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ADP Ribosylation Factor [ARF] / Related Products
Farnesylation / Isoprenylation Reagents
Geranyl-related Reagents
GTPase-activating Proteins [GAPs]
Guanine-nucleotide Exchange Factors [GEFs]
Rab / Related Products
Raf / Related Products
Ras / Related Products
Rho / Related Products
Rho-associated Protein Kinases [ROCK] / Related Products
Shc & Other Ras Adaptors / Related Products
Ras Signalling Pathway Other Products
ALX-290-001
Revised 29-Nov-04
N-Acetyl-S-farnesyl-L-cysteine
SYNONYMS
AFC
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
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ALX-290-001-M005
5 mg
50.00 USD
ALX-290-001-M025
25 mg
150.00 USD
Product Specification
FORMULA:
C
20
H
33
NO
3
S
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-290-007
N-Acetyl-S-geranyl-L-cysteine
ALX-290-010
Revised 20-Apr-07
N-Acetyl-S-farnesyl-L-cysteine-methyl ester
SYNONYMS
AFCME
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
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ALX-290-010-M010
10 mg
40.00 USD
Product Specification
FORMULA:
C
21
H
35
NO
3
S
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-290-007
Revised 02-Jun-08
N-Acetyl-S-geranyl-L-cysteine
SYNONYMS
AGC
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Geranyl-related Reagents
Ordering Information
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Format:
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ALX-290-007-M005
5 mg
90.00 USD
Product Specification
FORMULA:
C
15
H
25
NO
3
S
MW:
299.4
PURITY:
≥98% (TLC)
APPEARANCE:
Clear to pale yellow viscous oil.
SOLUBILITY:
> 25mg/ml soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Solutions may be stored at -20 °C for up to 3 months. Product is not sterile.
Product Description
Negative control for AFC (Prod. No.
ALX-290-001
)
and AGGC (Prod. No.
ALX-290-008
)
. Has a closely similar structure to these two compounds but lacks their biological activity.
Related Products
ALX-290-001
N-Acetyl-S-farnesyl-L-cysteine
ALX-290-008
N-Acetyl-S-geranylgeranyl-L-cysteine
ALX-290-008
Revised 13-Jul-06
N-Acetyl-S-geranylgeranyl-L-cysteine
SYNONYMS
AGGC
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Geranyl-related Reagents
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ALX-290-008-M005
5 mg
140.00 USD
Product Specification
FORMULA:
C
25
H
41
NO
3
S
MW:
435.7
CAS NUMBER:
139332-94-8
PURITY:
≥98%
APPEARANCE:
Viscous yellow oil.
SOLUBILITY:
Soluble in 100% ethanol or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Specifically blocks methyl esterification of geranylgeranylated proteins such as Rab proteins. Blocks receptor-mediated signal transduction in human neutrophils (IC
50
=4µM). Induces insulin release from HIT-T15 cells by mimicking the action of Rab3A. Inhibits β2-integrin-induced actin polymerization (IC
50
~45nM) in neutrophils.
Related Products
ALX-290-007
N-Acetyl-S-geranyl-L-cysteine
ALX-350-019
Revised 16-Oct-08
(+)-Brefeldin A
SYNONYMS
BFA
Ascotoxin
Decumbin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-350-019-M005
5 mg
80.00 USD
ALX-350-019-M010
10 mg
130.00 USD
ALX-350-019-M025
25 mg
270.00 USD
ALX-350-019-M050
50 mg
420.00 USD
Product Specification
FORMULA:
C
16
H
24
O
4
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-208-002
Revised 03-Nov-08
C3 Exoenzyme
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
ADP Ribosylation Factor [ARF] / Related Products
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ALX-208-002-C010
10 µg
160.00 USD
ALX-208-002-C050
50 µg
390.00 USD
Product Specification
SOURCE/HOST:
Isolated from
Clostridium botulinum
.
CONCENTRATION:
1mg/ml after reconstitution.
PURITY:
≥95% (SDS-PAGE)
APPEARANCE:
Lyophilized from 5mM HEPES, pH 8.0.
RECONSTITUTION:
Reconstitute with 10µl/50µl distilled water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
After reconstitution, prepare aliquots and store at -20°C. Avoid freeze/thaw cycles.
Product Description
Exhibits ADP-ribosyltransferase activity. Not neurotoxic. Not cell permeable. The substrate for C3 exoenzyme has been identified as Rho, a GTP-binding Ras-related protein. Rac proteins are approximately 100-fold less active as substrates. The ADP-ribosylation site of exoenzyme C3 on rho A has been identified as Asn
41
.
Product Specific Literature References
ADP-ribosylation of platelet actin by botulinum C2 toxin:
K. Aktories, et al.; Eur. J. Biochem.
161
, 155 (1986)
Abstract
K. Aktories, et al.; TIPS
8
, 158 (1987)
Clostridium botulinum type C produces a novel ADP-ribosyltransferase distinct from botulinum C2 toxin:
K. Aktories, et al.; FEBS Lett.
212
, 109 (1987)
Abstract
Botulinum C2 toxin ADP-ribosylates actin and disorganizes the microfilament network in intact cells
:
K.H. Reuner, et al.; Eur. J. Cell Biol.
43
, 134 (1987)
Abstract
Botulinum ADP-ribosyltransferase C3. Purification of the enzyme and characterization of the ADP-ribosylation reaction in platelet membranes:
K. Aktories, et al.; Eur. J. Biochem.
172
, 445 (1988)
Abstract
Functional modification of a 21-kilodalton G protein when ADP- ribosylated by exoenzyme C3 of Clostridium botulinum:
E.J. Rubin, et al.; Mol. Cell Biol.
8
, 418 (1988)
Abstract
The rho gene product expressed in E. coli is a substrate of botulinum ADP-ribosyltransferase C3:
K. Aktories, et al.; BBRC
158
, 209 (1989)
Abstract
K. Aktories and A. Hall; TIPS
10
, 415 (1989)
Abstract
The mammalian G protein rhoC is ADP-ribosylated by Clostridium botulinum exoenzyme C3 and affects actin microfilaments in Vero cells:
P. Chardin, et al.; EMBO J.
8
, 1087 (1989)
Abstract
Asparagine residue in the rho gene product is the modification site for botulinum ADP-ribosyltransferase
:
A. Sekine, et al.; J. Biol. Chem.
264
, 8602 (1989)
Abstract
;
Full Text
Microinjection of recombinant p21rho induces rapid changes in cell morphology:
H.F. Paterson, et al.; J. Cell. Biol.
111
, 1001 (1990)
Abstract
Characterization of the C3 gene of Clostridium botulinum types C and D and its expression in Escherichia coli:
A. Popoff, et al.; Infect. Immun.
59
, 3673 (1991)
Abstract
The ras protein family: evolutionary tree and role of conserved amino acids:
A. Valencia, et al.; Biochemistry
30
, 4637 (1991)
Abstract
ADP-ribosylation of the ras-related, GTP-binding protein RhoA inhibits lymphocyte-mediated cytotoxicity:
P. Lang, et al.; J. Biol. Chem.
267
, 11677 (1992)
Abstract
;
Full Text
A rho gene product in human blood platelets. II. Effects of the ADP- ribosylation by botulinum C3 ADP-ribosyltransferase on platelet aggregation:
N. Morii, et al.; J. Biol. Chem.
267
, 20921 (1992)
Abstract
;
Full Text
The small GTP-binding protein rho regulates the assembly of focal adhesions and actin stress fibers in response to growth factors:
A.J. Ridley, et al.; Cell
70
, 389 (1992)
Abstract
Involvement of rho p21 and its inhibitory GDP/GTP exchange protein (rho GDI) in cell motility:
K. Takaishi, et al.; Mol. Cell. Biol.
13
, 72 (1993)
Abstract
Effect of botulinum C3 exoenzyme on cell growth and cytoskeleton organization in transformed human epidermal cells in culture: a possible role for rho protein in epidermal cells:
M. Yamamoto, et al.; J. Dermatol. Sci.
8
, 103 (1994)
Abstract
General Information
All proteins encoded by the superfamily of ras genes are structurally related, bind GTP and exhibit GTPase activity which is regulated by divalent cations. In human cells, three slight variations of the Rho protein (Rho A, B and C, respectively) have been described.
BACKGROUND/TECHNICAL INFORMATION
APD-ribosylation is performed as described by Chardin et al. Target G proteins or subcellular fractions corresponding to 50-70µg protein are incubated for 1 hour at 37°C with 20-30ng of C3 in a 10mM HEPES buffer, pH 8.0 containing, 15mM isonicotinic acid hydrazide, 15mM thymidine, 1mM MgCl
2
, 1mM ATP, 2µM [
32
P]NAD. The reaction is stopped by addition of 0.06M TRIS-HCl, pH 7.0, 15% (v/v) glycerol, 5% β-mercaptoethanol, 2.3% SDS and 0.001% bromophenol blue. The mixture may then be subjected to SDS-PAGE.
Further Categories Containing This Product:
Enzymes
•
Natural Proteins
ALX-270-064
Revised 14-Jul-03
Chaetomellic acid A . disodium salt
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
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ALX-270-064-M001
1 mg
30.00 USD
ALX-270-064-M005
5 mg
70.00 USD
ALX-270-064-M010
10 mg
130.00 USD
Product Specification
FORMULA:
C
19
H
32
O
4
. 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-480-093
Revised 07-Feb-08
8-(4-Chlorophenylthio)-2'-O-methyladenosine 3',5'-cyclic Monophosphate . sodium salt
SYNONYMS
8-CPT-2'-O-Me-cAMP . Na
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cAMP Derivatives
Ordering Information
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ALX-480-093-M001
1 mg
130.00 USD
ALX-480-093-M005
5 mg
520.00 USD
Product Specification
FORMULA:
C
17
H
16
ClN
5
O
6
PS . Na
MW:
484.8 . 23.0
CAS NUMBER:
510774-50-2
PURITY:
≥98% (HPLC)
PURITY DETAIL:
Product is not sterile.
FORMULATION:
White to off-white powder.
SOLUBILITY:
Soluble in water, aqueous buffers, DMSO, dimethyl formamide or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Hygroscopic.
IDENTITY:
Determined by
1
H-NMR, MS and UV (λ
max
: 282nm, ε: 16’000, pH 7).
Product Description
Specific, potent and membrane permeant activator of the Epac cAMP receptor. Activates Epac1 and Epac2, the guanine nucleotide-exchange factors (GEFs) for the small GTPases Rap1 and Rap2. Does not activate protein kinase A (PKA), neither
in vitro
nor
in vivo
and is therefore a valuable tool to specifically discriminate between PKA- and Epac-mediated effects. Since a free 2'-ribose hydroxyl group in cyclic AMP is essential for stimulation of PKA, the methylated structure of 8-CPT-2'-O-Me-cAMP is an extremely poor PKA activator. Its high lipophilicity allows for good membrane permeability in most biosystems and its increased resistance towards phosphodiesterases prevents rapid hydrolysis.
Product Specific Literature References
A novel Epac-specific cAMP analogue demonstrates independent regulation of Rap1 and ERK
:
J.M. Enserink, et al.; Nat. Cell Biol.
4
, 901 (2002)
Abstract
;
Full Text
Epac-selective cAMP analog 8-pCPT-2'-O-Me-cAMP as a stimulus for Ca2+-induced Ca2+ release and exocytosis in pancreatic beta-cells
:
G. Kang, et al.; J. Biol. Chem.
278
, 8279 (2003)
Abstract
;
Full Text
Cyclic AMP induces integrin-mediated cell adhesion through Epac and Rap1 upon stimulation of the {beta}2-adrenergic receptor
:
S. Rangarajan, et al.; J. Cell Biol.
160
, 487 (2003)
Abstract
General Literature References
Signal transduction. New exchange, new target
:
J. Downward; Nature
396
, 416 (1998), Comment
Abstract
Epac is a Rap1 guanine-nucleotide-exchange factor directly activated by cyclic AMP
:
J. de Rooij, et al.; Nature
396
, 474 (1998)
Abstract
A family of cAMP-binding proteins that directly activate Rap1
:
H. Kawasaki, et al.; Science
282
, 2275 (1998)
Abstract
Further Categories Containing This Product:
PKA Activators
•
Guanine-nucleotide Exchange Factors [GEFs]
ALX-260-021
Revised 17-Sep-02
H-Cys-4-Abz-Met-OH
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
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ALX-260-021-M001
1 mg
40.00 USD
ALX-260-021-M005
5 mg
160.00 USD
Product Specification
FORMULA:
C
15
H
21
N
3
O
4
S
2
MW:
371.5
PURITY:
≥92%
APPEARANCE:
White lyophilized powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Potent inhibitor of Ras farnesyltransferase.
Product Specific Literature References
Inhibitors of Ras Farnesyltransferase as Novel Antitumor Agents
:
A.D. Hamilton & S.M. Sebti; Drug News Perspect.
8
, 138 (1995)
ALX-290-002
Revised 13-Dec-04
S-Farnesylated Cysteine Tetrapeptide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
Ordering Information
Product Numbers:
Format:
Size:
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ALX-290-002-M001
1 mg
45.00 USD
ALX-290-002-M005
5 mg
150.00 USD
Product Specification
SEQUENCE:
Ac-Cys(farnesyl)-Val-Ile-Met-OH
FORMULA:
C
36
H
62
N
4
O
6
S
2
MW:
711.0
PURITY:
≥95%
APPEARANCE:
Yellow solid.
SOLUBILITY:
Soluble in chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Hygroscopic. Protect from light and oxygen.
Product Description
Tetrapeptide substrate for the protein endoprotease that cleaves the modified protein at the isoprenylated cysteine residue.
Product Specific Literature References
Inhibitors of the isoprenylated protein endoprotease:
Y.-T. Ma, et al.; Biochemistry
32
, 2386 (1993)
Abstract
ALX-290-003
Revised 30-Jun-08
Farnesylpyrophosphate . triammonium salt
SYNONYMS
FPP . 3NH
4
3,7,11-Trimethyl-2,6,10-dodecatrien-1-ol pyrophosphate . 3NH
4
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
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ALX-290-003-C200
200 µg
62.00 USD
Product Specification
FORMULA:
C
15
H
25
O
7
P
2
. 3NH
4
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
