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ALX-155-022

Revised 29-Jun-05

EGF Receptor (human) (651-658) (N-Myristoylated)
SYNONYMS	Epidermal Growth Factor Receptor (human) (651-658) (N-Myristoylated) EGFR (human) (651-658) (N-Myristoylated) HER-1 (human) (651-658) (N-Myristoylated)
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	EGF / EGF Receptor [EGFR] Kinase Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-155-022-M001		1 mg	60.00 USD
ALX-155-022-M005		5 mg	240.00 USD

Product Specification

SEQUENCE:	Myr-Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH
FORMULA:	C₆₀H₁₁₇N₂₁O₁₁
MW:	1308.7
PURITY:	≥97%
APPEARANCE:	White lyophilized powder.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Potent, cell permeable and possibly selective inhibitor of protein kinase C (PKC). This product is the N-terminal myristoylated form of Prod. No. ALX-155-021.

Product Specific Literature References

A novel N-myristylated synthetic octapeptide inhibits protein kinase C activity and partially reverses murine fibrosarcoma cell resistance to adriamycin: C.A. O'Brian, et al.; Invest. New Drugs 9, 169 (1991) Abstract
Cyanobacteria secondary metabolites-the cyanotoxins: W.W. Carmichael; J. Appl. Bacteriol. 72, 445 (1992) Abstract
Inhibition of protein kinase C by N-myristoylated peptide substrate analogs: N.G. Ward & C.A. O'Brian; Biochemistry 32, 11903 (1993) Abstract

Further Categories Containing This Product:

Peptides • PKC Inhibitors

ALX-162-006

Revised 07-Apr-08

Melittin (natural)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-162-006-M001		1 mg	40.00 USD
ALX-162-006-M005		5 mg	160.00 USD

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 A₂impurity: <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)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-162-007-MC05		0.5 mg	70.00 USD
ALX-162-007-M001		1 mg	120.00 USD

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-162-017

Revised 08-Jan-03

N-Myristoyl-Lys-Arg-Thr-Leu-Arg-OH
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-162-017-M001		1 mg	70.00 USD
ALX-162-017-M005		5 mg	280.00 USD

Product Specification

FORMULA:	C₄₂H₈₂N₁₂O₈
MW:	883.2
PURITY:	≥96%
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Effective inhibitor of protein kinase C (PKC)-catalyzed histone phosphorylation.

Product Specific Literature References

Inhibition of IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat by a novel peptide inhibitor of protein kinase C: C.G. Ioannides, et al.; Cell. Immunol. 131, 242 (1990) Abstract
N-myristyl-Lys-Arg-Thr-Leu-Arg: a novel protein kinase C inhibitor: C.A. O'Brian, et al.; Biochem. Pharmacol. 39, 49 (1990) Abstract

Further Categories Containing This Product:

Peptides • Histones / Related Products

ALX-162-018

Revised 04-Jul-03

N-Myristoyl-Phe-Ala-Arg-Lys-Gly-Ala-Leu-Arg-Gln-OH
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-162-018-M001		1 mg	120.00 USD
ALX-162-018-M005		5 mg	480.00 USD

Product Specification

FORMULA:	C₆₀H₁₀₅N₁₇O₁₂
MW:	1256.6
PURITY:	≥97%
APPEARANCE:	White lyophilized powder.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Selective and cell permeable inhibitor of protein kinase C (PKC). The peptide corresponds to the pseudosubstrate domain of PKCα and PKCβ subtypes.

Product Specific Literature References

A myristoylated pseudosubstrate peptide, a novel protein kinase C inhibitor: T. Eichholtz, et al.; J. Biol. Chem. 268, 1982 (1993) Abstract; Full Text

Further Categories Containing This Product:

Peptides

ALX-165-009

Revised 20-Nov-06

Protein Kinase C (19-31)
SYNONYMS	PKC (19-31)
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-165-009-M001		1 mg	50.00 USD
ALX-165-009-M005		5 mg	200.00 USD

Product Specification

SEQUENCE:	H-Arg-Phe-Ala-Arg-Lys-Gly-Ala-Leu-Arg-Gln-Lys-Asn-Val-OH
FORMULA:	C₆₇H₁₁₈N₂₆O₁₆
MW:	1543.8
SOURCE/HOST:	Synthetic.
PURITY:	≥95%
APPEARANCE:	Lyophilized.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Pseudosubstrate prototope of the PKC regulatory domain. Inhibitor of protein kinase C (PKC).

Product Specific Literature References

Protein kinase C contains a pseudosubstrate prototope in its regulatory domain: C. House & B.E. Kemp; Science 238, 1726 (1987) Abstract

Further Categories Containing This Product:

Peptides

ALX-165-010

Revised 20-Nov-06

Protein Kinase C (19-36)
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-165-010-M001		1 mg	110.00 USD
ALX-165-010-M005		5 mg	440.00 USD

Product Specification

SEQUENCE:	H-Arg-Phe-Ala-Arg-Lys-Gly-Ala-Leu-Arg-Gln-Lys-Asn-Val-His-Glu-Val-Lys-Asn-OH
FORMULA:	C₉₃H₁₅₉N₃₅O₂₄
MW:	2151.5
SOURCE/HOST:	Synthetic.
PURITY:	≥97%
APPEARANCE:	Lyophilized.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Pseudosubstrate prototope of the protein kinase C (PKC) regulatory domain. Specifically inhibits both autophosphorylation and protein substrate phosphorylation. Does not inhibit cAMP-dependent protein kinase (PKA). Longer sequence and less potent inhibitor than Prod. No. ALX-165-009.

Product Specific Literature References

Protein kinase C contains a pseudosubstrate prototope in its regulatory domain: C. House & B.E. Kemp; Science 238, 1726 (1987) Abstract
A protein kinase C pseudosubstrate peptide inhibits phosphorylation of the CD3 antigen in streptolysin-O-permeabilized human T lymphocytes: D.R. Alexander, et al.; Biochem. J. 260, 893 (1989) Abstract

Further Categories Containing This Product:

Peptides

ALX-260-155

Revised 23-Jun-08

PKCζ Pseudosubstrate (Myristoylated)
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-260-155-M001		1 mg	140.00 USD

Product Specification

SEQUENCE:	Myr-Ser-Ile-Tyr-Arg-Arg-Gly-Ala-Arg-Arg-Trp-Arg-Lys-Leu-OH
FORMULA:	C₉₀H₁₅₄N₃₀O₁₇
MW:	1928.4
PEPTIDE CONTENT:	≥60%
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white powder.
FORMULATION:	Counter Ion: TFA
SOLUBILITY:	Soluble in water or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Selective cell permeable inhibitor of PKCζ. Activates eNOS (NOS III) through Akt phosphorylation and can be considered as a new class of nitric oxide production activators in endothelial cells.

Product Specific Literature References

Peptides modified by myristoylation activate eNOS in endothelial cells through Akt phosphorylation: K. Krotova, et al.; Br. J. Pharmacol. 148, 732 (2006) Abstract

Further Categories Containing This Product:

NOS Cofactors & Activators

ALX-270-016

Revised 05-May-08

H-7 . dihydrochloride
SYNONYMS	(±)-1-(5-Isoquinolinesulfonyl)-2-methylpiperazine . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-016-M010		10 mg	60.00 USD
ALX-270-016-M025		25 mg	120.00 USD

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
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
ALX-270-017-M005		5 mg	55.00 USD

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;