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cAMP Pathways
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ALX-480-024 Revised 18-Jun-08
8-Bromoadenosine 3',5'-cyclic Monophosphothioate, Rp-Isomer . sodium salt
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SYNONYMS Rp-8-Br-cAMPS . Na
8-Br-cAMPS . Na, Rp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-480-024-MC05   0.5 mg 95.00 USD Add To Cart
ALX-480-024-M001   1 mg 175.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O5PS . 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 1H-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-480-025 Revised 26-Jul-06
8-Bromoadenosine 3',5'-cyclic Monophosphothioate, Sp-Isomer . sodium salt
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SYNONYMS Sp-8-Br-cAMPS . Na
8-Br-cAMPS . Na, Sp-isomer
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY cAMP Derivatives
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-480-025-M001   1 mg 140.00 USD Add To Cart
ALX-480-025-M005   5 mg 560.00 USD Add To Cart
Product Specification
FORMULA: C10H10BrN5O5PS . Na
MW: 423.2 . 23.0
CAS NUMBER: 127634-20-2
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water or aqueous buffer.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Metabolically resistant activator of cAMP-dependent protein kinase (PKA) (cAMP agonist). No metabolic side effects as observed with dibutyryl-cAMP (N6,O2'-Dibutyryladenosine 3',5'-cyclic monophosphate, Prod. No. ALX-480-045) or 8-Br-cAMP (8-Bromoadenosine-3',5'-cyclic monophosphate, Prod. No. ALX-480-007). Significantly more lipophilic and membrane permeant as compared to Sp-cAMPS (Adenosine 3',5'-cyclic monophosphothioate, Sp isomer, Prod. No. ALX-480-013).
Product Specific Literature References
Cell-permeable non-hydrolyzable cAMP derivatives as tools for analysis of signaling pathways controlling gene regulation in Dictyostelium: P. Schaap, et al.; J. Biol. Chem. 268, 6323 (1993) Abstract; Full Text
Further Categories Containing This Product:
PKA Activators
 
 
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 ActivatorsPKA Activators
 
 
ALX-350-246 Revised 07-Oct-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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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. 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
 
 
ALX-550-322 Revised 11-Nov-08
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 to colorless powder.
SOLUBILITY: Soluble in chloroform, 100% alcohol or hot water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: HARMFUL.
IDENTITY: Identity determined by NIR.

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
 
 
ALX-430-026 Revised 12-Sep-06
Calmidazolium chloride
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SYNONYMS 1-[bis(p-Chlorophenyl)methyl]-3-[2,4-dichloro-β-(2,4-dichlorobenzyloxy)phenethyl] imidazolium chloride
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-026-M010   10 mg 85.00 USD Add To Cart
ALX-430-026-M050   50 mg 340.00 USD Add To Cart
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Product Specification
FORMULA: C31H23Cl7N2O
MW: 687.7
CAS NUMBER: 57265-65-3
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in methanol, 100% ethanol, chloroform, DMSO or propylene glycol; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Calmodulin antagonist. At least 150 times more potent than trifluoperazine (Prod. No. ALX- 550-310) as an inhibitor of brain calmodulin-dependent phosphodiesterase. Inhibitor of voltage-gated Ca2+ channels. Blocks Ca2+-calmodulin binding to NOS.
Product Specific Literature References
Inhibitors of calmodulin impair the constitutive but not the inducible nitric oxide synthase activity in the rat aorta: V.B. Schini & P.M. Vanhoutte; J. Pharmacol. Exp. Ther. 261, 553 (1992) Abstract
Calmidazolium, a calmodulin inhibitor, inhibits endothelium-dependent relaxations resistant to nitro-L-arginine in the canine coronary artery: S. Illiano, et al.; Br. J. Pharmacol. 107, 387 (1992) Abstract
The calmodulin antagonist calmidazolium stimulates release of nitric oxide in neuroblastoma N1E-115 cells: J. Hu & E.E. el-Fakahany; Neuroreport 4, 198 (1993) Abstract
Vasoactive intestinal peptide/pituitary adenylate cyclase-activating peptide-dependent activation of membrane-bound NO synthase in smooth muscle mediated by pertussis toxin-sensitive Gi1-2: K.S. Murthy & G.M. Makhlouf; J. Biol. Chem. 269, 15977 (1994) Abstract
Mitochondrial nitric oxide synthase is constitutively active and is functionally upregulated in hypoxia: Z. Lacza, et al.; Free Radic. Biol. Med. 31, 1609 (2001) Abstract
Mitochondrial calcium uptake stimulates nitric oxide production in mitochondria of bovine vascular endothelial cells: E.N. Dedkova, et al.; Am. J. Physiol. Cell Physiol. 286, C406 (2004) Abstract; Full Text
Neural tube closure depends on nitric oxide synthase activity: A. Nachmany, et al.; J. Neurochem. 96, 247 (2006) Abstract
Further Categories Containing This Product:
NOS Other ProductsCa2+ Channels (L-type)Phosphodiesterases / Related Products
 
 
ALX-350-027 Revised 19-Aug-08
Calphostin C
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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 Add To Cart
ALX-350-027-M001   1 mg 595.00 USD Add To Cart
Product Specification
FORMULA: C44H38O14
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 Ca2+ 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
 
 
ALX-201-224 Revised 22-Feb-06
cAMP-dependent Protein Kinase (Catalytic Subunit Cα) (mouse) (recombinant)
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SYNONYMS Protein Kinase A (Catalytic Subunit Cα) (mouse) (recombinant)
PKA (Catalytic Subunit Cα) (mouse) (recombinant)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-201-224-C025   25 µg 305.00 USD Add To Cart
ALX-201-224-C050   50 µg 474.00 USD Add To Cart
ALX-201-224-C100   100 µg 812.00 USD Add To Cart
Product Specification
MW: ~41kDa
SOURCE/HOST: Produced in E. coli.
CONCENTRATION:  
PURITY: ≥95% (SDS-PAGE)
FORMULATION: Liquid. In 25mM potassium phosphate, pH 6.5, containing 5mM β-mercaptoethanol, 5mM EDTA, 150mM NaCl and 50% glycerol.
SPECIFIC ACTIVITY: 1.5x107U/mg. One unit is defined as the amount of enzyme required to incorporate 1pmol phosphate per min into the specific substrate kemptide (Prod. No. ALX-160-006) at 30°C.
APPLICATION: - In vitro enzymological studies of neural and hormonal signal transduction
- Phosphorylation of target proteins in vivo (via microinjection) including ion channels, transcriptional activator proteins and regulatory enzymes of glycogen metabolism
SHIPPING: SHIPPED ON DRY ICE
SHORT TERM STORAGE: -20°C
LONG TERM STORAGE: -80°C
USE/STABILITY: Stable for 6 months after receipt when stored at -20°C. Stable for 2 weeks when stored at +4°C.
HANDLING: Avoid freeze/thaw cycles.
Further Categories Containing This Product:
EnzymesRecombinant Proteins / Fusion Proteins
 
 
ALX-201-229 Revised 15-May-07
cAMP-dependent Protein Kinase (Holoenzyme Type IIα, Cα2 (mouse)/RIIα2 (human)) (recombinant)
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SYNONYMS Protein Kinase A (Holoenzyme Type IIα, Cα2 (mouse)/RIIα2 (human)) (recombinant)
PKA (Holoenzyme Type IIα, Cα2 (mouse)/RIIα2 (human)) (recombinant)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-201-229-C020   20 µg 474.00 USD Add To Cart
ALX-201-229-C050   50 µg 812.00 USD Add To Cart