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PKC Inhibitors
You are here: Product Lines > Signal Transduction > Protein Kinase C [PKC] / Related Products > PKC 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:
PKA Inhibitors • PKG Inhibitors • Myosin Light Chain Kinase 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
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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 • PKG Inhibitors • Casein Kinase Inhibitors • PKC Inhibitors • Myosin Light Chain Kinase Inhibitors • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-270-019 Revised 27-Apr-06
Bisindolylmaleimide I . hydrochloride
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SYNONYMS GF-109203X . HCl
Gö 6850 . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-019-M001   1 mg 45.00 USD Add To Cart
ALX-270-019-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C25H24N4O2 . HCl
MW: 412.5 . 36.5
PURITY: ≥98%
APPEARANCE: Orange to red powder.
SOLUBILITY: Soluble in DMSO or methanol. Slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Water soluble form of bisindolylmaleimide I (Prod. No. ALX-270-049), a protein kinase C (PKC) inhibitor.
Product Specific Literature References
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C: D. Toullec, et al.; J. Biol. Chem. 266, 15771 (1991) Abstract; Full Text
Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model: S. Kuchera, et al.; Agents Actions 39, C169 (1993) Abstract
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
 
 
ALX-270-020 Revised 07-Dec-04
Bisindolylmaleimide IX . methanesulfonate
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SYNONYMS Ro 31-8220 . methanesulfonate
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-020-M001   1 mg 45.00 USD Add To Cart
ALX-270-020-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C25H23N5O2S . CH4O3S
MW: 457.6 . 96.1
CAS NUMBER: 138489-18-6
PURITY: ≥98%
APPEARANCE: Red solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective inhibitor of protein kinase C (PKC).
Product Specific Literature References
Atypical isoforms of pKc and insulin secretion from pancreatic beta- cells: evidence using Go 6976 and Ro 31-8220 as Pkc inhibitors: T.E. Harris, et al.; BBRC 227, 672 (1996) Abstract
 
 
ALX-270-021 Revised 03-Jul-08
Gö 6976
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SYNONYMS 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-021-MC05   0.5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C24H18N4O
MW: 378.4
CAS NUMBER: 136194-77-9
PURITY: ≥95% (HPLC)
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in DMSO (25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for at least 3-4 months when  stored at -20°C.
HANDLING: Protect from light.

Product Description
Very potent protein kinase C (PKC) inhibitor with high selectivity for the PKC isotypes (α, β and γ). Potent antagonist of HIV-1 induction.
Product Specific Literature References
Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C: J. Kleinschroth, et al.; Bioorg. Med. Chem. Lett 3, 1959 (1993)
Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976: G. Martiny-Baron, et al.; J. Biol. Chem. 268, 9194 (1993) Abstract; Full Text
Go 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low- level-producing reservoir cells in vitro: K.O. Qatsha, et al.; PNAS 90, 4674 (1993) Abstract
N-protein kinase C isoenzymes may be involved in the regulation of various neutrophil functions: K. Wenzel-Seifert, et al.; BBRC 200, 1536 (1994) Abstract
Atypical isoforms of pKc and insulin secretion from pancreatic beta- cells: evidence using Go 6976 and Ro 31-8220 as Pkc inhibitors: T.E. Harris, et al.; BBRC 227, 672 (1996) Abstract
 
 
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:
PKG Inhibitors • Casein Kinase Inhibitors • PKC Inhibitors • Myosin Light Chain Kinase Inhibitors
 
 
ALX-270-040 Revised 04-Feb-05
H-7, Iso-, . dihydrochloride
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SYNONYMS Iso-H-7 . 2HCl
(±)-1-(5-Isoquinolinesulfonyl)-3-methylpiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-040-M010   10 mg 120.00 USD Add To Cart
ALX-270-040-M025   25 mg 270.00 USD Add To Cart
Product Specification
FORMULA: C14H17N3O2S . 2HCl
MW: 291.4 . 73.0
CAS NUMBER: 8447-73-6
PURITY: ≥99%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Inhibitor of protein kinase C (PKC), but less potent than H-7 (Prod. No. ALX-270-016).
Product Specific Literature References
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
 
 
ALX-270-049 Revised 13-Nov-06
Bisindolylmaleimide I
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SYNONYMS GF-109203X
Gö 6850
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-049-M001   1 mg 45.00 USD Add To Cart
ALX-270-049-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C25H24N4O2
MW: 412.5
CAS NUMBER: 133052-90-1
PURITY: ≥98%
APPEARANCE: Orange solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (Ki=10nM) over several serine/threonine and tyrosine kinases as compared to staurosporine (Prod. No. ALX-380-014). Acts as a competetive inhibitor for the ATP-binding site of PKC. Also inhibits telomerase activity in quercetin (Prod. No. ALX-385-001), H-89 (Prod. No. ALX-270-017), or herbimycin A (Prod. No. ALX-350-029) treated NPC-076 cells. Inhibits protein kinase A at much higher concentrations (Ki=2µM).
Product Specific Literature References
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C: D. Toullec, et al.; J. Biol. Chem. 266, 15771 (1991) Abstract; Full Text
Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model: S. Kuchera, et al.; Agents Actions 39, C169 (1993) Abstract
The bisindolylmaleimide GF 109203X, a selective inhibitor of protein kinase C, does not inhibit the potentiating effect of phorbol ester on ethanol-induced phospholipase C-mediated hydrolysis of phosphatidylethanolamine: Z. Kiss, et al.; Biochim. Biophys. Acta 1265, 93 (1995) Abstract
Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance: V. Gekeler, et al.; Br. J. Cancer 74, 897 (1996) Abstract
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
Suprabasin, a Novel Epidermal Differentiation Marker and Potential Cornified Envelope Precursor: G.T. Park, et al.; JBC 277, 45195 (2002) Abstract; Full Text
 
 
ALX-270-050 Revised 26-May-08
Bisindolylmaleimide II
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-050-M001   1 mg 45.00 USD Add To Cart
ALX-270-050-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C27H26N4O2
MW: 438.5
PURITY: ≥97% (mixture of 2 isomers)
APPEARANCE: Orange solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

 
 
ALX-270-051 Revised 18-Jan-08
Bisindolylmaleimide III
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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-270-051-M001   1 mg 45.00 USD