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cGMP-dependent Protein Kinase [PKG] / Related Products
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ALX-270-067 Revised 04-Mar-05
H-8 . dihydrochloride
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SYNONYMS N-[2-(Methylamino)ethyl]-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-270-067-M005   5 mg 40.00 USD Add To Cart
ALX-270-067-M025   25 mg 160.00 USD Add To Cart
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Product Specification
FORMULA: C12H15N3O2S . 2HCl
MW: 265.3 . 73.0
CAS NUMBER: 113276-94-1
PURITY: ≥98%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent inhibitor of cAMP- and cGMP-dependent protein kinases (PKA and PKG). Also inhibits myosin light chain kinase.
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
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract
Specific binding of a novel compound, N-[2-(methylamino)ethyl]-5- isoquinolinesulfonamide (H-8) to the active site of cAMP-dependent protein kinase: M. Hagiwara, et al.; Mol. Pharmacol. 31, 523 (1987) Abstract
Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives: M. Hagiwara, et al.; Mol. Pharmacol. 32, 7 (1987) Abstract
Differential growth inhibition of isoquinolinesulfonamides H-8 and H-7 towards multidrug-resistant P388 murine leukaemia cells: M. Ido, et al.; Br. J. Cancer 64, 1103 (1991) Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996) Abstract; Full Text
Further Categories Containing This Product:
PKG Inhibitors • Myosin Light Chain Kinase Inhibitors
 
 
ALX-270-017 Revised 27-Apr-06
H-89 . dihydrochloride
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SYNONYMS N-[2-(p-Bromocinnamylamino)ethyl]-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-270-017-M001   1 mg 22.00 USD Add To Cart
ALX-270-017-M005   5 mg 55.00 USD Add To Cart
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Product Specification
FORMULA: C20H20BrN3O2S . 2HCl
MW: 446.4 . 73.0
CAS NUMBER: 127243-85-0
PURITY: ≥97% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or methanol; also soluble in ethanol: water (1:1).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for at least 3-4 weeks when stored at +4°C. We recommend using a fresh solution each day.

Product Description
Cell permeable potent and selective inhibitor of cAMP- and cGMP-dependent protein kinases (PKA and PKG) and protein kinase Cµ (PKCµ). In contrast, most other protein kinase C (PKC) isotypes are much more weakly inhibited. Also inhibits Ca2+/calmodulin-dependent protein kinase II, casein kinase I and myosin light chain kinase. Induces apoptosis.
Product Specific Literature References
Polyamines differentially inhibit cyclic AMP-dependent protein kinase- mediated phosphorylation in the brain of the tobacco hornworm, Manduca sexta: W.L. Combest, et al.; J. Neurochem. 51, 1581 (1988) Abstract
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5- isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma: T. Chijiwa, et al.; J. Biol. Chem. 265, 5267 (1990) Abstract; Full Text
A selective inhibitor of cyclic AMP-dependent protein kinase, N-[2- bromocinnamyl(amino)ethyl]-5-isoquinolinesulfonamide (H-89), inhibits phosphatidylcholine biosynthesis in HeLa cells: C.C. Geilen; FEBS Lett. 309, 381 (1992) Abstract
Protein kinase A inhibitors enhance radiation-induced apoptosis: D. Findik, et al.; J. Cell. Biochem. 57, 12 (1995) Abstract
Characterization of activators and inhibitors of protein kinase C mu: F.-J. Johannes, et al.; Eur. J. Biochem. 227, 303 (1995) Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996) Abstract; Full Text
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:
CAM Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Casein Kinase Inhibitors
 
 
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
Ordering Information
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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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
Further Categories Containing This Product:
PKG Substrates • Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products • Peptides
 
 
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:
Peptides • PKG 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 Substrates • Peptides
 
 
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • PKA Inhibitors • CAM Kinase Inhibitors • PKG Inhibitors • Myosin Light Chain Kinase Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Staurosporine / Related Products • Alkaloids
 
 
ALX-380-029 Revised 20-Feb-08
K-252b
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
Ordering Information
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
Further Categories Containing This Product:
PKA Inhibitors • CAM Kinase Inhibitors • PKG Inhibitors • Myosin Light Chain Kinase Inhibitors • Staurosporine / Related Products • Alkaloids
 
 
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.

Product Description
Potent and selective inhibitor of cGMP-dependent protein kinase (PKG).
Product Specific Literature References
K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases: H. Kase, et al.; BBRC 142, 436 (1987) Abstract
Further Categories Containing This Product: