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ALX-270-039
Revised 15-Nov-06
A-3 . hydrochloride
SYNONYMS
N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide . HCl
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKA Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-039-M010
10 mg
65.00 USD
ALX-270-039-M050
50 mg
260.00 USD
Product Specification
FORMULA:
C
12
H
13
ClN
2
O
2
S . HCl
MW:
284.8 . 36.5
PURITY:
≥98%
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Inhibitor of cAMP- and cGMP-dependent protein kinase (PKA and PKG), protein kinase C (PKC), casein kinase I and II, and myosin light chain kinase.
Product Specific Literature References
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors:
M. Inagaki, et al.; Mol. Pharmacol.
29
, 577 (1986)
Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors
•
PKC Inhibitors
•
PKG Inhibitors
•
Casein Kinase Inhibitors
ALX-340-004
Revised 18-Aug-08
Arachidonic acid
SYNONYMS
5Z,8Z,11Z,14Z-Eicosatetraenoic acid
PRODUCT LINE
Inflammation
PRODUCT CATEGORY
Arachidonic Acid / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-340-004-M100
100 mg
147.00 USD
Product Specification
FORMULA:
C
20
H
32
O
2
MW:
304.5
CAS NUMBER:
506-32-1
MERCK INDEX:
14:
765
RTECS:
CE6675000
CONCENTRATION:
100mg/ml
PURITY:
≥98%
FORMULATION:
Liquid. Solution in ethanol containing 0.1% BHT.
SOLUBILITY:
100mg/ml soluble in DMSO or dimethyl formamide; sparingly soluble in basic aqueous buffers (1.7mg/ml). To prevent oxidation, the solvent should be purged with an inert gas.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stable for at least 6 months after receipt when stored at -20°C. Keep aqueous solutions on ice and use within 12 hours.
HANDLING:
Protect from light and oxygen.
HAZARD:
TOXIC.
Product Description
Precursor to a large family of eicosanoids. Activator for several protein kinase C (PKC) isotypes.
Product Specific Literature References
Arachidonic acid metabolism:
P. Needleman, et al.; Ann. Rev. Biochem.
55
, 69 (1986)
Abstract
Kinetic analysis of the Ca2+-dependent, membrane-bound, macrophage phospholipase A2 and the effects of arachidonic acid:
M.D. Lister, et al.; J. Biol. Chem.
263
, 7506 (1988)
Abstract
;
Full Text
Characterization of the L-arginine:nitric oxide pathway in human platelets:
M.W. Radomski, et al.; Br. J. Pharmacol.
101
, 325 (1990)
Abstract
The LDL receptor pathway delivers arachidonic acid for eicosanoid formation in cells stimulated by platelet-derived growth factor:
A.J.R. Habenicht, et al.; Nature
345
, 634 (1990)
Abstract
The control of free arachidonic acid levels:
R.D. Burgoyne & A. Morgan; TIBS
15
, 365 (1990)
Abstract
A unique pool of free arachidonate serves as substrate for both cyclooxygenase and lipoxygenase in platelets:
F. Chevy, et al.; Lipids
26
, 1080 (1991)
Abstract
Regulation of Ras-GAP and the neurofibromatosis-1 gene product by eicosanoids:
J.W. Han, et al.; Science
252
, 576 (1991)
Abstract
Arachidonic acid as a second messenger. Interactions with a GTP-binding protein of human neutrophils:
S.B. Abramson, et al.; J. Immunol.
147
, 231 (1991)
Abstract
The immediate activator of the NADPH oxidase is arachidonate not phosphorylation:
Henderson, et al.; Eur. J. Biochem.
211
, 157 (1993)
Abstract
Nitric oxide and arachidonic acid modulation of calcium currents in postganglionic neurones of avian cultured ciliary ganglia:
G. Khurana & M.R. Bennett; Br. J. Pharmacol.
109
, 480 (1993)
Abstract
Arachidonic acid-induced Ca2+ release from isolated sarcoplasmic reticulum:
C. Dettbarn & P. Palade; Biochem. Pharmacol.
45
, 1301 (1993)
Abstract
Covalent binding of arachidonate to G protein alpha subunits of human platelets:
H. Hallak, et al.; J. Biol. Chem.
269
, 4713 (1994)
Abstract
;
Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION
To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
PKC Activators
•
Nitric Oxide Pathway Other Products
•
Fatty Acids
ALX-450-014
Revised 22-Feb-08
BAPTA/AM
SYNONYMS
1,2-
bis
(2-Aminophenoxy)ethane-N,N,N',N'-tetraacetic acid
tetrakis
(acetoxymethyl) ester
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calcium Chelators / Caged Calcium Chelators
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-450-014-M010
10 mg
48.00 USD
ALX-450-014-M050
50 mg
195.00 USD
Product Specification
FORMULA:
C
34
H
40
N
2
O
18
MW:
764.7
CAS NUMBER:
126150-97-8
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO (10mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Packaged under inert gas. Protect from light and moisture.
HAZARD:
IRRITANT.
IDENTITY:
Determined by
1
H-NMR.
Product Description
Cell permeable acetoxymethyl ester derivative of BAPTA (Prod. No.
ALX-450-013
). Useful for controlling intracellular Ca
2+
concentration. Induces inactivation of protein kinase C. Also inhibits thapsigargin-induced apoptosis in rat thymocytes.
Product Specific Literature References
Physiological [Ca2+]i level and pump-leak turnover in intact red cells measured using an incorporated Ca chelator:
V.L. Lew, et al.; Nature
298
, 478 (1982)
Abstract
BAPTA induces a decrease of intracellular free calcium and a translocation and inactivation of protein kinase C in macrophages:
P. Dieter, et al.; Biol. Chem. Hoppe-Seyler
374
, 171 (1993)
Abstract
Intracellular calcium chelator, BAPTA-AM, prevents cocaine-induced ventricular fibrillation:
G.E. Billman; Am. J. Physiol.
265
, H1529 (1993)
Abstract
Intracellular Ca2+ signals activate apoptosis in thymocytes: studies using the Ca(2+)-ATPase inhibitor thapsigargin:
S. Jiang, et al.; Exp. Cell. Res.
212
, 84 (1994)
Abstract
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells:
T. Bouschet, et al.; J. Biol. Chem.
278
, 4778 (2003)
Abstract
;
Full Text
Further Categories Containing This Product:
PKC Inhibitors
•
Apoptosis Inducers & Inhibitors Other Products
•
Nuclear Envelope & Nuclear Transport
ALX-270-049
Revised 13-Nov-06
Bisindolylmaleimide I
SYNONYMS
GF-109203X
Gö 6850
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKC Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-049-M001
1 mg
45.00 USD
ALX-270-049-M005
5 mg
150.00 USD
Product Specification
FORMULA:
C
25
H
24
N
4
O
2
MW:
412.5
CAS NUMBER:
133052-90-1
PURITY:
≥98%
APPEARANCE:
Orange solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
MAY BE CARCINOGENIC. HARMFUL.
Product Description
Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (K
i
=10nM) over several serine/threonine and tyrosine kinases as compared to staurosporine (Prod. No.
ALX-380-014
). Acts as a competetive inhibitor for the ATP-binding site of PKC. Also inhibits telomerase activity in quercetin (Prod. No.
ALX-385-001
), H-89 (Prod. No.
ALX-270-017
), or herbimycin A (Prod. No.
ALX-350-029
) treated NPC-076 cells. Inhibits protein kinase A at much higher concentrations (K
i
=2µM).
Product Specific Literature References
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C:
D. Toullec, et al.; J. Biol. Chem.
266
, 15771 (1991)
Abstract
;
Full Text
Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model:
S. Kuchera, et al.; Agents Actions
39
, C169 (1993)
Abstract
The bisindolylmaleimide GF 109203X, a selective inhibitor of protein kinase C, does not inhibit the potentiating effect of phorbol ester on ethanol-induced phospholipase C-mediated hydrolysis of phosphatidylethanolamine:
Z. Kiss, et al.; Biochim. Biophys. Acta
1265
, 93 (1995)
Abstract
Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance
:
V. Gekeler, et al.; Br. J. Cancer
74
, 897 (1996)
Abstract
Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture
:
W.C. Ku, et al.; Biochem. Biophys. Res. Commun.
241
, 730 (1997)
Abstract
Suprabasin, a Novel Epidermal Differentiation Marker and Potential Cornified Envelope Precursor
:
G.T. Park, et al.; JBC
277
, 45195 (2002)
Abstract
;
Full Text
ALX-270-019
Revised 27-Apr-06
Bisindolylmaleimide I . hydrochloride
SYNONYMS
GF-109203X . HCl
Gö 6850 . HCl
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKC Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-019-M001
1 mg
45.00 USD
ALX-270-019-M005
5 mg
150.00 USD
Product Specification
FORMULA:
C
25
H
24
N
4
O
2
. HCl
MW:
412.5 . 36.5
PURITY:
≥98%
APPEARANCE:
Orange to red powder.
SOLUBILITY:
Soluble in DMSO or methanol. Slightly soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Water soluble form of bisindolylmaleimide I (Prod. No.
ALX-270-049
), a protein kinase C (PKC) inhibitor.
Product Specific Literature References
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C:
D. Toullec, et al.; J. Biol. Chem.
266
, 15771 (1991)
Abstract
;
Full Text
Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model:
S. Kuchera, et al.; Agents Actions
39
, C169 (1993)
Abstract
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells:
T. Bouschet, et al.; J. Biol. Chem.
278
, 4778 (2003)
Abstract
;
Full Text
ALX-270-050
Revised 26-May-08
Bisindolylmaleimide II
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKC Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-050-M001
1 mg
45.00 USD
ALX-270-050-M005
5 mg
150.00 USD
Product Specification
FORMULA:
C
27
H
26
N
4
O
2
MW:
438.5
PURITY:
≥97% (mixture of 2 isomers)
APPEARANCE:
Orange solid.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
ALX-270-051
Revised 18-Jan-08
Bisindolylmaleimide III
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKC Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-051-M001
1 mg
45.00 USD
ALX-270-051-M005
5 mg
150.00 USD
Product Specification
FORMULA:
C
23
H
20
N
4
O
2
MW:
384.4
PURITY:
≥98%
APPEARANCE:
Red solid.
SOLUBILITY:
Soluble in methanol or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Potent and selective inhibitor of protein kinase C (PKC).
Product Specific Literature References
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C:
D. Toullec, et al.; J. Biol. Chem.
266
, 15771 (1991)
Abstract
;
Full Text
Protein kinase C inhibitors; structure-activity relationships in K252c- related compounds:
S. Fabre and M. Prudhomme; Bioorg. Med. Chem.
1
, 193 (1993)
Abstract
Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides:
P.D. Davis, et al.; J. Med. Chem.
35
, 177 (1992)
Abstract
Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors:
D. Brehmer, et al.; Mol. Cell Proteomics
3
, 490 (2004)
Abstract
;
Full Text
ALX-270-052
Revised 05-Oct-06
Bisindolylmaleimide IV
SYNONYMS
Ro 31-6233
Arcyriarubin A
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKC Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-052-M001
1 mg
45.00 USD
ALX-270-052-M005
5 mg
150.00 USD
Product Specification
FORMULA:
C
20
H
13
N
3
O
2
MW:
327.3
CAS NUMBER:
119139-23-0
PURITY:
≥98%
APPEARANCE:
Red solid.
SOLUBILITY:
Soluble in DMSO or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Specific Literature References
D. Toullec, et al.; J. Biol. Chem.
266
, 15771 (1991)
Abstract
;
Full Text
Protein kinase C inhibitors; structure-activity relationships in K252c- related compounds:
S. Fabre & M. Prudhomme; Bioorg. Med. Chem.
1
, 193 (1993)
Abstract
Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides:
P.D. Davis, et al.; J. Med. Chem.
35
, 177 (1992)
Abstract
ALX-270-053
Revised 29-Jul-05
Bisindolylmaleimide V
SYNONYMS
Ro 31-6045
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKC Negative Controls
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-053-M001
1 mg
45.00 USD
ALX-270-053-M005
5 mg
150.00 USD
Product Specification
FORMULA:
C
21
H
15
N
3
O
2
MW:
341.4
CAS NUMBER:
113963-68-1
PURITY:
≥98%
APPEARANCE:
Red solid.
SOLUBILITY:
Soluble in DMSO or methanol; very slightly soluble in 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Negative control for the protein kinase C (PKC)-inhibitory activity.
Product Specific Literature References
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C:
D. Toullec, et al.; J. Biol. Chem.
266
, 15771 (1991)
Abstract
;
Full Text
Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides:
P.D. Davis, et al.; J. Med. Chem.
35
, 177 (1992)
Abstract
ALX-270-054
Revised 07-Dec-04
Bisindolylmaleimide VI
PRODUCT LINE
Signal Transduction
