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PKA Inhibitors
You are here: Product Lines > Signal Transduction > cAMP Pathways > cAMP-dependent Protein Kinase [PKA] / Related Products > PKA Inhibitors
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ALX-151-014 Revised 15-Dec-04
cAMP-dependent Protein Kinase Inhibitor (5-24)
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SYNONYMS PKA Inhibitor (5-24)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-151-014-MC05   0.5 mg 90.00 USD Add To Cart
ALX-151-014-M001   1 mg 160.00 USD Add To Cart
Product Specification
SEQUENCE: H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-OH
FORMULA: C94H148N32O31
MW: 2222.4
PURITY: ≥97%
APPEARANCE: White to off-white powder.
FORMULATION: Lyophilized.
SOLUBILITY: Soluble in water or 5 % acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.
Product Description
Potent inhibitor of cAMP-dependent protein kinase (PKA). The peptide corresponds to the active site of the skeletal muscle inhibitor protein.
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase: H.-C. Cheng, et al.; J. Biol. Chem. 261, 989 (1986) Abstract; Full Text
Phosphorylation of Avena phytochrome in vitro as a probe of light- induced conformational changes: Y.S. Wong, et al.; J. Biol. Chem. 261, 12089 (1986) Abstract; Full Text
Further Categories Containing This Product:
Peptides
 
 
ALX-151-016 Revised 17-Jan-05
cAMP-dependent Protein Kinase Inhibitor (5-22) amide
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SYNONYMS PKA Inhibitor (5-22) amide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-151-016-MC05   0.5 mg 110.00 USD Add To Cart
ALX-151-016-M001   1 mg 180.00 USD Add To Cart
Product Specification
SEQUENCE: H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-NH2
FORMULA: C84H137N29O26
MW: 1969.2
PURITY: ≥97%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Potent inhibitor of cAMP-dependent protein kinase (PKA).
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase: H.-C. Cheng, et al.; J. Biol. Chem. 261, 989 (1986) Abstract; Full Text
Primary structural determinants essential for potent inhibition of cAMP- dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitor protein: D.B. Glass, et al.; J. Biol. Chem. 264, 8802 (1989) Abstract; Full Text
Further Categories Containing This Product:
Peptides
 
 
ALX-151-017 Revised 15-Dec-04
cAMP-dependent Protein Kinase Inhibitor (14-24) amide
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SYNONYMS PKA Inhibitor (14-24) amide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-151-017-M001   1 mg 90.00 USD Add To Cart
ALX-151-017-M005   5 mg 360.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-NH2
FORMULA: C49H86N24O15
MW: 1251.4
PURITY: ≥97%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Further Categories Containing This Product:
Peptides
 
 
ALX-151-018 Revised 13-Feb-06
cAMP-dependent Protein Kinase Inhibitor (5-24) amide
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SYNONYMS PKA Inhibitor (5-24) amide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-151-018-MC05   0.5 mg 90.00 USD Add To Cart
ALX-151-018-M001   1 mg 160.00 USD Add To Cart
Product Specification
SEQUENCE: H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-NH2
FORMULA: C94H149N33O30
MW: 2221.4
PURITY: ≥97%
APPEARANCE: White to off-white lyophilized powder.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Specific Literature References
A potent synthetic peptide inhibitor of the cAMP-dependent protein kinase: H.-C. Cheng, et al.; J. Biol. Chem. 261, 989 (1986) Abstract; Full Text
Further Categories Containing This Product:
Peptides
 
 
ALX-151-021 Revised 14-Aug-02
H-Arg-Gly-Tyr-Ser-Leu-Gly-OH
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-151-021-M001   1 mg 40.00 USD Add To Cart
ALX-151-021-M005   5 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C28H45N9O9
MW: 651.7
PURITY: ≥97%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cAMP-dependent protein kinase (PKA).
Product Specific Literature References
Synthetic hexapeptide substrates and inhibitors of 3':5'-cyclic AMP- dependent protein kinase: B.E. Kemp, et al.; PNAS 73, 1038 (1976) Abstract
Synthetic peptide substrates of the cAMP-dependent protein kinase: B.E. Kemp, et al.; Fed. Proc. 35, 1384 (1976)
Further Categories Containing This Product:
Peptides
 
 
ALX-165-024 Revised 06-Feb-05
PKI-tide
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-165-024-M001   1 mg 75.00 USD Add To Cart
ALX-165-024-M005   5 mg 290.00 USD Add To Cart
Product Specification
SEQUENCE: H-Ile-Ala-Ala-Gly-Arg-Thr-Gly-Arg-Arg-Gln-Ala-Ile-His-Asp-Ile-Leu-Val-Ala-Ala-OH
FORMULA: C85H149N31O24
MW: 1989.3
PURITY: ≥98%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Specific inhibitor of cAMP-dependent protein kinase (PKA).
Product Specific Literature References
Calcium . calmodulin-dependent protein kinase II and calcium . phospholipid-dependent protein kinase activities in rat tissues assayed with a synthetic peptide: Y. Hashimoto & T.R. Soderling; Arch. Biochem. Biophys. 252, 418 (1987) Abstract
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Peptides
 
 
ALX-270-016 Revised 05-May-08
H-7 . dihydrochloride
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SYNONYMS (±)-1-(5-Isoquinolinesulfonyl)-2-methylpiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-016-M010   10 mg 60.00 USD Add To Cart
ALX-270-016-M025   25 mg 120.00 USD Add To Cart
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Product Specification
FORMULA: C14H17N3O2S . 2 HCl
MW: 291.4 . 73.0
CAS NUMBER: 108930-17-2
PURITY: ≥98%
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in water, 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of protein kinase C (PKC), cAMP- and cGMP-dependent protein kinase (PKA and PKG). Also inhibits myosin light chain kinase. Induces apoptotic DNA fragmentation and cell death. Inhibits telomerase activity in treated NPC-076 cells.
Product Specific Literature References
1-(5-Isoquinolinesulfonyl)-2-methylpiperazine (H-7) is a selective inhibitor of protein kinase C in rabbit platelets: S. Kawamoto & H. Hidaka; BBRC 125, 258 (1984) Abstract
Stimulus-dependent inhibition of platelet aggregation by the protein kinase C inhibitors polymyxin B, H-7 and staurosporine: C. Schächtele, et al.; BBRC 151, 542 (1988) Abstract
Blockade of the spinal excitatory effect of cAMP on the startle reflex by intrathecal administration of the isoquinoline sulfonamide H-8: comparison to the protein kinase C inhibitor H-7: N.M. Boulis & M. Davis; Brain Res. 525, 198 (1990) Abstract
Potent selective inhibition of 7-O-methyl UCN-01 against protein kinase C: I. Takahashi, et al.; J. Pharmacol. Exp. Ther. 255, 1218 (1990) Abstract
The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source: J. Quick, et al.; BBRC 187, 657 (1992) Abstract
Modulation of neutrophil superoxide generation by inhibitors of protein kinase C, calmodulin, diacylglycerol and myosin light chain kinases, and peptidyl prolyl cis-trans isomerase: H. Bergstrand, et al.; J. Pharmacol. Exp. Ther. 263, 1334 (1992) Abstract
C. Gimond and M. Aumailley; Exp. Cell Res. 203, 365 (1992) 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
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
Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; Biochem. Biophys. Res. Commun. 241, 730 (1997) Abstract
Further Categories Containing This Product:
PKA Inhibitors • Myosin Light Chain Kinase Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products
 
 
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
Ordering Information
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 • Casein Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKG Inhibitors • PKC Inhibitors • Apoptosis Inducers & Inhibitors Other Products
 
 
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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:
PKC Inhibitors • Casein Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKG Inhibitors
 
 
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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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:
Myosin Light Chain Kinase Inhibitors • PKG Inhibitors
 
 
ALX-270-068 Revised 28-Jan-05
H-9 . dihydrochloride