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cGMP Pathways
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ALX-270-039 Revised 15-Nov-06
A-3 . hydrochloride
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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 Add To Cart
ALX-270-039-M050   50 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C12H13ClN2O2S . 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 • Casein Kinase Inhibitors • PKG Inhibitors
 
 
ALX-420-030 Revised 12-Dec-06
BAY 41-2272
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SYNONYMS 3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY Guanylyl Cyclases, Guanosine Phosphate Metabolism/Related Products
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ALX-420-030-M005   5 mg 92.00 USD Add To Cart
ALX-420-030-M025   25 mg 358.00 USD Add To Cart
Product Specification
FORMULA: C20H17FN6
MW: 360.4
PURITY: ≥98%
APPEARANCE: White to off-white needles.
SOLUBILITY: Soluble in DMSO, dichloromethane, 100% ethanol or 2-pyrrolidone. Practically insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
NO-independent activator of soluble guanylyl cyclase (sGC) [1,2]. Activates both isoforms α1β1 and α1β2 of sGC [3]. While the related compound YC-1 (Prod. No. ALX-420-025) also acts as a non-specific phosphodiesterase inhibitor, BAY 41-2272 has no effect on phosphodiesterases. Stimulation of sGC is not blocked by high concentrations of NO scavengers (e.g. PTIO, Prod. No. ALX-430-007) and the combination of  BAY 41-2272 with the NO donor DEA NONOate (Prod. No. ALX-430-034) potentiates the activation of sGC. Although BAY 41-2272 alone is not as strong a stimulator of sGC as NO, concentrations as low as 10-100nM stimulate sGC to a level that would be expected to cause biologically important increases in cGMP [1]. ODQ (Prod. No. ALX-270-034), a potent and selective inhibitor of sGC, completely inhibited the effect of BAY 41-2272 [1]. The activity of BAY 41-2272 is described in selected literature references [4-6].
Product Specific Literature References
[1] NO-independent regulatory site on soluble guanylate cyclase: J.P. Stasch, et al.; Nature 410, 212 (2001) Abstract
[2] NO-independent regulatory site of direct sGC stimulators like YC-1 and BAY 41-2272: E.M. Becker, et al.; BMC Pharmacol. 1, 13 (2001) Abstract; Full Text
NO-independent stimulators of soluble guanylate cyclase: A. Straub, et al.; Bioorg. Med. Chem. Lett. 11, 781 (2001) Abstract
[3] BAY 41-2272 activates two isoforms of nitric oxide-sensitive guanylyl cyclase: M. Koglin, et al.; BBRC 292, 1057 (2002) Abstract
[4] Cardiorenal and humoral properties of a novel direct soluble guanylate cyclase stimulator BAY 41-2272 in experimental congestive heart failure: G. Boerrigter, et al.; Circulation 107, 686 (2003) Abstract
[5] BAY 41-2272: a stimulator of soluble guanylyl cyclase induces nitric oxide-dependent penile erection in vivo: E. Bischoff, et al.; Urology 61, 464 (2003) Abstract
[6] Macrophage endothelial nitric oxide synthase auto-regulates cellular activation and pro-inflammatory protein expression: L. Connelly, et al.; J. Biol. Chem 278, 26480 (2003) Abstract; Full Text
Antiinflammatory activity of soluble guanylate cyclase: cGMP-dependent down-regulation of P-selectin expression and leukocyte recruitment: A. Ahluwalia, et al.; PNAS 101, 1386 (2004) Abstract; Full Text
Identification of residues crucially involved in soluble guanylate cyclase activation: C. Rothkegel, et al.; FEBS Lett. 580, 4205 (2006) Abstract
 
 
ALX-270-421 Revised 14-Feb-07
BAY 60-7550
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SYNONYMS 2-(3,4-Dimethoxybenzyl)-7-[(1R)-1-[(1R)-1-hydroxyethyl]-4-phenylbutyl]-5-methylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphodiesterases/Related Products
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ALX-270-421-M005   5 mg 98.00 USD Add To Cart
ALX-270-421-M025   25 mg 395.00 USD Add To Cart
Product Specification
FORMULA: C27H32N4O4
MW: 476.6
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetone, DMSO or 100% ethanol. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of human phosphodiesterase 2 (PDE2) (IC50=5nM). Selective (>50-fold) versus other human PDEs tested (1C,3A, 4B, 5A, 6, 7B, 8A, 9A, 10A, 11A) and does not affect adenosine deaminase. Raises cGMP levels in cell culture, particularly in combination with a suitable activator of soluble guanylyl cyclase (sGC). Raises cAMP in combination with forskolin (Prod. No. ALX-350-001). Increases memory performance in rodents in vivo.
Product Specific Literature References
Inhibition of phosphodiesterase 2 increases neuronal cGMP, synaptic plasticity and memory performance: F.G. Boess, et al.; Neuropharmacology 47, 1081 (2004) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Please also see our Product Flyer "BAY 60-7550 - A Novel Potent & Selective PDE2 Inhibitor".
General Literature References
Dynamic regulation of cAMP signaling by cGMP in the cardiovascular system: roles of phosphodiesterase 2 and phosphodiesterase 3 enzymes: D.H. Maurice; Proc. West. Pharmacol. Soc. 46, 32 (2003) Abstract
Cyclic nucleotide phosphodiesterases and their role in immunomodulatory responses: advances in the development of specific phosphodiesterase inhibitors: A. Castro, et al.; Med. Res. Rev. 25, 229 (2005) Abstract
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases: D.T. Manallack, et al.; J. Med. Chem. 48, 3449 (2005) Abstract
Related Products
Further Categories Containing This Product:
Phosphodiesterases/Related Products
 
 
ALX-152-022 Revised 04-Jul-03
BPDEtide
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKG Substrates
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ALX-152-022-M001   1 mg 60.00 USD Add To Cart
ALX-152-022-M005   5 mg 240.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Ile-Ser-Ala-Ser-Glu-Phe-Asp-Arg-Pro-Leu-Arg-OH
FORMULA: C68H115N23O20
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. Døskeland; 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
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SYNONYMS 8-Br-cGMP . Na
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cGMP Derivatives
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ALX-480-006-M010   10 mg 48.00 USD Add To Cart
ALX-480-006-M050   50 mg 145.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O7P . 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 1H-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)
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SYNONYMS Rp-8-Br-cGMPS . Na
8-Br-cGMPS . Na, Rp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cGMP Derivatives
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ALX-480-026-MC05   0.5 mg 90.00 USD Add To Cart
ALX-480-026-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O6PS . 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)
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SYNONYMS Sp-8-Br-cGMPS . Na
8-Br-cGMPS . Na, Sp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cGMP Derivatives
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ALX-480-027-M001   1 mg 80.00 USD Add To Cart
ALX-480-027-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O6PS . 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, 1H-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-350-246 Revised 07-Mar-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol that acts as a specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Glutathione S-Transferase • Natural Products - Anti-inflammatory Agents • Phosphodiesterases/Related Products • IkB Kinases [IKKs]/Related Products • EGFR Kinase Inhibitors • Glutathione/Related Products • Natural Products - Antioxidants • Natural Products - Chemopreventive Agents • Flavonoids/Related Products
 
 
ALX-550-322 Revised 29-Oct-07
Caffeine
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SYNONYMS 1,3,7-Trimethylxanthine
3,7-Dihydro-1,3,7-trimethyl-1H-purine-2,6-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-550-322-G005   5 g 10.00 USD Add To Cart
Product Specification
FORMULA: C8H10N4O2
MW: 194.2
CAS NUMBER: 58-08-2
MERCK INDEX: 14: 1636
SOURCE/HOST: Found in tea leaves, coffee beans, cocoa beans, maté leaves, guarana paste and kola nuts.
PURITY: ≥99%
APPEARANCE: White powder.
SOLUBILITY: Soluble in chloroform, 100% alcohol or hot water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: TOXIC.

Product Description
CNS stimulant. Blocks adenosine A1 and A2A receptors. cAMP phosphodiesterase inhibitor. Interferes with the uptake and storage of Ca2+ by the sarcoplasmic reticulum in skeletal muscle. Prevents apoptosis and cell cycle effects induced by various chemicals. Inhibits cellular DNA repair mechanisms. Anti-inflammatory.
Product Specific Literature References
Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors: J.W. Daly, et al.; J. Med. Chem. 29, 1305 (1986) Abstract
Caffeine as an analgesic adjuvant: a review of pharmacology and mechanisms of action: J. Sawynok & T.L. Yaksh; Pharmacol. Rev. 45, 43 (1993) Abstract
Caffeine prevents apoptosis and cell cycle effects induced by camptothecin or topotecan in HL-60 cells: F. Traganos, et al.; Cancer Res. 53, 4613 (1993) Abstract
Multiple effects of caffeine on calcium current in rat ventricular myocytes: I. Zahradnik & P. Palade; Pfluegers Arch. 424, 129 (1993) Abstract
Acute effects of caffeine on arterial stiffness, wave reflections, and central aortic pressures: T.G. Papaioannou, et al.; Am. J. Hypertens. 18, 129 (2005), (Review) Abstract
Caffeine and the dopaminergic system: O. Cauli & M. Morelli; Behav. Pharmacol. 16, 63 (2005), (Review) Abstract
Immunomodulatory effects of caffeine: friend or foe: L. A. Horrigan, et al.; Pharmacol. Ther. 111, 877 (2006), (Review) Abstract
Novel neuroprotection by caffeine and adenosine A(2A) receptor antagonists in animal models of Parkinson’s disease: A. Kalda, et al.; J. Neurol. Sci. 248, 9 (2006), (Review) Abstract
The enigmatic effects of caffeine in cell cycle and cancer: A. M. & Bode and Z. Dong; Cancer Lett. 247, 26 (2007), (Review) Abstract
Further Categories Containing This Product:
Natural Products - Other Signal Transduction Pathway Modulators • Ca2+ Modulators • Phosphodiesterases/Related Products • DNA Repair Other Products • Neuroactive Agents Other Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products for Cell Cycle Research • Natural Products - Anti-inflammatory Agents •