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PKA Inhibitors
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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:
Myosin Light Chain Kinase Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • PKA 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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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-270-039 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 • PKG Inhibitors • Casein Kinase 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:
PKG Inhibitors • Myosin Light Chain Kinase Inhibitors
 
 
ALX-270-068 Revised 28-Jan-05
H-9 . dihydrochloride
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SYNONYMS N-(2-Aminoethyl)-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-068-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C11H13N3O2S . 2HCl
MW: 251.3 . 73.0
CAS NUMBER: 84468-17-7
PURITY: ≥97%
APPEARANCE: Lyophilized solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent inhibitor of cyclic nucleotide-dependent protein kinases.
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
N-(2-Aminoethyl)-5-isoquinolinesulfonamide, a newly synthesized protein kinase inhibitor, functions as a ligand in affinity chromatography. Purification of Ca2+-activated, phospholipid-dependent and other protein kinases: M. Inagaki, et al.; J. Biol. Chem. 260, 2922 (1985) Abstract; Full Text
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract
Stimulation of phosphorylation of rat brush-border membrane proteins by Escherichia coli heat-stable enterotoxin, cholera enterotoxin and cyclic nucleotides, and its inhibition by protein kinase inhibitors, isoquinolinesulfonamides: T. Hirayama, et al.; Microb. Pathog. 8, 421 (1990) Abstract
 
 
ALX-270-069 Revised 04-Feb-05
HA-100 . dihydrochloride
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SYNONYMS 1-(5-Isoquinolinylsulfonyl)piperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-069-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C13H15N3O2S . 2HCl
MW: 277.3 . 73.0
CAS NUMBER: 84468-24-6
PURITY: ≥99%
APPEARANCE: Lyophilized solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of myosin light chain kinase, cAMP-dependent protein kinase (PKA) and protein kinase C (PKC).
Product Specific Literature References
Role of protein kinases in stimulation of human polymorphonuclear leukocyte oxidative metabolism by various agonists. Differential effects of a novel protein kinase inhibitor: C. Gerard, et al.; J. Clin. Invest. 77, 61 (1986) 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
Further Categories Containing This Product:
PKC Inhibitors • Myosin Light Chain 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
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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-270-075 Revised 08-Oct-08
KT5720
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-075-C100   100 µg 110.00 USD Add To Cart
ALX-270-075-C500   500 µg 330.00 USD Add To Cart
ALX-270-075-M001   1 mg 590.00 USD Add To Cart
Product Specification
FORMULA: C32H31N3O5
MW: 537.6
CAS NUMBER: 108068-98-0
SOURCE/HOST: Semisynthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol (5mg/ml) or DMSO (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Potent, reversible, cell permeable and selective inhibitor of cAMP-dependent protein kinase (PKA).
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
Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells: D.M. Gadbois, et al.; PNAS 89, 8626 (1992) Abstract
Effects of selective inhibition of protein kinase C, cyclic AMP- dependent protein kinase, and Ca(2+)-calmodulin-dependent protein kinase on neurite development in cultured rat hippocampal neurons: L. Cabell and G. Audesirk; Int. J. Dev. Neurosci. 11, 357 (1993), (Review) Abstract
Further Categories Containing This Product:
Staurosporine / Related Products • Alkaloids
 
 
ALX-270-081 Revised 20-Dec-02
MDL-27,032
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SYNONYMS 4-Propyl-5-(4-pyridinyl)-2(3H)-oxazolone
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-081-C100   100 µg 50.00 USD Add To Cart
ALX-270-081-M001   1 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C11H12N2O2
MW: 204.2
PURITY: ≥97%
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent vasodilator. Inhibitor of protein kinase C and cAMP-dependent protein kinase (PKA). Inhibition is competitive with ATP and not competitive with phospholipid, diacylglycerol, phorbol ester and calcium.
Product Specific Literature References
MDL 27,032 [4-propyl-5-(4-pyridinyl)-2(3H)-oxazolone], an active site- directed inhibitor of protein kinase C and cyclic AMP-dependent protein kinase that relaxes vascular smooth muscle: P.J. Robinson, et al.; J. Pharmacol. Exp. Ther. 255, 1392 (1990) Abstract
Further Categories Containing This Product:
PKA Inhibitors
 
 
ALX-270-084 Revised 28-Jan-05
ML-9 . hydrochloride
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SYNONYMS 1-(5-Chloronaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Myelin Basic Protein / Related Products
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ALX-270-084-M010   10 mg 65.00 USD Add To Cart