ALEXIS Biochemicals: STO-609

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ALX-151-029

Revised 23-Nov-06

Autocamtide-2-Related Inhibitory Peptide
SYNONYMS	AIP
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	CAM Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-151-029-M001		1 mg	75.00 USD
ALX-151-029-M005		5 mg	300.00 USD

Product Specification

SEQUENCE:	H-Lys-Lys-Ala-Leu-Arg-Arg-Gln-Glu-Ala-Val-Asp-Ala-Leu-OH
FORMULA:	C₆₄H₁₁₆N₂₂O₁₉
MW:	1497.8
PURITY:	≥98%
APPEARANCE:	Lyophilized.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Highly specific and potent inhibitor of Ca²⁺/calmodulin-dependent protein kinase II without affecting cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and Ca²⁺/calmodulin-dependent protein kinase IV.

Product Specific Literature References

A novel highly specific and potent inhibitor of calmodulin-dependent protein kinase II: A. Ishida, et al.; BBRC 212, 806 (1995) Abstract
Stabilization of calmodulin-dependent protein kinase II through the autoinhibitory domain: A. Ishida & H. Fujisawa; J. Biol. Chem. 270, 2163 (1995) Abstract; Full Text

Further Categories Containing This Product:

Peptides

ALX-151-030

Revised 05-Feb-08

Autocamtide-2-Related Inhibitory Peptide (Myristoylated)
SYNONYMS	AIP Myristoylated
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	CAM Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-151-030-MC05		0.5 mg	90.00 USD

Product Specification

SEQUENCE:	Myr-Lys-Lys-Ala-Leu-Arg-Arg-Gln-Glu-Ala-Val-Asp-Ala-Leu-OH
FORMULA:	C₇₈H₁₄₂N₂₂O₂₀
MW:	1708.1
PURITY:	≥98%
APPEARANCE:	Lyophilized.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Corresponds to Prod. No. ALX-151-029 but this one is N-terminal myristoylated to increase cell permeability.

Further Categories Containing This Product:

Peptides

ALX-153-010

Revised 16-Feb-05

[Ala286]-Ca2+/Calmodulin-dependent Protein Kinase II (281-302)
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	CAM Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-153-010-MC01		0.1 mg	50.00 USD
ALX-153-010-M001		1 mg	190.00 USD

Product Specification

SEQUENCE:	H-Met-His-Arg-Gln-Glu-Ala-Val-Asp-Cys-Leu-Lys-Lys-Phe-Asn-Ala-Arg-Arg-Lys-Leu-Lys-Gly-Ala-OH
FORMULA:	C₁₁₁H₁₉₁N₃₉O₂₉S₂
MW:	2600.1
PURITY:	≥97%
APPEARANCE:	White lyophilized powder.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Inhibitor of Ca²⁺/calmodulin-dependent protein kinase II catalytic fragment, competitive with ATP. The sequence for this product matches that of the original article describing this "CaM kinase II inhibitor" peptide.

Product Specific Literature References

Functional determinants in the autoinhibitory domain of calcium/calmodulin-dependent protein kinase II. Role of His282 and multiple basic residues: M.K. Smith, et al.; J. Biol. Chem. 267, 1761 (1992) Abstract; Full Text

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Peptides

ALX-153-006

Revised 20-Sep-05

Ca2+/Calmodulin-dependent Protein Kinase II (290-309)
SYNONYMS	CaM Kinase II (290-309) CAMK2 (290-309)
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	CAM Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-153-006-MC01		0.1 mg	40.00 USD
ALX-153-006-M001		1 mg	120.00 USD

Product Specification

SEQUENCE:	H-Leu-Lys-Lys-Phe-Asn-Ala-Arg-Arg-Lys-Leu-Lys-Gly-Ala-Ile-Leu-Thr-Thr-Met-Leu-Ala-OH
FORMULA:	C₁₀₃H₁₈₅N₃₁O₂₄S
MW:	2273.9
PURITY:	≥98%
APPEARANCE:	White lyophilized powder.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Potent inhibitor of Ca²⁺/calmodulin-dependent protein kinase II.

Product Specific Literature References

Calcium/calmodulin-dependent protein kinase II. Characterization of distinct calmodulin binding and inhibitory domains: M.E. Payne, et al.; J. Biol. Chem. 263, 7190 (1988) Abstract; Full Text

Further Categories Containing This Product:

Peptides

ALX-380-284

Revised 08-Apr-08

Cyclosporin D
SYNONYMS	Val²-cyclosporin 7-L-Valine-cyclosporin A
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Immunomodulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-284-M001		1 mg	80.00 USD
ALX-380-284-M005		5 mg	320.00 USD

Product Specification

FORMULA:	C₆₃H₁₁₃N₁₁O₁₂
MW:	1216.6
CAS NUMBER:	63775-96-2
MERCK INDEX:	14: 2752
SOURCE/HOST:	Isolated from Fusarium solani.
PURITY:	≥95% (HPLC)
APPEARANCE:	Colorless to off-white crystalline solid.
SOLUBILITY:	Soluble in 100% ethanol, acetone or ethyl acetate; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	MAY BE TERATOGENIC. TOXIC. MAY BE CARCINOGENIC.

Product Description

Weak immunosuppressor. Potent inhibitor of tumor promoting phorbol ester TPA/PMA (Prod. No. ALX-445-004) in vivo. Potent inhibitor of Ca²⁺/calmodulin dependent EF-2 phosphorylation in vitro.

Product Specific Literature References

Further Categories Containing This Product:

CAM Kinase Inhibitors • MPTP [Mitochondrial Transition Pore] / Related Products

ALX-380-286

Revised 08-Apr-08

Cyclosporin H
SYNONYMS	Csh-cyclosporin 5-(N-Methyl-D-valine)-cyclosporin A
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Immunomodulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-286-M001		1 mg	80.00 USD
ALX-380-286-M005		5 mg	320.00 USD

Product Specification

FORMULA:	C₆₂H₁₁₁N₁₁O₁₂
MW:	1202.6
CAS NUMBER:	83602-39-5
SOURCE/HOST:	Isolated from Fusarium solani.
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in 100% ethanol, acetone or ethyl acetate; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	MAY BE TERATOGENIC. TOXIC. MAY BE CARCINOGENIC.

Product Description

Immunologically inactive. Does not bind to immunophilin. Potent inhibitor of tumor promoting phorbol ester TPA/PMA (Prod. No. ALX-445-004) in mouse skin in vivo. Potent inhibitor of Ca²⁺/calmodulin dependent EF-2 phosphorylation in vitro. Potent and selective antagonist of formyl peptide receptor. Inhibits formyl peptide-induced superoxide formation.

Product Specific Literature References

The weak immunosuppressant cyclosporine D as well as the immunologically inactive cyclosporine H are potent inhibitors in vivo of phorbol ester TPA-induced biological effects in mouse skin and of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro: M. Gschwendt, et al.; BBRC 150, 545 (1988) Abstract
Differential inhibition of human neutrophil activation by cyclosporins A, D, and H. Cyclosporin H is a potent and effective inhibitor of formyl peptide-induced superoxide formation: K. Wenzel-Seifert, et al.; J. Immunol. 147, 1940 (1991) Abstract
Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L- leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E: K. Wenzel-Seifert & R. Seifert; J. Immunol. 150, 4591 (1993) Abstract
Cyclosporin H is a potent and selective competitive antagonist of human basophil activation by N-formyl-methionyl-leucyl-phenylalanine: A. de Paulis, et al.; J. Allergy Clin. Immunol. 98, 152 (1996) Abstract
Cyclosporin H, Boc-MLF and Boc-FLFLF are antagonists that preferentially inhibit activity triggered through the formyl peptide receptor: A.L. Stenfeldt, et al.; Inflammation 30, 224 (2007) Abstract

Further Categories Containing This Product:

Antibiotics - Apoptosis Inducers & Inhibitors • Antibiotics - Nitric Oxide Pathway Modulators • CAM Kinase Inhibitors • MPTP [Mitochondrial Transition Pore] / Related Products • Non-apoptotic Cell Death / Necrosis

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; 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-270-071

Revised 06-Aug-07

HA-1077 . dihydrochloride
SYNONYMS	Fasudil 1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Rho-associated Protein Kinases [ROCK] / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-071-M001		1 mg	21.00 USD
ALX-270-071-M005		5 mg	63.00 USD

Product Specification

FORMULA:	C₁₄H₁₇N₃O₂S . 2HCl
MW:	291.4 . 73.0
CAS NUMBER:	103745-39-7
MERCK INDEX:	14: 3942
PURITY:	≥98%
APPEARANCE:	Lyophilized.
SOLUBILITY:	Soluble in water, methanol or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Inhibitor of myosin light chain kinase and Ca²⁺/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ. Cell permeable Ca²⁺ antagonist with antivasospastic properties.

Product Specific Literature References

The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs: O. Shibuya, et al.; Acta Neurochir. 90, 53 (1988) Abstract
Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase: T. Asano, et al.; Br. J. Pharmacol. 98, 1091 (1989) Abstract
Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator: Y. Sasaki & Y. Sasaki; BBRC 171, 1182 (1990) Abstract
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
A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture: M. Shirotani, et al.; J. Pharmacol. Exp. Ther. 259, 738 (1991) Abstract
Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle: S. Takizawa, et al.; Eur. J. Pharmacol. 250, 431 (1993) Abstract
Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells: H. Nagumo, et al.; Am. J. Physiol. Cell. Physiol. 278, C57 (2000) Abstract
Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCbetaI, PKCbetaII and PKCzeta in human neutrophils: X. Siomboing, et al.; Mediators Inflamm. 10, 315 (2001) Abstract
Effects of HA-1077 and Y-27632, Two Rho-Kinase Inhibitors, in the Human Umbilical Artery: M. Ark, et al.; Cell Biochem. Biophys. 41, 331 (2004) Abstract

Further Categories Containing This Product:

CAM Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors

ALX-380-027

Revised 09-May-08

K-252a
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-027-C100		100 µg	98.00 USD
ALX-380-027-C500		500 µg	290.00 USD
ALX-380-027-M001		1 mg	395.00 USD

Product Specification

FORMULA:	C₂₇H₂₁N₃O₅
MW:	467.5
CAS NUMBER:	97161-97-2
SOURCE/HOST:	Isolated from Nocardiopsis sp.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in DMSO, methanol or methylene chloride (5mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Alkaloid isolated from soil fungi. General, cell permeable protein kinase inhibitor. Potent inhibitor of Ca²⁺/calmodulin kinase II. Inhibits myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC), and cGMP-dependent protein kinase (PKG). Induces apoptosis.

Product Specific Literature References

K-252a, a potent inhibitor of protein kinase C from microbial origin: H. Kase, et al.; J. Antibiot. (Tokyo) 39, 1059 (1986) Abstract
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. (Tokyo) 39, 1072 (1986) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
K252a is a potent and selective inhibitor of phosphorylase kinase: L.H. Elliott, et al.; BBRC 171, 148 (1990) Abstract
Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926: Y. Hashimoto, et al.; BBRC 181, 423 (1991) Abstract
Differentiation of PC12 cells with K-ras: comparison with nerve growth factor: D.L. Simpson, et al.; J. Neurosci. Res. 28, 486 (1991) Abstract
K-252a inhibits nerve growth factor-induced trk proto-oncogene tyrosine phosphorylation and kinase activity: M.M. Berg, et al.; J. Biol. Chem. 267, 13 (1992) Abstract; Full Text
K-252 compounds: modulators of neurotrophin signal transduction: B. Knusel & F. Hefti; J. Neurochem. 59, 1987 (1992) Abstract
pp42/44MAP kinase is a component of the neurogenic pathway utilized by nerve growth factor in PC12 cells: E.D. Lloyd & M.W. Wooten; J. Neurochem. 59, 1099 (1992) Abstract
K-252a and staurosporine selectively block autophosphorylation of neurotrophin receptors and neurotrophin-mediated responses: S.H. Nye, et al.; Mol. Biol. Cell 3, 677 (1992) Abstract
K-252a and staurosporine promote choline acetyltransferase activity in rat spinal cord cultures: M.C. Glicksman, et al.; J. Neurochem. 61, 210 (1993) Abstract
Staurosporine-related compounds, K252a and UCN-01, inhibit both cPKC and nPKC: K. Mizuno, et al.; FEBS Lett. 330, 114 (1993) Abstract
Ecto-protein kinase and surface protein phosphorylation in PC12 cells: interactions with nerve growth factor: Z. Pawlowska, et al.; J. Neurochem. 60, 678 (1993) Abstract
Staurosporine, K-252a, and K-252b stabilize calcium homeostasis and promote survival of CNS neurons in the absence of glucose: B. Cheng, et al.; J. Neurochem. 62, 1319 (1994) Abstract
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review Abstract

Further Categories Containing This Product:

CAM Kinase Inhibitors • CDK & Cyclin Inhibitors • Myosin Light Chain Kinase Inhibitors • PKG Inhibitors • Alkaloids • Staurosporine / Related Products • PKA Inhibitors • Apoptosis Inducers & Inhibitors Other Products

ALX-380-029

Revised 20-Feb-08

K-252b
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

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