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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
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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-480-085
Revised 05-Sep-07
Adenosine-3’,5’-cyclic Monophosphothioate, Rp-Isomer . sodium salt
SYNONYMS
Rp-cAMPS . Na
cAMPS . Na, Rp-Isomer
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cAMP Derivatives
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ALX-480-085-M001
1 mg
120.00 USD
ALX-480-085-M005
5 mg
490.00 USD
Product Specification
FORMULA:
C
10
H
11
N
5
NaO
5
PS
MW:
367.3
CAS NUMBER:
73208-40-9
PURITY:
≥99% (low adenosine, cAMP and Sp-cAMPS content)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water or aqueous buffers.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
For application and literature references see the triethylammonium salt (Prod. No.
ALX-480-012
).
Further Categories Containing This Product:
PKA Inhibitors
ALX-480-012
Revised 27-Apr-06
Adenosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . triethylammonium salt
SYNONYMS
Rp-cAMPS . TEA
cAMPS . TEA, Rp-Isomer
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cAMP Derivatives
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ALX-480-012-M001
1 mg
110.00 USD
ALX-480-012-M005
5 mg
460.00 USD
Product Specification
FORMULA:
C
10
H
12
N
5
O
5
PS . C
6
H
16
N
MW:
345.5 . 101.0
CAS NUMBER:
151837-09-1
PURITY:
≥99%
APPEARANCE:
White lyophilized solid.
SOLUBILITY:
Soluble in water
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Competitive inhibitor of protein cAMP-dependent protein kinase type I and II (cAMP antagonist). Resistant against mammalian cyclic nucleotide-dependent phosphodiesterases. Significantly more lipophilic as compared to cAMP and thus membrane permeable in many biological systems.
Product Specific Literature References
A mechanistic and kinetic analysis of the interactions of the diastereoisomers of adenosine 3',5'-(cyclic)phosphorothioate with purified cyclic AMP-dependent protein kinase:
J.D. Rothermel; Biochem. J.
251
, 757 (1988)
Abstract
Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3',5'-cyclic phosphorothioates:
W.R.G. Dostmann, et al.; J. Biol. Chem.
265
, 10484 (1990)
Abstract
;
Full Text
Inhibition of cGMP-dependent protein kinase by (Rp)-guanosine 3',5'- monophosphorothioates:
E. Butt, et al.; FEBS Lett.
263
, 47 (1990)
Abstract
Regulation of kainate receptors by cAMP-dependent protein kinase and phosphatases
:
L.Y. Wang, et al.; Science
253
, 1132 (1991)
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:
PKA Inhibitors
ALX-151-016
Revised 17-Jan-05
cAMP-dependent Protein Kinase Inhibitor (5-22) amide
SYNONYMS
PKA Inhibitor (5-22) amide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKA Inhibitors
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ALX-151-016-MC05
0.5 mg
110.00 USD
ALX-151-016-M001
1 mg
180.00 USD
Product Specification
SEQUENCE:
H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-NH
2
FORMULA:
C
84
H
137
N
29
O
26
MW:
1969.2
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Potent inhibitor of cAMP-dependent protein kinase (PKA).
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase:
H.-C. Cheng, et al.; J. Biol. Chem.
261
, 989 (1986)
Abstract
;
Full Text
Primary structural determinants essential for potent inhibition of cAMP- dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitor protein:
D.B. Glass, et al.; J. Biol. Chem.
264
, 8802 (1989)
Abstract
;
Full Text
Further Categories Containing This Product:
Peptides
ALX-151-014
Revised 15-Dec-04
cAMP-dependent Protein Kinase Inhibitor (5-24)
SYNONYMS
PKA Inhibitor (5-24)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKA Inhibitors
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ALX-151-014-MC05
0.5 mg
90.00 USD
ALX-151-014-M001
1 mg
160.00 USD
Product Specification
SEQUENCE:
H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-OH
FORMULA:
C
94
H
148
N
32
O
31
MW:
2222.4
PURITY:
≥97%
APPEARANCE:
White to off-white powder.
FORMULATION:
Lyophilized.
SOLUBILITY:
Soluble in water or 5 % acetic acid.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry.
Product Description
Potent inhibitor of cAMP-dependent protein kinase (PKA). The peptide corresponds to the active site of the skeletal muscle inhibitor protein.
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase:
H.-C. Cheng, et al.; J. Biol. Chem.
261
, 989 (1986)
Abstract
;
Full Text
Phosphorylation of Avena phytochrome in vitro as a probe of light- induced conformational changes:
Y.S. Wong, et al.; J. Biol. Chem.
261
, 12089 (1986)
Abstract
;
Full Text
Further Categories Containing This Product:
Peptides
ALX-151-018
Revised 13-Feb-06
cAMP-dependent Protein Kinase Inhibitor (5-24) amide
SYNONYMS
PKA Inhibitor (5-24) amide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKA Inhibitors
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ALX-151-018-MC05
0.5 mg
90.00 USD
ALX-151-018-M001
1 mg
160.00 USD
Product Specification
SEQUENCE:
H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-NH
2
FORMULA:
C
94
H
149
N
33
O
30
MW:
2221.4
PURITY:
≥97%
APPEARANCE:
White to off-white lyophilized powder.
SOLUBILITY:
Soluble in water or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase:
H.-C. Cheng, et al.; J. Biol. Chem.
261
, 989 (1986)
Abstract
;
Full Text
Further Categories Containing This Product:
Peptides
ALX-151-017
Revised 15-Dec-04
cAMP-dependent Protein Kinase Inhibitor (14-24) amide
SYNONYMS
PKA Inhibitor (14-24) amide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKA Inhibitors
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ALX-151-017-M001
1 mg
90.00 USD
ALX-151-017-M005
5 mg
360.00 USD
Product Specification
SEQUENCE:
H-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-NH
2
FORMULA:
C
49
H
86
N
24
O
15
MW:
1251.4
PURITY:
≥97%
APPEARANCE:
White powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Further Categories Containing This Product:
Peptides
ALX-151-021
Revised 14-Aug-02
H-Arg-Gly-Tyr-Ser-Leu-Gly-OH
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKA Inhibitors
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ALX-151-021-M001
1 mg
40.00 USD
ALX-151-021-M005
5 mg
140.00 USD
Product Specification
FORMULA:
C
28
H
45
N
9
O
9
MW:
651.7
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Substrate for cAMP-dependent protein kinase (PKA).
Product Specific Literature References
Synthetic hexapeptide substrates and inhibitors of 3':5'-cyclic AMP- dependent protein kinase:
B.E. Kemp, et al.; PNAS
73
, 1038 (1976)
Abstract
Synthetic peptide substrates of the cAMP-dependent protein kinase:
B.E. Kemp, et al.; Fed. Proc.
35
, 1384 (1976)
Further Categories Containing This Product:
Peptides
ALX-480-024
Revised 18-Jun-08
8-Bromoadenosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . sodium salt
SYNONYMS
Rp-8-Br-cAMPS . Na
8-Br-cAMPS . Na, Rp-isomer
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cAMP Derivatives
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ALX-480-024-MC05
0.5 mg
95.00 USD
ALX-480-024-M001
1 mg
175.00 USD
Product Specification
FORMULA:
C
10
H
10
BrN
5
O
5
PS . Na
MW:
423.2 . 23.0
CAS NUMBER:
129735-00-8
PURITY:
≥99% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
250 mM soluble in water, aqueous solutions, DMSO or dimethyl formamide.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Solutions should be stored in the refrigerator and should be lyophilized and frozen for longer storage periods.
IDENTITY:
Identity determined by
1
H-NMR, MS and UV.
Product Description
Inhibitor of cAMP-dependent protein kinase (PKA), preferentially binding to type I PKA. Lipophilic analog of Rp-cAMPS (Prod. No.
ALX-480-012
, and Prod. No.
ALX-480-085
). Resistant to mammalian cyclic nucleotide-dependent phosphodiesterases. Significantly more lipophilic and membrane permeant as compared to Rp-cAMPS or 8-Br-cAMP (Prod. No.
ALX-480-007
).
Product Specific Literature References
Activation of intestinal CFTR Cl- channel by heat-stable enterotoxin and guanylin via cAMP-dependent protein kinase:
A.C. Chao, et al.; EMBO J.
13
, 1065 (1994)
Abstract
Novel (Rp)-cAMPS analogs as tool for inhibition of cAMP-kinase in cell culture:
B.T. Gjertsen, et al.; J. Biol. Chem.
270
, 20599 (1995)
Abstract
;
Full Text
Further Categories Containing This Product:
PKA Inhibitors
ALX-350-027
Revised 19-Aug-08
Calphostin C
SYNONYMS
UCN-1028C
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Natural Products - Protein Kinase Inhibitors
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ALX-350-027-C100
100 µg
85.00 USD
ALX-350-027-M001
1 mg
595.00 USD
Product Specification
FORMULA:
C
44
H
38
O
14
MW:
790.8
CAS NUMBER:
121263-19-2
SOURCE/HOST:
Isolated from
Cladosporium cladosporioides
MST-FP1798.
PURITY:
≥95% (HPLC)
APPEARANCE:
Dark red solid.
SOLUBILITY:
Soluble in 100% ethanol, methanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STABILITY:
Stock solutions are stable for 3 months when stored at -20°C.
HANDLING:
Protect from light.
Product Description
Potent and selective inhibitor of the protein kinase C (PKC) regulatory site of diacylglycerol and phorbol esters. At higher concentrations inhibits myosin light chain kinase, cAMP-dependent protein kinase, protein kinase G and pp60v-src protein tyrosine kinase. Induces apoptotic DNA fragmentation and cell death. Kills breast cancer cells. Has antiviral potential. Inhibits cardiac L-type Ca
2+
channels.
Product Specific Literature References
Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C:
E. Kobayashi, et al.; BBRC
159
, 548 (1989)
Abstract
Potent and specific inhibitors of protein kinase C of microbial origin:
T. Tamaoki and H. Nakano; Biotechnology
8
, 732 (1990)
Abstract
Inhibition of protein kinase C by calphostin C is light-dependent:
R.F. Bruns, et al.; BBRC
176
, 288 (1991)
Abstract
Irreversible oxidative inactivation of protein kinase C by photosensitive inhibitor calphostin C:
R. Gopalakrishna, et al.; FEBS Lett.
314
, 149 (1992)
Abstract
Calphostin C, a specific protein kinase C inhibitor, activates human neutrophils: effect on phospholipase A2 and aggregation:
S. Svetlov and S. Nigam; Biochim. Biophys. Acta
1177
, 75 (1993)
Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C:
W.D. Jarvis, et al.; Cancer Res.
54
, 1707 (1994)
Abstract
Growth inhibition of herpes simplex virus-type 1 in calphostin C-treated astrocytes:
C.G. Castagnino, et al.; Intervirology
38
, 332 (1995)
Abstract
Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels:
H.C. Hartzell & A. Rinderknecht; Am. J. Physiol.
270
, C1293 (1996)
Abstract
Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity:
C.L. Chen, et al.; Pharm. Res.
16
, 1003 (1999)
Abstract
Potent killing of paclitaxel- and doxorubicin-resistant breast cancer cells by calphostin C accompanied by cytoplasmic vacuolization:
B. Guo, et al.; Breast Cancer Res. Treat.
82
, 125 (2003)
Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors
•
Tyrosine Kinase Inhibitors
•
PKA Inhibitors
•
PKC Inhibitors
•
PKG Inhibitors
•
Ca2+ Channels (L-type)
•
Natural Products - Antitumor Reagents
•
Natural Products - Apoptosis Inducers & Inhibitors
•
Natural Products - Antiviral / anti-HIV Agents
ALX-270-281
Revised 28-Sep-06
Daphnetin
SYNONYMS
7,8-Dihydroxycoumarin
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
EGFR Kinase Inhibitors
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ALX-270