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Ras Signalling Pathway
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ALX-350-019 Revised 16-Oct-08
(+)-Brefeldin A
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SYNONYMS BFA
Ascotoxin
Decumbin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-019-M005   5 mg 80.00 USD Add To Cart
ALX-350-019-M010   10 mg 130.00 USD Add To Cart
ALX-350-019-M025   25 mg 270.00 USD Add To Cart
ALX-350-019-M050   50 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C16H24O4
MW: 280.4
CAS NUMBER: 20350-15-6
MERCK INDEX: 14: 1369
SOURCE/HOST: Isolated from Eupenicillium brefeldianum.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, methanol, acetone or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Inhibitor of intracellular protein transport and protein secretion, interfering with trafficking in the trans-Golgi network, leading to the accumulation of cycling proteins in ERGIC clusters. Blocks ADP-ribosylation factor (Arf) in an inactive GDP-bound conformation and thereby prevents binding of COPI coats to ERGIC and Golgi membranes. Upon brefeldin A treatment the Golgi rapidly tubulates and fuses with the ER by an energy-, temperature-, and microtubule-dependent process. In contrast, the drug has little effect on the ERGIC, which keeps its identity, although the ERGIC clusters become larger and more uniformly distributed in the cytoplasm of the cells. Inhibits intracellular collagen degradation. Also inhibits apical Na+ channels in epithelia. Induces apoptosis.
Product Specific Literature References
Decumbin, a new compound from a species of Penicillium: V.L. Singleton, et al.; Nature 181, 1072 (1958)
Über die Isolierung neuer Stoffwechselprodukte aus Penicillium brefeldianum Dodge.: E. Harri, et al.; Helv. Chim. Acta 46, 1235 (1963)
Novel blockade by brefeldin A of intracellular transport of secretory proteins in cultured rat hepatocytes: Y. Misumi, et al.; J. Biol. Chem. 261, 11398 (1986) Abstract; Full Text
Brefeldin A causes disassembly of the Golgi complex and accumulation of secretory proteins in the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 263, 18545 (1988) Abstract; Full Text
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Brefeldin A and the endocytic pathway. Possible implications for membrane traffic and sorting: W. Hunziker, et al.; FEBS Lett. 307, 93 (1992), (Review) Abstract
Brefeldin A inhibits degradation as well as production and secretion of collagen in human lung fibroblasts: C.R. Ripley, et al.; J. Biol. Chem. 268, 3677 (1993) Abstract
Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53: R.G. Shao, et al.; Exp. Cell Res. 227, 190 (1996) Abstract
Brefeldin A inhibition of apical Na+ channels in epithelia: R.S. Fisher, et al.; Am. J. Physiol. 270, C138 (1996) Abstract
Brefeldin A: deciphering an enigmatic inhibitor of secretion: A. Nebenfuhr, et al.; Plant Physiol. 130, 1102 (2002), Review Abstract
NKT cells provide help for dendritic cell-dependent priming of MHC class I-restricted CD8+ T cells in vivo: D. Stober, et al.; J. Immunol. 170, 2540 (2003) Abstract; Full Text
Interaction of BIG2, a brefeldin A-inhibited guanine nucleotide-exchange protein, with exocyst protein Exo70: K.F. Xu, et al.; PNAS 102, 2784 (2005) Abstract
Further Categories Containing This Product:
ADP Ribosylation Factor [ARF] / Related Products • Golgi Apparatus • Collagen / Related Products • Na+ Channels • Antitumor Antibiotics • Antibiotics - Antiviral / Anti-HIV • Antitumor Agents (Apoptosis Inducers) • Antibiotics - Antifungal • Autophagy Other Products
 
 
ALX-350-240 Revised 05-Dec-07
Ilimaquinone
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SYNONYMS 3-[(Decahydro-1β,2β,4αβ-trimethyl-5-methylene-1-naphthyl)methyl]-2-hydroxy-5-methoxybenzoquinone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-240-C100   100 µg 140.00 USD Add To Cart
Product Specification
FORMULA: C22H30O4
MW: 358.5
CAS NUMBER: 71678-03-0
PURITY: ≥98%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Displays antimicrobial, anti-HIV and anti-inflammatory properties. Induces reversible breakdown of Golgi membranes. Inhibits the association of β-COP and ADP-ribosylation factor to Golgi membranes. Interacts with methylation enzymes. Shows anticancer activity.
Product Specific Literature References
R.T. Luibrand, et al.; Tetrahedron 35, 609 (1979)
Complete vesiculation of Golgi membranes and inhibition of protein transport by a novel sea sponge metabolite, ilimaquinone: P.A. Takizawa, et al.; Cell 73, 1079 (1993) Abstract
Interactions of (-)-ilimaquinone with methylation enzymes: implications for vesicular-mediated secretion: H.S. Radeke, et al.; Chem. Biol. 6, 639 (1999) Abstract
Ilimaquinone inhibits gap-junctional communication prior to Golgi fragmentation and block in protein transport: V. Cruciani, et al.; Exp. Cell Res. 287, 130 (2003) Abstract
Natural products with anti-HIV activity from marine organisms: L.A. Tziveleka, et al.; Curr. Top. Med. Chem. 3, 1512 (2003), Review Abstract
Interaction of the smooth endoplasmic reticulum and mitochondria: J.G. Goetz & I.R. Nabi; Biochem. Soc. Trans. 34, 370 (2006), Review Abstract
Ilimaquinone, a marine sponge metabolite, displays anticancer activity via GADD153-mediated pathway: P.H. Lu, et al.; Eur. J. Pharmacol. 556, 45 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Anti-inflammatory Agents • Golgi Apparatus • ADP Ribosylation Factor [ARF] / Related Products • Natural Products - Chemopreventive Agents • Natural Products - Antiviral / anti-HIV Agents • PRMTs, Mono- & Dimethylarginine / Related Products • Marine Natural Products
 
 
ALX-270-064 Revised 14-Jul-03
Chaetomellic acid A . disodium salt
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-270-064-M001   1 mg 30.00 USD Add To Cart
ALX-270-064-M005   5 mg 70.00 USD Add To Cart
ALX-270-064-M010   10 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C19H32O4. 2Na
MW: 324.5 . 46.0
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in warm water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent inhibitor of farnesyltransferase in isolated enzyme assays but is inactive in whole cells. Inhibition of farnesyltransferase is selective over geranylgeranyltransferase I and II.
Product Specific Literature References
Selective inhibition of farnesyl-protein transferase blocks ras processing in vivo: J.B. Gibbs, et al.; J. Biol. Chem. 268, 7617 (1993) Abstract; Full Text
Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review) Abstract
 
 
ALX-270-111 Revised 31-Jul-08
Patulin
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SYNONYMS 4-Hydroxy-4H-furo[3,2-c]pyran-2(6H)-one
Clairformin
Clavacin
Clavatin
Claviformin
Leucopin
Mycoin C3
Mycosin
Penicidin
Terinin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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ALX-270-111-M001   1 mg 20.00 USD Add To Cart
ALX-270-111-M005   5 mg 80.00 USD Add To Cart
ALX-270-111-M025   25 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C7H6O4
MW: 154.1
CAS NUMBER: 149-29-1
MERCK INDEX: 14: 7053
RTECS: LV2625000
SOURCE/HOST: Isolated from Penicillium expansum.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water, 100% ethanol, ethyl acetate or DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE CARCINOGENIC. TOXIC.

Product Description
Inhibitor of protein farnesylation in a cell free assay. Inhibits incorporation of tritiated mevalonate into proteins in whole cells. Mycotoxin with anti-bacterial, potassium uptake inhibitory and possibly carcinogenic activities. Known contaminant of spoiled apples.
Product Specific Literature References
M. Birkinshaw, et al.; Lancet 245, 625 (1943)
J. Kahn; J. Pharmacol. Exp. Ther. 121, 234 (1957)
IARC Monographs 10, 205 (1976)
Chronology of patulin-induced alterations in membrane function of cultured renal cells, LLC-PK: R.T. Riley, et al.; Toxicol. Appl. Pharmacol. 102, 128 (1990) Abstract
Inhibition of protein prenylation by patulin: S. Miura, et al.; FEBS Lett. 318, 88 (1993) Abstract
Aneuploidogenic and clastogenic potential of the mycotoxins citrinin and patulin: E. Pfeiffer, et al.; Carcinogenesis 19, 1313 (1998) Abstract
Hplc detection of patulin in apple juice with GC/MS confirmation of patulin identity: J.A. Roach, et al.; Adv. Exp. Med. Biol. 504, 135 (2002), Review Abstract
Further Categories Containing This Product:
Mycotoxins • Farnesylation / Isoprenylation Reagents
 
 
ALX-290-001 Revised 29-Nov-04
N-Acetyl-S-farnesyl-L-cysteine
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SYNONYMS AFC
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-001-M005   5 mg 50.00 USD Add To Cart
ALX-290-001-M025   25 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C20H33NO3S
MW: 367.6
CAS NUMBER: 135304-07-3
PURITY: ≥97%
APPEARANCE: Clear oil.
SOLUBILITY: Soluble in DMSO, methanol or ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Specific inhibitor of S-farnesylcysteine methyl transferase.
Related Products
 
 
ALX-290-003 Revised 30-Jun-08
Farnesylpyrophosphate . triammonium salt
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SYNONYMS FPP . 3NH4
3,7,11-Trimethyl-2,6,10-dodecatrien-1-ol pyrophosphate . 3NH4
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-003-C200   200 µg 62.00 USD Add To Cart
Product Specification
FORMULA: C15H25O7P2 . 3NH4
MW: 379.3 . 54.1
CAS NUMBER: 13058-04-3
PURITY: ≥98% (TLC)
APPEARANCE: Liquid. Solution in 0.25M ammonium bicarbonate containing 70% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY:

Store solutions at -20°C for up to 3 months.
HANDLING: Protect from light and moisture.

Product Description
Farnesyl donor in enzymatic protein farnesylation catalyzed by farnesyltransferase.
Product Specific Literature References
Tautomycin from the bacterium Streptomyces verticillatus. Another potent and specific inhibitor of protein phosphatases 1 and 2A: C. MacKintosh & S. Klumpp; FEBS Lett. 277, 137 (1990) Abstract
M. Ubukata, et al.; J. C. S. Chem. Commun. 244 (1990)
Divalent cation and prenyl pyrophosphate specificities of the protein farnesyltransferase from rat brain, a zinc metalloenzyme: Y. Reiss, et al.; J. Biol. Chem. 267, 6403 (1992) Abstract; Full Text
Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review) Abstract
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic: J.B. Gibbs, et al.; Cell 77, 175 (1994) Abstract
 
 
ALX-290-004 Revised 25-Oct-06
Farnesylthioacetic acid
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SYNONYMS FTA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-004-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C17H28O2S
MW: 296.5
CAS NUMBER: 135784-48-4
PURITY: ≥98%
APPEARANCE: Yellow viscous oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions are stable for up to 6 months when stored at -20°C. Product is not sterile.
HANDLING: Protect from light.

Product Description
Potent and specific inhibitor of methyl esterification of farnesylated proteins (e.g. the γ subunit of transducin). This compound is not a methyltransferase substrate.
Product Specific Literature References
Identifying the recognition unit for G protein methylation: E.W. Tan, et al.; J. Biol. Chem. 266, 10719 (1991) Abstract; Full Text
 
 
ALX-290-009 Revised 02-Apr-04
α-Hydroxyfarnesylphosphonic acid
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-009-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C15H27O4P
MW: 302.4
PURITY: ≥96%
FORMULATION: Liquid. 1mg dissolved in 500µl ethanol.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Product decomposes rapidly when not in solution. Do not evaporate to dryness.

Product Description
Potent inhibitor of farnesyltransferase in cell-free enzyme preparations (IC50=30nM) and in whole cells. Selectively inhibits farnesyltransferase over geranylgeranyltransferases I and II (IC50=35.8µM and IC50=67.0µM).
Product Specific Literature References
Steady-state kinetic mechanism of Ras farnesyl:protein transferase: D.L. Pompliano, et al.; Biochemistry 31, 3800 (1992) Abstract
Selective inhibition of farnesyl-protein transferase blocks ras processing in vivo: J.B. Gibbs, et al.; J. Biol. Chem. 268, 7617 (1993) Abstract; Full Text
Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review) Abstract
 
 
ALX-290-010 Revised 20-Apr-07
N-Acetyl-S-farnesyl-L-cysteine-methyl ester
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SYNONYMS AFCME
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-010-M010   10 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C21H35NO3S
MW: 381.6
CAS NUMBER: 135304-08-4
PURITY: ≥95%
APPEARANCE: White to slightly yellow powder.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.

Product Description
Substrate for studying the reversibility of carboxyl methylation in signal-transducing G-proteins.
Product Specific Literature References
Methylation and demethylation reactions of guanine nucleotide-binding proteins of retinal rod outer segments: D. Pérez-Sala, et al.; PNAS 88, 3043 (1991) Abstract
Identifying the recognition unit for G protein methylation: E.W. Tan, et al.; J. Biol. Chem. 266, 10719 (1991) Abstract; Full Text
 
 
ALX-350-241 Revised 07-Dec-07
Manumycin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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ALX-350-241-M001   1 mg 58.00 USD Add To Cart
ALX-350-241-M005   5 mg 170.00 USD Add To Cart
ALX-350-241-M010   10 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C31H38N2O7
MW: 550.7
CAS NUMBER: 52665-74-4
SOURCE/HOST: Isolated from Streptomyces parvulus.
PURITY: ≥96% (HPLC)
APPEARANCE: Yellow to brown powder.
SOLUBILITY: Soluble in methanol or DMSO; insoluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR.