mg 190.00 USD Add To Cart
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Product Specification
FORMULA: C26H26ClN2O3S2 . Na
MW: 514.1 . 23.0
CAS NUMBER: 115104-28-4
PURITY: ≥97% (HPLC)
APPEARANCE: Off-white to light yellow solid.
SOLUBILITY: Soluble in water (20mg/ml), aqueous buffers, 100% ethanol (10mg/ml) or DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Aqueous stock solutions may be stable for more than 24 hours but we recommend making a fresh preparation before use.
HANDLING: Hygroscopic.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Leukotriene LTD4 receptor antagonist that potently inhibits MRP1.
Product Specific Literature References
The leukotriene LTD4 receptor antagonist MK571 specifically modulates MRP associated multidrug resistance: V. Gekeler, et al.; BBRC 208, 345 (1995) Abstract
Resistance of human multidrug resistance-associated protein 1-overexpressing lung tumor cells to the anticancer drug arsenic trioxide: L. Vernhet, et al.; Biochem. Pharmacol. 61, 1387 (2001) Abstract
Overexpression of glutathione S-transferase II and multidrug resistance transport proteins is associated with acquired tolerance to inorganic arsenic: J. Liu, et al.; Mol. Pharmacol. 60, 302 (2001) Abstract
P-Glycoprotein and transporter MRP1 reduce HIV protease inhibitor uptake in CD4 cells: potential for accelerated viral drug resistance?: K. Jones, et al.; Aids 15, 1353 (2001) Abstract
Impact of BCRP/MXR, MRP1 and MDR1/P-Glycoprotein on thermoresistant variants of atypical and classical multidrug resistant cancer cells: U. Stein, et al.; Int. J. Cancer 97, 751 (2002) Abstract
Further Categories Containing This Product:
MDR Inhibitors
 
 
ALX-350-015 Revised 02-Dec-08
(S)-(+)-Camptothecin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
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ALX-350-015-M050   50 mg 40.00 USD Add To Cart
ALX-350-015-M250   250 mg 150.00 USD Add To Cart
ALX-350-015-G001   1 g 295.00 USD Add To Cart
Product Specification
FORMULA: C20H16N2O4
MW: 348.4
CAS NUMBER: 7689-03-4
MERCK INDEX: 14: 1735
RTECS: UQ0492000
SOURCE/HOST: Isolated from Mappia foetida Miers (Nothapodytes foetida (Wt.) Sleumer).
PURITY: ≥98% (HPLC)
APPEARANCE: Pale yellow powder.
SOLUBILITY: Soluble in DMSO (10mg/ml), methanol (40mg/ml), 0.1N sodium hydroxide (50mg/ml) or acetic acid; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and moisture. After reconstitution, prepare aliquots and store at -20°C.
HAZARD: TOXIC.

Product Description
Potent antitumor agent. Inhibitor of DNA-topoisomerase I. Activates p53 resulting in upregulated expression of TRAIL-R2 (DR5) and Bak to overcome TRAIL resistance in Bax-deficient human colon carcinoma cells. Suppresses nitric oxide (NO) biosynthesis.
Product Specific Literature References
M.E. Wall, et al.; JACS 88, 3888 (1966)
The current status of camptothecin analogues as antitumor agents: W.J. Slichenmyer, et al.; J. Natl. Cancer Inst. 85, 271 (1993), (Review) Abstract
RNA synthesis inhibitors increase melatonin production in Y79 human retinoblastoma cells: J.L. Janavs, et al.; Mol. Brain Res. 23, 47 (1994) Abstract
Camptothecins: from bench research to hospital wards: M. Potmesil; Cancer Res. 54, 1431 (1994), (Review) Abstract
Forskolin and camptothecin induce a 30 kDa protein associated with melatonin production in Y79 human retinoblastoma cells: J.L. Janavs, et al.; J. Neurosci. 15, 298 (1995) Abstract
Differential stabilization of eukaryotic DNA topoisomerase I cleavable complexes by camptothecin derivatives: A. Tanizawa, et al.; Biochemistry 34, 7200 (1995) Abstract
The anti-cancer drug camptothecin inhibits elongation but stimulates initiation of RNA polymerase II transcription: M. Ljungman & P.C. Hanawalt; Carcinogenesis 17, 31 (1996) Abstract
The cell cycle effects of camptothecin: Z. Darzynkiewicz, et al.; Ann. N. Y. Acad. Sci. 803, 93 (1996) Abstract
Camptothecin-induced apoptosis in p53-null human leukemia HL60 cells and their isolated nuclei: effects of the protease inhibitors Z-VAD-fmk and dichloroisocoumarin suggest an involvement of both caspases and serine proteases: T. Shimizu & Y. Pommier; Leukemia 11, 1238 (1997) Abstract
Camptothecin and taxol: discovery to clinic: M.E. Wall; Med. Res. Rev. 18, 299 (1998), Review Abstract
Camptothecin suppresses nitric oxide biosynthesis in RAW 264.7 macrophages: W.F. Chiou, et al.; Life Sci. 69, 625 (2001) Abstract
Reversal of multidrug resistance-associated protein-mediated daunorubicin resistance by camptothecin: D. Chauvier, et al.; J. Pharm. Sci. 91, 1765 (2002) Abstract
Camptothecin and taxol: historic achievements in natural products research: N.H. Oberlies & D.J. Kroll; J. Nat. Prod. 67, 129 (2004), Review Abstract
Camptothecin and its analogues: a review on their chemotherapeutic potential: D. Sriram, et al.; Nat. Prod. Res. 19, 393 (2005), Review Abstract
The effects of camptothecin on RNA polymerase II transcription: roles of DNA topoisomerase I:: G. Capranico, et al.; Biochimie 89, 482 (2007) Abstract
Related Products
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Natural Products - Nitric Oxide Pathway Modulators • p53 Other Products • MDR Inhibitors • Natural Products - Antitumor Reagents • Alkaloids
 
 
ALX-350-127 Revised 07-May-08
Fumitremorgin C
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SYNONYMS FTC
SM-Q
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Mycotoxins
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ALX-350-127-C250   250 µg 130.00 USD Add To Cart
Product Specification
FORMULA: C22H25N3O3
MW: 379.5
CAS NUMBER: 118974-02-0
SOURCE/HOST: Isolated from Aspergillus fumigatus.
PURITY: ≥96% (HPLC)
APPEARANCE: Off-white to light brown powder.
SOLUBILITY: Soluble in DMSO, methanol or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: TOXIC.

Product Description
Mycotoxin. Tremorgenic. Potent and specific inhibitor of the breast cancer resistance protein (BCRP; ABCG2). Reverses multidrug resistance mediated by BCRP and increases cytotoxicity of several anticancer agents in vitro.
Product Specific Literature References
Mycotoxins produced by Aspergillus fumigatus species isolated from molded silage: R.J. Cole, et al.; J. Agric. Food Chem. 25, 826 (1977) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. I. Taxonomy, fermentation, isolation and biological properties: C.B. Cui, et al.; J. Antibiot. 49, 527 (1996) Abstract
Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin: S.K. Rabindran, et al.; Cancer Res. 58, 5850 (1998) Abstract
Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein.: S.K. Rabindran, et al.; Cancer Res. 60, 47 (2000) Abstract
Characterization of drug transport, ATP hydrolysis, and nucleotide trapping by the human ABCG2 multidrug transporter. Modulation of substrate specificity by a point mutation.: Ozvegy, et al.; J. Biol. Chem. 277, 47980 (2002) Abstract
The role of breast cancer resistance protein in acute lymphoblastic leukemia.: S.L. Plasschaert, et al.; Clin. Cancer Res. 9, 5171 (2003) Abstract
Plasma pharmacokinetics and tissue distribution of the breast cancer resistance protein (BCRP/ABCG2) inhibitor fumitremorgin C in SCID mice bearing T8 tumors: T.S. Garimella, et al.; Cancer Chemother. Pharmacol. 55, 101 (2005) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Optical Rotation: [α]D= +19° ±1° (c=1.0 in methanol).
Further Categories Containing This Product:
Other Natural Products for Cancer Research • Breast Cancer Resistance Protein [BCRP / MXR] / Related Products • MDR Inhibitors
 
 
ALX-350-330 Revised 05-Apr-08
Evodiamine
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SYNONYMS 8,13,13b,14-Tetrahydro-14-methylindolo[2’3’-3,4]pyrido[2,1-b]quinazolin-5-[7H]-one
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-350-330-M010   10 mg 20.00 USD Add To Cart
ALX-350-330-M050   50 mg 50.00 USD Add To Cart
Product Specification
FORMULA: C19H17N3O
MW: 303.4
CAS NUMBER: 518-17-2
MERCK INDEX: 14: 3908
SOURCE/HOST: Synthetic. Originally isolated from Evodia rutaecarpa.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to light yellow solid.
SOLUBILITY: Soluble in DMSO (5mg/ml; warm).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
A cell permeable, non-pungent vanilloid receptor agonist that induces apoptosis. Inhibits nitric oxide (NO) production. Also inhibits tumor cell migration in vitro. Is effective against multidrug-resistant cancer cells.
Product Specific Literature References
Isolation of evodiamine, a powerful cardiotonic principle, from Evodia rutaecarpa Bentham (Rutaceae): N. Shoji, et al.; J. Pharm. Sci. 75, 612 (1986) Abstract
Inhibitory effect of dehydroevodiamine and evodiamine on nitric oxide production in cultured murine macrophages: W.F. Chiou, et al.; J. Nat. Prod. 60, 708 (1997) Abstract
Inhibitory effects of evodiamine on in vitro invasion and experimental lung metastasis of murine colon cancer cells: M. Ogasawara, et al.; Biol. Pharm. Bull. 24, 917 (2001) Abstract
Evodiamine, a constituent of Evodiae Fructus, induces anti-proliferating effects in tumor cells: X.F. Fei, et al.; Cancer Sci. 94, 92 (2003) Abstract
Evodiamine induces tumor cell death through different pathways: apoptosis and necrosis: Y. Zhang, et al.; Acta Pharmacol. Sin. 25, 83 (2004) Abstract
Antitumor mechanism of evodiamine, a constituent from Chinese herb Evodiae fructus, in human multiple-drug resistant breast cancer NCI/ADR-RES cells in vitro and in vivo: C.H. Liao, et al.; Carcinogenesis 26, 968 (2005) Abstract
Caspase-dependent and caspase-independent apoptosis induced by evodiamine in human leukemic U937 cells: T.J. Lee, et al.; Mol. Cancer Ther. 5, 2398 (2006) Abstract
Further Categories Containing This Product:
Natural Products - Nitric Oxide Pathway Modulators • TRPV1 Agonists and Antagonists / Related Products • Natural Products - Apoptosis Inducers & Inhibitors • MDR Inhibitors • Natural Products for Neurological Research
 
 
ALX-350-346 Revised 17-Dec-08
Silybin
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SYNONYMS Silibinin
2,3-Dihydro-3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-6-(3,5,7-trihydroxy-4-oxobenzopyran-2-yl)benzodioxin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-346-G001   1 g 10.00 USD Add To Cart
ALX-350-346-G005   5 g 35.00 USD Add To Cart
Product Specification
FORMULA: C25H22O10
MW: 482.4
CAS NUMBER: 22888-70-6; 65666-07-1
MERCK INDEX: 14: 8532
RTECS: DJ2981770
SOURCE/HOST: Originally isolated from Silybum marianum.
PURITY: ≥98%
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in 100% ethanol (0.1mg/ml), DMSO (10mg/ml), dimethyl formamide (20mg/ml), acetone or methanol; 0.5mg/ml soluble in a 1:9 solution of dimethyl formamide:PBS (pH 7.2) (dilute the dimethyl formamide solution with PBS).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: We do not recommend storing aqueous solutions for more than one day.
HAZARD: IRRITANT.

Product Description
Major active constituent of silymarin. Anti-inflammatory, cytoprotective and anti-cancer compound. Shows chemopreventive effect against skin cancer. Inhibits mitogen-activated protein kinase (MAPK). Inhibits P-glycoprotein (Pgp)-mediated cellular efflux. Inhibits cytochrome P450 enzymes. Apoptosis inducer. Blocks the production of superoxide in Kupffer cells (EC50=100µM). Antioxidant. Free radical scavenger.
Product Specific Literature References
[On the chemistry of silymarin (silybin), the active principle of the fruits from Silybum marianum (L.) Gaertn. (Carduus marianus L.)]: H. Wagner, et al.; Arzneimittelforschung 18, 688 (1968) Abstract
Inhibition of Kupffer cell functions as an explanation for the hepatoprotective properties of silibinin: C. Dehmlow, et al.; Hepatology 23, 749 (1996) Abstract; Full Text
Silibinin decreases prostate-specific antigen with cell growth inhibition via G1 arrest, leading to differentiation of prostate carcinoma cells: implications for prostate cancer intervention: X. Zi & R. Agarwal; PNAS 96, 7490 (1999) Abstract; Full Text
The flavanolignan silybin and its hemisynthetic derivatives, a novel series of potential modulators of P-glycoprotein: M. Maitrejean, et al.; Bioorg. Med. Chem. Lett. 10, 157 (2000) Abstract
Silibinin inhibits constitutive and TNFalpha-induced activation of NF-kappaB and sensitizes human prostate carcinoma DU145 cells to TNFalpha-induced apoptosis: S. Dhanalakshmi, et al.; Oncogene 21, 1759 (2002) Abstract; Full Text
Silibinin upregulates the expression of cyclin-dependent kinase inhibitors and causes cell cycle arrest and apoptosis in human colon carcinoma HT-29 cells: C. Agarwal, et al.; Oncogene 22, 8271 (2003) Abstract; Full Text
Epidermal growth factor receptor mediates silibinin-induced cytotoxicity in a rat glioma cell line: L. Qi, et al.; Cancer Biol. Ther. 2, 526 (2003) Abstract; Full Text
Silibinin down-regulates survivin protein and mRNA expression and causes caspases activation and apoptosis in human bladder transitional-cell papilloma RT4 cells: A.K. Tyagi, et al.; BBRC 312, 1178 (2003) Abstract
Silibinin causes cell cycle arrest and apoptosis in human bladder transitional cell carcinoma cells by regulating CDKI-CDK-cyclin cascade, and caspase 3 and PARP cleavages: A. Tyagi, et al.; Carcinogenesis 25, 1711 (2004)