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Protein Kinase C [PKC] / Related Products
You are here: Product Lines > Signal Transduction > Protein Kinase C [PKC] / Related Products
 
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ALX-270-348 Revised 07-Jul-08
LY-333,531 . hydrochloride
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SYNONYMS (S)-13-[(Dimethylamino)methyl-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H-13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)dione . HCl
Ruboxistaurin . hydrochloride
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-348-M001   1 mg Inquire
ALX-270-348-M005   5 mg Inquire
Product Specification
FORMULA: C28H28N4O3 . HCl
MW: 468.6 . 36.5
CAS NUMBER: 169939-93-9
MERCK INDEX: 14: 8290
PURITY: ≥98% (1H-NMR)
APPEARANCE: Red solid
SOLUBILITY: Soluble in DMSO; slightly soluble in 100% ethanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Isozyme selective inhibitor of protein kinase Cβ (PKCβ). Inhibits both the PKCβI (IC50=4.7nM) and PKCβII (IC50=5.9nM) isozymes. 76- and 61-fold more selective for inhibition of PKCβI and PKCβII over PKCα.

Not offered in the US.
Product Specific Literature References
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase : M.R. Jirousek, et al.; J. Med. Chem. 39, 2664 (1996) Abstract
Effects of the protein kinase C beta inhibitor LY333531 on neural and vascular function in rats with streptozotocin-induced diabetes: M.A. Cotter, et al.; Clin Sci (Lond) 103, 311 (2002) Abstract
Protein kinase Cbeta selective inhibitor LY333531 attenuates diabetic hyperalgesia through ameliorating cGMP level of dorsal root ganglion neurons: H. Kim, et al.; Diabetes 52, 2102 (2003) Abstract; Full Text
Role of p90 ribosomal S6 kinase (p90RSK) in reactive oxygen species and protein kinase C beta (PKC-beta)-mediated cardiac troponin I phosphorylation: S. Itoh, et al.; J. Biol. Chem. 280, 24135 (2005) Abstract; Full Text
Protein kinase C beta inhibitor LY333531 attenuates intercellular adhesion molecule-1 and monocyte chemotactic protein-1 expression in the kidney in diabetic rats: Y. Wu, et al.; J. Pharmacol. Sci. 101, 335 (2006) Abstract; Full Text
Ruboxistaurin: C.A. Taulien & S.V. Joy; Drugs Today (Barc) 42, 577 (2006) Abstract
Ruboxistaurin: LY 333531: Drugs R. D. 8, 193 (2007), (Review) Abstract
Role of PKC and TGF-beta receptor in glucose-induced proliferation of smooth muscle cells: Y. Yasuda, et al; BBRC 281, 71 (2001) Abstract
General Literature References
Protein kinase C and the development of diabetic vascular complications: K.J. Way, et al.; Diabet. Med. 18, 945 (2001), Review Abstract
 
 
ALX-162-004 Revised 05-Feb-05
MARCKS Protein (151-175) (bovine brain)
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Substrates
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ALX-162-004-MC05   0.5 mg 120.00 USD Add To Cart
ALX-162-004-M001   1 mg 210.00 USD Add To Cart
Product Specification
SEQUENCE: H-Lys-Lys-Lys-Lys-Lys-Arg-Phe-Ser-Phe-Lys-Lys-Ser-Phe-Lys-Leu-Ser-Gly-Phe-Ser-Phe-Lys-Lys-Asn-Lys-Lys-OH
FORMULA: C147H243N41O31
MW: 3081.8
CAS NUMBER: 125267-21-2
PURITY: ≥98%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Excellent substrate for protein kinase C (PKC). The peptide consists of residues 151-175 of the myristoylated alanine-rich C-kinase substrate (MARCKS) protein phosphorylation site. Protein kinase C isotypes (including PKCε) phosphorylate serines 8, 12 and 19 of this peptide. It is a very weak substrate for cAMP- and cGMP-dependent protein kinase and CaM kinases I, II and III.
Product Specific Literature References
Protein kinase C substrate and inhibitor characteristics of peptides derived from the myristoylated alanine-rich C kinase substrate (MARCKS) protein phosphorylation site domain: J.M. Graff, et al.; J. Biol. Chem. 266, 14390 (1991) Abstract; Full Text
The MARCKS family of cellular protein kinase C substrates: P.J. Blackshear; J. Biol. Chem. 268, 1501 (1993), (Minireview) Abstract; Full Text
Further Categories Containing This Product:
Peptides
 
 
ALX-162-005 Revised 04-Jul-03
MARCKS Protein (159-165) amide (bovine brain)
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Substrates
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ALX-162-005-M001   1 mg 105.00 USD Add To Cart
ALX-162-005-M005   5 mg 420.00 USD Add To Cart
Product Specification
SEQUENCE: H-Phe-Lys-Lys-Ser-Phe-Lys-Leu-NH2
FORMULA: C45H73N11O8
MW: 896.1
PURITY: ≥98%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
The peptide consists of residues 159-165 of the myristoylated alanine-rich C-kinase substrate (MARCKS) protein. It is sufficiently selective for protein kinase C (PKC) to permit specific assay of this enzyme in crude cell extracts and permeabilized cells.
Product Specific Literature References
The MARCKS family of cellular protein kinase C substrates: P.J. Blackshear; J. Biol. Chem. 268, 1501 (1993) Abstract; Full Text
: T. Spencker, et al.; Liebigs Ann. Chem. 237, (1993)
Further Categories Containing This Product:
Peptides
 
 
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-162-006 Revised 07-Apr-08
Melittin (natural)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-162-006-M001   1 mg 40.00 USD Add To Cart
ALX-162-006-M005   5 mg 160.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Ile-Gly-Ala-Val-Leu-Lys-Val-Leu-Thr-Thr-Gly-Leu-Pro-Ala-Leu-Ile-Ser-Trp-Ile-Lys-Arg-Lys-Arg-Gln-Gln-NH2
FORMULA: C131H229N39O31
MW: 2846.5
CAS NUMBER: 37231-28-0
MERCK INDEX: 14: 5824
RTECS: OS3960000
SOURCE/HOST: Isolated from bee venom.
PURITY: ≥85% (HPLC)
APPEARANCE: Off-white to faint tan powder.
PURITY DETAIL: Phospholipase A2 impurity: <5 units per mg solid.
SOLUBILITY: Soluble in PBS (5mg/ml) or water (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Very hygroscopic. Protect from light.
HAZARD: HARMFUL.
Product Description
Causes disruption of normal cellular activity and cell lysis. Binds calmodulin in a calcium-dependent manner. Activates phospholipase A2 (PLA2) and inhibits protein kinase C (PKC) by binding to the catalytic domain in a Mg-ATP sensitive manner. Antirheumatic.
Product Specific Literature References
Rapid purification of calmodulin and S-100 protein by affinity chromatography with melittin immobilized to sepharose: R.L. Kincaid & C.C. Coulson; BBRC 133, 256 (1985) Abstract
Comparison of S100b protein with calmodulin: interactions with melittin and microtubule-associated tau proteins and inhibition of phosphorylation of tau proteins by protein kinase C: J. Baudier, et al.; Biochemistry 26, 2886 (1987) Abstract
Possible mechanisms of action of cobra snake venom cardiotoxins and bee venom melittin: J.E. Fletcher & M.S. Jiang; Toxicon. 31, 669 (1993) Abstract
Melittin and phospholipase A2 from bee (Apis mellifera) venom cause necrosis of murine skeletal muscle in vivo: C.L. Ownby, et al.; Toxicon. 35, 67 (1997) Abstract
Melittin binds to secretory phospholipase A2 and inhibits its enzymatic activity: S.S. Saini, et al.; BBRC 238, 436 (1997) Abstract
Phospholipase A2-independent Ca2+ entry and subsequent apoptosis induced by melittin in human MG63 osteosarcoma cells: S.T. Chu, et al.; Life Sci. 80, 364 (2007) Abstract
Further Categories Containing This Product:
Calmodulin Other Products • PKC Inhibitors • Peptides • PLA2 Activators
 
 
ALX-162-007 Revised 12-May-05
Melittin (synthetic)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-162-007-MC05   0.5 mg 70.00 USD Add To Cart
ALX-162-007-M001   1 mg 120.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Ile-Gly-Ala-Val-Leu-Lys-Val-Leu-Thr-Thr-Gly-Leu-Pro-Ala-Leu-Ile-Ser-Trp-Ile-Lys-Arg-Lys-Arg-Gln-Gln-NH2
FORMULA: C131H229N39O31
MW: 2846.5
CAS NUMBER: 37231-28-0
MERCK INDEX: 14: 5824
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.
Product Description
For technical information see melittin (natural) (Prod. No. ALX-162-006).
Further Categories Containing This Product:
PLA2 Activators • Calmodulin Other Products • PKC Inhibitors • Peptides
 
 
ALX-350-042 Revised 08-Oct-08
Mezerein (high purity)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-042-M001   1 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C38H38O10
MW: 654.7
CAS NUMBER: 34807-41-5
RTECS: HB5425500
SOURCE/HOST: Isolated from Daphne mezereum.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE CARCINOGENIC. IRRITANT.

Product Description
Protein kinase C (PKC) activator. Second stage tumor promoter whereas phorbol-12-myristate 13-acetate (PMA) (Prod. No. ALX-445-004) is a first stage tumor promoter. May be of use for studying phorbol ester receptor isotypes. Induces interleukin-1α. Coinducer of interferon with phytohemagglutinin.
Product Specific Literature References
Studies on the mechanism of skin tumor promotion: evidence for several stages in promotion: T.J. Slaga, et al.; PNAS 77, 3659 (1980) Abstract
Two phorbol ester receptor affinities in partially transformed human urothelial cells and decrease of receptor binding in desensitized cells: B. Christensen, et al.; Experientia 49, 80 (1993) Abstract
Relationship between mezerein-mediated biological responses and phorbol ester receptor occupancy: S. Jaken, et al.; Cancer Res. 43, 11 (1983) Abstract
Modulation of interleukin-1 alpha mRNA expression in mouse epidermis by tumor promoters and antagonists: W.Y. Lee, et al.; Mol. Carcinog. 7, 26 (1993) Abstract
Induction of differentiation in human promyelocytic HL-60 leukemia cells activates p21, WAF1/CIP1, expression in the absence of p53: H. Jiang, et al.; Oncogene 9, 3397 (1994) Abstract
Stimulation of calcium sequestration by mezerein, a protein kinase C activator, in saponized rabbit platelets: H. Nishio, et al.; Gen. Pharmacol. 25, 413 (1994) Abstract
Further Categories Containing This Product:
Carcinogens & Tumor Promoters Other Products • PKC Activators • Natural Products - Other Tumor Promoters
 
 
ALX-270-088 Revised 07-Apr-05
ML-7 . hydrochloride
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SYNONYMS 1-(5-Iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-270-088-M005   5 mg 40.00 USD Add To Cart
ALX-270-088-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C15H17IN2O2S . HCl
MW: 416.0 . 36.5
CAS NUMBER: 110448-33-4
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (can be further diluted with water), 100% ethanol (warm) or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibits smooth-muscle myosin light chain kinase, protein kinase C (PKC), and cAMP-dependent protein kinase (PKA).
Product Specific Literature References
Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase: M. Saitoh, et al.; J. Biol. Chem. 262, 7796 (1987) Abstract; Full Text
Further Categories Containing This Product:
PKC Inhibitors • PKA Inhibitors • Myosin Light Chain Kinase 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
ALX-270-084-M025   25 mg 125.00 USD Add To Cart
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Product Specification
FORMULA: C15H17ClN2O2S . HCl
MW: 324.8 . 36.5
CAS NUMBER: 105637-50-1
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of myosin light chain kinase, protein kinase C (PKC) and protein cAMP-dependent protein kinase (PKA). Also inhibits catecholamine secretion in intact and permeabilized chromaffin cells.
Product Specific Literature References
The modulatory role of myosin light chain phosphorylation in human platelet activation [published erratum appears in Biochem Biophys Res Commun 1987 Jan 15;142(1):287]: M. Saitoh, et al.; BBRC 140, 280 (1986) Abstract
Effects of myosin light-chain kinase inhibitor on catecholamine secretion from rat pheochromocytoma PC12h cells: T. Nagatsu, et al.; BBRC 143, 1045 (1987) Abstract
Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase: M. Saitoh, et al.; J. Biol. Chem. 262, 7796 (1987) Abstract; Full Text
Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle: M. Seto, et al.; Eur. J. Pharmacol. 195, 267 (1991) Abstract
Naphthalenesulfonamide derivatives ML9 and W7 inhibit catecholamine secretion in intact and permeabilized chromaffin cells: J.A. Reig, et al.; Neurochem. Res. 18, 317 (1993) Abstract
Further Categories Containing This Product:
PKC Inhibitors • PKA Inhibitors • Myosin Light Chain Kinase Inhibitors
 
 
ALX-162-009 Revised 04-Jul-07
Myelin Basic Protein (4-14) (bovine)
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SYNONYMS MBP (4-14) (bovine)
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Myelin Basic Protein / Related Products
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ALX-162-009-M001   1 mg 85.00 USD Add To Cart
ALX-162-009-M005   5 mg 330.00 USD