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cGMP Pathways
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ALX-270-070 Revised 16-Jun-06
HA-1004 . dihydrochloride
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SYNONYMS N-(2'-Guanidinoethyl)-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-070-M005   5 mg 35.00 USD Add To Cart
ALX-270-070-M025   25 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C12H15N5O2S . 2HCl
MW: 293.3 . 73.0
CAS NUMBER: 92564-34-6
PURITY: ≥99%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Inhibitor of cAMP- and cGMP-dependent kinases (PKA and PKG). Intracellular Ca2+ antagonist with no effect on cardiac function. Causes selective pulmonary vasodilation during pulmonary hypertension.
Product Specific Literature References
Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C: H. Hidaka, et al.; Biochemistry 23, 5036 (1984) Abstract
Differential effects of isoquinolinesulfonamide protein kinase inhibitors on CA1 responses in hippocampal slices [published erratum appears in Neuroscience 1993 Apr;53(4):1173]: J.C. Leahy & M.L. Vallano; Neuroscience 44, 361 (1991) Abstract
Further Categories Containing This Product:
PKG Inhibitors
 
 
ALX-158-003 Revised 04-Jul-03
Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones/Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-158-003-M001   1 mg 50.00 USD Add To Cart
ALX-158-003-M005   5 mg 200.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ser-Arg-Lys-Glu-OH
FORMULA: C38H74N18O11
MW: 959.1
PURITY: ≥97%
APPEARANCE: White powder.
FORMULATION: Lyophilized.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cGMP-dependent protein kinase corresponding to residues 29-35 of histone H2B. For the corresponding alanine-for-serine substituted peptides see Prod. No. ALX-158-002 and Prod. No. ALX-158-004.
Product Specific Literature References
Comparison of the substrate specificity of adenosine 3':5'- monophosphate- and guanosine 3':5'-monophosphate-dependent protein kinases. Kinetic studies using synthetic peptides corresponding to phosphorylation sites in histone H2B: D.B. Glass & E.G. Krebs; J. Biol. Chem. 254, 9728 (1979) Abstract; Full Text
 
 
ALX-158-002 Revised 28-Feb-06
[Ala32]-Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones/Related Products
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ALX-158-002-M001   1 mg 75.00 USD Add To Cart
ALX-158-002-M005   5 mg 300.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ala-Arg-Lys-Glu-OH
FORMULA: C38H74N18O10
MW: 943.1
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Inhibitor of cGMP-dependent protein kinase, derived by a serine-to-alanine substitution at position 32 of histone H2B (29-35). For the corresponding unsubstituted histone fragment see Prod. No. ALX-158-003.
Product Specific Literature References
D.B. Glass & M.D. Miller; Fed. Proc. 39, 867 (1980)
Differential responses of cyclic GMP-dependent and cyclic AMP-dependent protein kinases to synthetic peptide inhibitors: D.B. Glass; Biochem. J. 213, 159 (1983) Abstract
Further Categories Containing This Product:
PeptidesPKG Inhibitors
 
 
ALX-158-004 Revised 13-Jan-05
[Ala34]-Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones/Related Products
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ALX-158-004-M001   1 mg 60.00 USD Add To Cart
ALX-158-004-M005   5 mg 240.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ser-Arg-Ala-Glu-OH
FORMULA: C35H67N17O11
MW: 902.0
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cGMP-dependent protein kinase. For the corresponding unsubstituted histone fragment see Prod. No. ALX-158-003.
Product Specific Literature References
Phosphorylation by guanosine 3':5'-monophosphate-dependent protein kinase of synthetic peptide analogs of a site phosphorylated in histone H2B: D.B. Glass & E.G. Krebs; J. Biol. Chem. 257, 1196 (1982) Abstract; Full Text
Further Categories Containing This Product:
PKG SubstratesPeptides
 
 
ALX-480-038 Revised 18-Jun-08
IBMX
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SYNONYMS 3-Isobutyl-1-methylxanthine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Adenosine Receptors/Related Products
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ALX-480-038-M500   500 mg 99.00 USD Add To Cart
ALX-480-038-G001   1 g 195.00 USD Add To Cart
Product Specification
FORMULA: C10H14N4O2
MW: 222.3
CAS NUMBER: 28822-58-4
RTECS: ZD8500000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or methanol (warm, 50mg/ml); almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.
IDENTITY: Identity determined by IR.

Product Description
Potent, non-specific inhibitor of phosphodiesterases. More potent than theophylline (Prod. No. ALX-480-062) at adenosine receptors. Accelerates conversion of mouse fibroblast cells into adipose cells.
Product Specific Literature References
Effects of xanthine derivatives on lipolysis and on adenosine 3',5'- monophosphate phosphodiesterase activity: J.A. Beavo, et al.; Mol. Pharmacol. 6, 597 (1970) Abstract
Adenosine 3':5'-cyclic monophosphate and insulin release: W. Montague & J.R. Cook; Biochem. J. 120, 9P (1970) Abstract
The role of adenosine 3':5'-cyclic monophosphate in the regulation of insulin release by isolated rat islets of Langerhans: W. Montague & J.R. Cook; Biochem. J. 122, 115 (1971) Abstract
Cyclic nucleotide phosphodiesterase activity in normal mouse pancreatic islets: S.J. Ashcroft, et al.; FEBS Lett. 20, 263 (1972) Abstract
The mode of action of adenosine 3’:5’-cyclic monophosphate in mammalian islets of Langerhans. Effects of insulin secretagogues on islet-cell protein kinase activity: W. Montague & S.L. Howell; Biochem. J. 134, 321 (1973) Abstract
Effects of methylxanthines on adenosine 3’,5’-monophosphate and corticosterone in the rat adrenal: A. Peytremann, et al.; Endocrinology 92, 525 (1973) Abstract
Concentration of adenosine 3’:5’-cyclic monophosphate in mouse pancreatic islets measured by a protein-binding radioassay: R.H. Cooper, et al.; Biochem. J. 134, 599 (1973) Abstract
Determination of theophylline in plasma by electron capture gas chromatography: H.A. Schwertner, et al.; Anal. Chem. 48, 1875 (1976) Abstract
Methyl xanthine phosphodiesterase inhibitors behave as prostaglandin antagonists in a perfused rat mesenteric artery preparation: D.F. Horrobin, et al.; Prostaglandins 13, 33 (1977) Abstract
Selective inhibition of cyclic nucleotide phosphodiesterases by analogues of 1-methyl-3-isobutylxanthine: G.L. Kramer, et al.; Biochemistry 16, 3316 (1977) Abstract
Cyclic nucleotide phosphodiesterases of human and rat gastric mucosa: U. Klotz, et al.; Naunyn-Schmiedebergs Arch. Pharmacol. 296, 187 (1977) Abstract
Allergic reactions, cyclic AMP and histamine release: P.S. Skov, et al.; Experientia 33, 965 (1977) Abstract
Differentiation of 3T3-L2 fibroblasts into adipose cells in bromodeoxyuridine-suppressed cultures: T.R. Russell; PNAS 76, 4451 (1979) Abstract
Inhibition of growth of primary and metastatic Lewis lung carcinoma cells by the phosphodiesterase inhibitor isobutylmethylxanthine: P. Janik, et al.; Cancer Res. 40, 1950 (1980) Abstract
Induction of a transient elevation in intracellular levels of adenosine-3’,5’-cyclic monophosphate by chemotactic factors: an early event in human neutrophil activation: L. Simchowitz, et al.; J. Immunol. 124, 1482 (1980) Abstract
Selective inhibition of cyclic AMP and cyclic GMP phosphodiesterases of cardiac nuclear fraction: G.S. Ahluwalia & A.R. Rhoads; Biochem. Pharmacol. 31, 665 (1982) Abstract
Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes: R.F. Bruns, et al.; Mol. Pharmacol. 29, 331 (1986) Abstract
Methylxanthine inhibitors of phosphodiesterases: J.N. Wells & J.R. Miller; Methods Enzymol. 159, 489 (1988) Abstract
Psychomotor-stimulant effects of 3-isobutyl-1-methylxanthine: comparison with caffeine and 7-(2-chloroethyl) theophylline: V.L. Coffin and R.D. Spealman; Eur. J. Pharmacol. 170, 35 (1989) Abstract
Differential effects of Ro 20-1724 and isobutylmethylxanthine on the basal force of contraction and beta-adrenoceptor-mediated response in the rat ventricular myocardium: Y. Katano & M. Endoh; BBRC 167, 123 (1990) Abstract
Bemoradan--a novel inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue: J.B. Moore, Jr., et al.; Biochem. Pharmacol. 42, 679 (1991) Abstract
Effect of an antihypertensive hydrazine derivative on Ca2+ current of single frog cardiac cells: F. Scamps, et al.; Eur. J. Pharmacol. 244, 119 (1993) Abstract
Isobutylmethylxanthine and other classical cyclic nucleotide phosphodiesterase inhibitors affect cAMP-dependent protein kinase activity: C. Tomes, et al.; Cell. Signal. 5, 615 (1993) Abstract
Further Categories Containing This Product:
Phosphodiesterases/Related Products
 
 
ALX-270-208 Revised 04-Feb-05
J-8 . hydrochloride
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SYNONYMS (N-8-Aminooctyl)-5-iodo-1-naphthalenesulfonamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-270-208-M005   5 mg 35.00 USD Add To Cart
ALX-270-208-M025   25 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C18H25IN2O2S . HCl
MW: 460.4 . 36.5
APPEARANCE: Off-white powder.
SOLUBILITY: Soluble in DMSO; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic .

Product Description
Highly selective calmodulin (CaM) antagonist. Inhibitor of Ca2+/calmodulin-dependent phosphodiesterase. Has a selectivity of ~300-fold over Ca2+/CaM-dependent enzymes compared with Ca2+-dependent but CaM-independent enzymes, e.g. protein kinase C (PKC) and transglutaminase.
Product Specific Literature References
Calmodulin antagonists of improved potency and specificity for use in the study of calmodulin biochemistry: S. MacNeil, et al.; Biochem. Pharmacol. 37, 1717 (1988) Abstract
Complexes formed between calmodulin and the antagonists J-8 and TFP in solution: C.J. Craven, et al.; Biochemistry 35, 10287 (1996) Abstract
Further Categories Containing This Product:
Phosphodiesterases/Related Products
 
 
ALX-380-027 Revised 09-May-08
K-252a
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-380-027-C100   100 µg 98.00 USD Add To Cart
ALX-380-027-C500   500 µg 290.00 USD Add To Cart
ALX-380-027-M001   1 mg 395.00 USD Add To Cart
Product Specification
FORMULA: C27H21N3O5
MW: 467.5
CAS NUMBER: 97161-97-2
SOURCE/HOST: Isolated from Nocardiopsis sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, methanol or methylene chloride (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Alkaloid isolated from soil fungi. General, cell permeable protein kinase inhibitor. Potent inhibitor of Ca2+/calmodulin kinase II. Inhibits myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC), and cGMP-dependent protein kinase (PKG). Induces apoptosis.
Product Specific Literature References
K-252a, a potent inhibitor of protein kinase C from microbial origin: H. Kase, et al.; J. Antibiot. (Tokyo) 39, 1059 (1986) Abstract
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. (Tokyo) 39, 1072 (1986) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
K252a is a potent and selective inhibitor of phosphorylase kinase: L.H. Elliott, et al.; BBRC 171, 148 (1990) Abstract
Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926: Y. Hashimoto, et al.; BBRC 181, 423 (1991) Abstract
Differentiation of PC12 cells with K-ras: comparison with nerve growth factor: D.L. Simpson, et al.; J. Neurosci. Res. 28, 486 (1991) Abstract
K-252a inhibits nerve growth factor-induced trk proto-oncogene tyrosine phosphorylation and kinase activity: M.M. Berg, et al.; J. Biol. Chem. 267, 13 (1992) Abstract; Full Text
K-252 compounds: modulators of neurotrophin signal transduction: B. Knusel & F. Hefti; J. Neurochem. 59, 1987 (1992) Abstract
pp42/44MAP kinase is a component of the neurogenic pathway utilized by nerve growth factor in PC12 cells: E.D. Lloyd & M.W. Wooten; J. Neurochem. 59, 1099 (1992) Abstract
K-252a and staurosporine selectively block autophosphorylation of neurotrophin receptors and neurotrophin-mediated responses: S.H. Nye, et al.; Mol. Biol. Cell 3, 677 (1992) Abstract
K-252a and staurosporine promote choline acetyltransferase activity in rat spinal cord cultures: M.C. Glicksman, et al.; J. Neurochem. 61, 210 (1993) Abstract
Staurosporine-related compounds, K252a and UCN-01, inhibit both cPKC and nPKC: K. Mizuno, et al.; FEBS Lett. 330, 114 (1993) Abstract
Ecto-protein kinase and surface protein phosphorylation in PC12 cells: interactions with nerve growth factor: Z. Pawlowska, et al.; J. Neurochem. 60, 678 (1993) Abstract
Staurosporine, K-252a, and K-252b stabilize calcium homeostasis and promote survival of CNS neurons in the absence of glucose: B. Cheng, et al.; J. Neurochem. 62, 1319 (1994) Abstract
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review Abstract
 
 
ALX-380-029 Revised 20-Feb-08
K-252b
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-029-C100   100 µg 98.00 USD Add To Cart
ALX-380-029-C500   500 µg 295.00 USD Add To Cart
ALX-380-029-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C26H19N3O5
MW: 453.5
CAS NUMBER: 99570-78-2
SOURCE/HOST: Isolated from Nocardiopsis sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to brown powder.
SOLUBILITY: Soluble in DMSO, dimethyl formamide or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
General, cell permeable protein kinase inhibitor. Potent inhibitor of Ca2+/calmodulin kinase II. Inhibits myosin light chain kinase, cAMP- dependent protein kinase (PKA), protein kinase C (PKC), and cGMP-dependent protein kinase (PKG).
Product Specific Literature References
K-252b, c and d, potent inhibitors of protein kinase C from microbial origin: S. Nakanishi, et al.; J. Antibiot. (Tokyo) 39, 1066 (1986) Abstract
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. 39, 1072 (1986) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Rüegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926: Y. Hashimoto, et al.; BBRC 181, 423 (1991) Abstract
K-252b selectively potentiates cellular actions and trk tyrosine phosphorylation mediated by neurotrophin-3: B. Knusel, et al.; J. Neurochem. 59, 715 (1992) Abstract
K-252 compounds: modulators of neurotrophin signal transduction: B. Knusel & F. Hefti; J. Neurochem. 59, 1987 (1992) Abstract
Ecto-protein kinase and surface protein phosphorylation in PC12 cells: interactions with nerve growth factor: Z. Pawlowska, et al.; J. Neurochem. 60, 678 (1993) Abstract
Staurosporine, K-252a, and K-252b stabilize calcium homeostasis and promote survival of CNS neurons in the absence of glucose: B. Cheng, et al.; J. Neurochem. 62, 1319 (1994) Abstract
 
 
ALX-270-087 Revised 12-Mar-08
KT5823
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKG Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-087-C100   100 µg 110.00 USD Add To Cart
ALX-270-087-C500   500 µg 330.00 USD Add To Cart
ALX-270-087-M001   1 mg 590.00 USD Add To Cart
Product Specification
FORMULA: C29H25N3O5
MW: 495.5
CAS NUMBER: 126643-37-6
SOURCE/HOST: Semisynthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.