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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:
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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-152-022
Revised 04-Jul-03
BPDEtide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKG Substrates
Ordering Information
Product Numbers:
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ALX-152-022-M001
1 mg
60.00 USD
ALX-152-022-M005
5 mg
240.00 USD
Product Specification
SEQUENCE:
H-Arg-Lys-Ile-Ser-Ala-Ser-Glu-Phe-Asp-Arg-Pro-Leu-Arg-OH
FORMULA:
C
68
H
115
N
23
O
20
MW:
1574.8
PURITY:
≥97%
APPEARANCE:
White lyophilized powder.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Substrate for cGMP-dependent protein kinase corresponding to a peptide sequence surrounding the phosphorylation site of cGMP-binding cGMP-specific phosphodiesterase.
Product Specific Literature References
Studies of two different intrachain cGMP-binding sites of cGMP- dependent protein kinase:
J.D Corbin & S.O. Dřskeland; J. Biol. Chem.
258
, 11391 (1983)
Abstract
;
Full Text
A phenylalanine in peptide substrates provides for selectivity between cGMP- and cAMP-dependent protein kinases:
J.L. Colbran, et al.; J. Biol. Chem.
267
, 9589 (1992)
Abstract
;
Full Text
Further Categories Containing This Product:
Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products
•
Peptides
ALX-480-006
Revised 18-Jun-08
8-Bromoguanosine-3',5'-cyclic Monophosphate . sodium salt
SYNONYMS
8-Br-cGMP . Na
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cGMP Derivatives
Ordering Information
Product Numbers:
Format:
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ALX-480-006-M010
10 mg
48.00 USD
ALX-480-006-M050
50 mg
145.00 USD
Product Specification
FORMULA:
C
10
H
10
BrN
5
O
7
P . Na
MW:
423.1 . 23.0
CAS NUMBER:
51116-01-9
PURITY:
≥99% (HPLC)
APPEARANCE:
White to off-white powder.
PURITY DETAIL:
Low in fluorescent and colored impurities.
SOLUBILITY:
Soluble in water or aqueous buffers.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
IDENTITY:
Identity determined by
1
H-NMR, MS and UV.
Product Description
Activator of cGMP-dependent protein kinases (PKGs) 1α, 1β and type II and cGMP-gated ion channels (cGMP agonist). Has increased metabolic stability and membrane permeability compared to cGMP (Prod. No.
ALX-480-059
).
Product Specific Literature References
Sodium nitroprusside-induced protein phosphorylation in intact rat aorta is mimicked by 8-bromo cyclic GMP:
R.M. Rapoport, et al.; PNAS
79
, 6470 (1982)
Abstract
The nitric oxide--cyclic GMP pathway and synaptic depression in rat hippocampal slices:
C.L. Boulton, et al.; Eur. J. Neurosci.
6
, 1528 (1994)
Abstract
Nitric oxide in skeletal muscle:
L. Kobzik, et al.; Nature
372
, 546 (1994)
Abstract
Nitric oxide. More jobs for that molecule:
S. Snyder; Nature
372
, 504 (1994)
Abstract
Further Categories Containing This Product:
PKG Activators
ALX-480-026
Revised 03-Aug-06
8-Bromoguanosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . sodium salt (high purity)
SYNONYMS
Rp-8-Br-cGMPS . Na
8-Br-cGMPS . Na, Rp-isomer
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cGMP Derivatives
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-480-026-MC05
0.5 mg
90.00 USD
ALX-480-026-M001
1 mg
160.00 USD
Product Specification
FORMULA:
C
10
H
10
BrN
5
O
6
PS . Na
MW:
439.2 . 23.0
CAS NUMBER:
150418-07-8
PURITY:
≥99% (HPLC)
APPEARANCE:
White lyophilized powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Inhibitor of cGMP-dependent protein kinase (PKG) 1α and 1β. Resistant to mammalian cyclic nucleotide-dependent phosphodiesterases; no metabolic side effects. Significantly more lipophilic and membrane permeant as compared to cyclic GMP (Prod. No.
ALX-480-059
) or Rp-cGMPS (Prod. No.
ALX-480-072
).
Product Specific Literature References
Nitric oxide regulates luteinizing hormone-releasing hormone secretion:
M. Moretto, et al.; Endocrinology
133
, 2399 (1993)
Abstract
Role of guanylyl cyclase and cGMP-dependent protein kinase in long-term potentiation:
M. Zhuo, et al.; Nature
368
, 635 (1994)
Abstract
Further Categories Containing This Product:
PKG Inhibitors
ALX-480-027
Revised 25-Jun-08
8-Bromoguanosine 3',5'-cyclic Monophosphothioate, Sp-Isomer . sodium salt (high purity)
SYNONYMS
Sp-8-Br-cGMPS . Na
8-Br-cGMPS . Na, Sp-isomer
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cGMP Derivatives
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-480-027-M001
1 mg
80.00 USD
ALX-480-027-M005
5 mg
320.00 USD
Product Specification
FORMULA:
C
10
H
10
BrN
5
O
6
PS . Na
MW:
439.2 . 23.0
CAS NUMBER:
153660-03-8
PURITY:
≥99% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
IDENTITY:
Identity determined by MS,
1
H-NMR and UV.
Product Description
Unspecific activator of both cGMP-dependent protein kinase (PKG) 1α and cAMP-dependent protein kinase (PKA). Resistant to cyclic nucleotide phosphodiesterases. Much more lipophilic and membrane permeant as compared to cyclic GMP (Prod. No.
ALX-480-059
) or Sp-cGMPS (Prod. No.
ALX-480-073
).
Product Specific Literature References
Evidence for two intracellular calcium pools in Dictyostelium: the cAMP- induced calcium influx is directed into a NBD-Cl- and 2,5-di-(tert- butyl)1,4-hydroquinone-sensitive pool:
H. Flaadt, et al.; J. Cell Sci.
105
, 1131 (1993)
Abstract
Further Categories Containing This Product:
PKG Activators
•
PKA Activators
ALX-350-027
Revised 19-Aug-08
Calphostin C
SYNONYMS
UCN-1028C
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Natural Products - Protein Kinase Inhibitors
Ordering Information
Product Numbers:
Format:
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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:
Tyrosine Kinase Inhibitors
•
PKA Inhibitors
•
PKC Inhibitors
•
PKG Inhibitors
•
Myosin Light Chain Kinase Inhibitors
•
Ca2+ Channels (L-type)
•
Natural Products - Antiviral / anti-HIV Agents
•
Natural Products - Antitumor Reagents
•
Natural Products - Apoptosis Inducers & Inhibitors
ALX-480-030
Revised 07-Jun-06
8-(4-Chlorophenylthio)adenosine 3',5'-cyclic Monophosphate . sodium salt
SYNONYMS
8-pCPT-cAMP . Na
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cAMP Derivatives
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-480-030-M010
10 mg
25.00 USD
ALX-480-030-M025
25 mg
50.00 USD
Product Specification
FORMULA:
C
16
H
14
ClN
5
O
6
PS . Na
MW:
470.8 . 23.0
CAS NUMBER:
93882-12-3
PURITY:
≥99%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions should be stored in the refrigerator and should be lyophilized and frozen for longer storage periods.
Product Description
Lipophilic, membrane permeable activator of both cAMP- and cGMP-dependent protein kinases (PKA, PKG). More potent than cAMP and more resistant to phosphodiesterases, with good selectivity for site B of PKA. For specific activation of the cAMP pathway the highly membrane permeable Sp-5,6-DCl-cBIMPS (Prod. No.
ALX-480-047
) is a recommended.
Product Specific Literature References
cAMP analogs promote survival and neurite outgrowth in cultures of rat sympathetic and sensory neurons independently of nerve growth factor:
R.E. Rydel & L.A. Greene; PNAS
85
, 1257 (1988)
Abstract
Comparison of the two classes of binding sites (A and B) of type I and type II cyclic-AMP-dependent protein kinases by using cyclic nucleotide analogs:
D. Ogreid, et al.; Eur. J. Biochem.
181
, 19 (1989)
Abstract
8-(4-Chlorophenyl)thio-cyclic AMP is a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA):
B.J. Connolly, et al.; Biochem. Pharmacol.
44
, 2303 (1992)
Abstract
Role of cGMP and cGMP-dependent protein kinase in nitrovasodilator inhibition of agonist-evoked calcium elevation in human platelets:
J. Geiger, et al.; PNAS
89
, 1031 (1992)
Abstract
The role of protein kinase A anchoring via the RII alpha regulatory subunit in the murine immune system:
R.V. Schillace, et al.; J. Immunol.
174
, 6847 (2005)
Abstract
;
Full Text
Further Categories Containing This Product:
PKG Activators
•
PKA Activators
ALX-480-088
Revised 31-Oct-06
8-(4-Chlorophenylthio)guanosine 3',5'-cyclic Monophosphate . sodium salt
SYNONYMS
8-pCPT-cGMP . Na
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cGMP Derivatives
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-480-088-M001
1 mg
50.00 USD
ALX-480-088-M005
5 mg
190.00 USD
Product Specification
FORMULA:
C
16
H
14
ClN
5
O
7
PS . Na
MW:
486.8 . 23.0
CAS NUMBER:
51239-26-0
PURITY:
≥99% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Selective activator of cGMP-dependent protein kinase (PKG) Iα, Iβ, and type II as well as of cGMP-gated ion channels. Higher activation potential as compared to cGMP; excellent cell membrane permeability and phosphodiesterase stability. Preferred alternative to unsuitable analogs such as dibutyryl-cGMP.
Product Specific Literature References
Role of cGMP and cGMP-dependent protein kinase in nitrovasodilator inhibition of agonist-evoked calcium elevation in human platelets
:
J. Geiger, et al.; PNAS
89
, 1031 (1992)
Abstract
Analysis of the functional role of cGMP-dependent protein kinase in intact human platelets using a specific activator 8-para-chlorophenylthio-cGMP
:
E. Butt, et al.; Biochem. Pharmacol.
43
, 2591 (1992)
Abstract
Further Categories Containing This Product:
PKG Activators
ALX-480-031
Revised 03-Feb-05
8-(4-Chlorophenylthio)guanosine 3',5'-cyclic Monophosphate . triethylammonium salt
SYNONYMS
8-pCPT-cGMP . TEA
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cGMP Derivatives
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-480-031-M001
1 mg
42.00 USD
ALX-480-031-M005
5 mg
168.00 USD
Product Specification
FORMULA:
C
16
H
14
ClN
5
O
7
PS . C
6
H
15
N
MW:
486.8 . 101.2
CAS NUMBER:
54364-02-2
PURITY:
≥99%
APPEARANCE:
White lyophilized powder.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Selective activator of cGMP-dependent protein kinase Iα, Iβ and type II as well as of cGMP-gated ion channels. Higher activation potential as compared to cGMP; excellent cell membrane permeability and phosphodiesterase stability. Preferred alternative to unsuitable analogs such as dibutyryl-cGMP.
Product Specific Literature References
Analysis of the functional role of cGMP-dependent protein kinase in intact human platelets using a specific activator 8-para- chlorophenylthio-cGMP:
E. Butt, et al.; Biochem. Pharmacol.
43
, 2591 (1992)
Abstract
Role of cGMP and cGMP-dependent protein kinase in nitrovasodilator inhibition of agonist-evoked calcium elevation in human platelets:
J. Geiger, et al.; PNAS
89
, 1031 (1992)
Abstract
Further Categories Containing This Product:
PKG Activators
ALX-480-087
Revised 21-Dec-06
8-(4-Chlorophenylthio)guanosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . sodium salt
SYNONYMS
Rp-8-pCPT-cGMPS . Na
8-pCPT-cGMPS . Na, Rp-Isomer
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
cGMP Derivatives
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-480-087-C100
100 µg
50.00 USD
ALX-480-087-M001
1 mg
280.00 USD
Product Specification