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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:
Calmodulin Inhibitors • Phosphodiesterases / Related Products • Natural Products with Antibiotic Activity • MDR Inhibitors • P-glycoprotein [Pgp] / Related Products • Other Toxins • 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-270-304 Revised 26-Nov-04
Reversin 205
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SYNONYMS [Boc-Glu(OBzl)]2-Lys-OMe
PRODUCT LINE Cancer
PRODUCT CATEGORY MDR Inhibitors
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ALX-270-304-M005   5 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C41H58N4O12
MW: 798.8
PURITY: ≥98%
APPEARANCE: White to off white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.
Product Description
Selective high affinity inhibitor of P-glycoprotein (MDR1).
Product Specific Literature References
Micellar electrokinetic chromatography of highly hydrophobic peptides: M. Idei, et al.; Anal. Chim. Acta 372, 273 (1998)
Insights into the structure and substrate interactions of the P- glycoprotein multidrug transporter from spectroscopic studies: F.J. Sharom, et al.; Biochim. Biophys. Acta 1461, 327 (1999) Abstract
Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells: F.J. Sharom, et al.; Biochem. Pharmacol. 58, 571 (1999) Abstract
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ALX-270-305 Revised 14-May-07
Reversin 121
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SYNONYMS Boc-Asp(OBzl)-Lys(Z)-OtBu
PRODUCT LINE Cancer
PRODUCT CATEGORY MDR Inhibitors
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ALX-270-305-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C34H47N3O9
MW: 641.8
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Selective high affinity inhibitor of P-glycoprotein (MDR1).
Product Specific Literature References
Micellar electrokinetic chromatography of highly hydrophobic peptides: M. Idei, et al.; Anal. Chim. Acta 372, 273 (1998)
Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells: F.J. Sharom, et al.; Biochem. Pharmacol. 58, 571 (1999) Abstract
Insights into the structure and substrate interactions of the P- glycoprotein multidrug transporter from spectroscopic studies: F.J. Sharom, et al.; Biochim. Biophys. Acta 1461, 327 (1999) Abstract
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ALX-270-307 Revised 08-Nov-06
JS-2190
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SYNONYMS Boc-Glu(OBzl)-N,N’-dicyclohexylurea
PRODUCT LINE Cancer
PRODUCT CATEGORY MDR Inhibitors
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ALX-270-307-M005   5 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C30H45N3O6
MW: 543.7
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in chloroform (>10%); also soluble in 100% ethanol or ethanol:water 8:1 (mild heating up to 40°C).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

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Product Description
Inhibitor of P-glycoprotein (Pgp) and MRP1. Results obtained with the calcein assay protocol [1] indicate that JS-2190 is efficiently taken up by living cells.
General Literature References
[1] Calcein accumulation as a fluorometric functional assay of the multidrug transporter: Z. Hollo, et al.; Biochim. Biophys. Acta 1191, 384 (1994) 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 • NOS Inhibitors (NOS Induction & Enzyme Activity) • MDR Inhibitors • Prostaglandins Other Products • P-glycoprotein [Pgp] / Related Products • Natural Products - Nitric Oxide Pathway Modulators • 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 15-Sep-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) or 0.1N sodium hydroxide (50mg/ml).
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
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Further Categories Containing This Product:
MDR Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Natural Products - Antitumor Reagents • Natural Products - Nitric Oxide Pathway Modulators • p53 Other Products • 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: