• Home
  • Sitemap
  • Help
  • Technical Support
  • Contact
MDR Inhibitors
You are here: Product Lines > Cancer > Multidrug Resistance [MDR] > MDR Inhibitors
Toolbar - View Selection
 
 Items 1-20 of 22 Page 1 of 2 Select Page: 1 2  >>  
ALX-350-015 Revised 15-Sep-08
(S)-(+)-Camptothecin
Add to Clipboard
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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
Related Products
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-380-007 Revised 16-Jun-08
Enniatin B
Add to Clipboard
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-007-M001   1 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C33H57N3O9
MW: 639.8
CAS NUMBER: 917-13-5
MERCK INDEX: 14: 3585
SOURCE/HOST: Isolated from Fusarium orthoceras var. enniatum.
PURITY: ≥90% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO or other organic solvents; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Ionophore antibiotic. Inhibitor of the S. cerevisiae ABC transporter Pdr5p.
Inhibitor of acyl-CoA-cholesterol acyltransferase and of phosphodiesterase. Potential anticancer compound.
Product Specific Literature References
Ionophore antibiotics produced by the fungus Fusarium orthoceras var. enniatum and other Fusaria: E. Gaumann, et al.; Experientia 3, 202 (1947)
"Sandwich" complexation in cyclopeptides and its implications in membrane processes: V.T. Ivanov; Ann. N. Y. Acad. Sci. 264, 221 (1975) Abstract
Interaction of cyclic peptides and depsipeptides with calmodulin: K.A. Mereish, et al.; Pept. Res. 3, 233 (1990) Abstract
Enniatin has a new function as an inhibitor of Pdr5p, one of the ABC transporters in Saccharomyces cerevisiae: K. Hiraga, et al.; Biochem. Biophys. Res. Commun. 328, 1119 (2005) Abstract
Enniatin exerts p53-dependent cytostatic and p53-independent cytotoxic activities against human cancer cells: R. Dornetshuber, et al.; Chem. Res. Toxicol. 20, 465 (2007) Abstract
Further Categories Containing This Product:
MDR Inhibitors • Other Toxins • Antitumor Antibiotics • Antibiotics - Other Signal Transduction Pathway Modulators
 
 
ALX-350-330 Revised 05-Apr-08
Evodiamine
Add to Clipboard
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
Ordering Information
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:
MDR Inhibitors • TRPV1 Agonists and Antagonists / Related Products • Natural Products for Neurological Research • Natural Products - Nitric Oxide Pathway Modulators • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-350-127 Revised 07-May-08
Fumitremorgin C
Add to Clipboard
SYNONYMS FTC
SM-Q
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Mycotoxins
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-380-078 Revised 07-Apr-08
Josamycin
Add to Clipboard
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics for Cancer Research
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-078-M100   100 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C42H69NO15
MW: 828.0
CAS NUMBER: 16846-24-5
MERCK INDEX: 14: 5267
RTECS: OH4725810
SOURCE/HOST: Isolated from Streptomyces narbonenensis, var. josamyceticus nov. var.
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol, 100% ethanol, acetone, ethyl acetate, dioxane, or acidic water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C

Product Description
Macrolide antibiotic that may overcome anticancer drug resistance by inhibiting the binding of vinblastine (Prod. No. ALX-350-257) or cyclosporin A (Prod. No. ALX-380-002) to P-glycoprotein (Pgp).
Product Specific Literature References
A new antibiotic, josamyicn. I. Isolation and physico-chemical characteristics: T. Osono, et al.; J. Antibiot. (Tokyo) 20, 174 (1967) Abstract
Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo: L. Wang, et al.; Clin. Exp. Pharmacol. Physiol. 27, 587 (2000) Abstract
Kinetics of macrolide action: the josamycin and erythromycin cases: M. Lovmar, et al.; J. Biol. Chem. 279, 53506 (2004) Abstract
Further Categories Containing This Product:
MDR Inhibitors
 
 
ALX-270-307 Revised 08-Nov-06
JS-2190
Add to Clipboard
SYNONYMS Boc-Glu(OBzl)-N,N’-dicyclohexylurea
PRODUCT LINE Cancer
PRODUCT CATEGORY MDR Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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

Product Images
Please click on thumbnails to enlarge.
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-380-097 Revised 23-Apr-08
Mithramycin A
Add to Clipboard
SYNONYMS Mithracin
Aureolic acid
Aurelic acid
Plicamycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-097-M001   1 mg 30.00 USD Add To Cart
ALX-380-097-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C52H76O24
MW: 1085.2
CAS NUMBER: 18378-89-7
MERCK INDEX: 14: 7536
RTECS: PZ2800000
SOURCE/HOST: Isolated from Streptomyces argillaceus.
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description

Antineoplastic and immunosuppressive antibiotic. Inhibits transcription and protein synthesis. Substrate of P-glycoprotein (Pgp) in multidrug resistant (MDR) cancer cells. Binds to DNA in native chromatin. DNA-binding fluorescent dye.
Product Specific Literature References
Aureolic acid group of anti-tumour antibiotics: Y.U. Berlin, et al.; Nature 218, 193 (1968) Abstract
Chromomycin A3, mithramycin, and olivomycin: antitumor antibiotics of related structure: M. Slavik & S.K. Carter; Adv. Pharmacol. Chemother. 12, 1 (1975) Abstract
Mithramycin blocks protein binding and function of the SV40 early promoter: R. Ray, et al.; J. Clin. Invest. 83, 2003 (1989) Abstract; Full Text
Association of chromatin with anticancer antibiotics, mithramycin and chromomycin A3: M.A. Mir, et al.; Bioorg. Med. Chem. 11, 2791 (2003) Abstract
Tumor necrosis factor-alpha induces fractalkine expression preferentially in arterial endothelial cells and mithramycin A suppresses TNF-alpha-induced fractalkine expression: S.Y. Ahn, et al.; Am. J. Pathol. 164, 1663 (2004) Abstract; Full Text
Mithramycin A activates Fas death pathway in leukemic cell lines: I. Leroy, et al.; Apoptosis 11, 113 (2006) Abstract
Further Categories Containing This Product:
DNA Fragmentation & Chromatin Condensation • Antibiotics - Immunomodulators • MDR Inhibitors
 
 
ALX-340-021 Revised 04-Jun-08
MK-571 . sodium salt
Add to Clipboard
PRODUCT LINE Inflammation
PRODUCT CATEGORY Leukotrienes Other Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-021-M005   5 mg 45.00 USD Add To Cart
ALX-340-021-M025   25 mg 190.00 USD Add To Cart
Inquire
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-450-008 Revised 11-Mar-08
Nonactin
Add to Clipboard
SYNONYMS Polynactin
Werramycin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-450-008-M005   5 mg 40.00 USD Add To Cart
ALX-450-008-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C40H64O12
MW: 736.9
CAS NUMBER: 6833-84-7
MERCK INDEX: 14: 6675
RTECS: RH1685000
SOURCE/HOST: Isolated from Streptomyces griseus.
PURITY: ≥98% (Total homologs)
APPEARANCE: White to off-white solid.
PURITY DETAIL: Mixture of 2 homologs (~95% nonactin and ~5% monactin).
SOLUBILITY: Soluble in DMSO, dichloromethane, methanol, 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from moisture.
HAZARD: IRRITANT.

Product Description
Macrotetrolide