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Signal Transduction Enzymes / Related Products
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ALX-158-001 Revised 28-Feb-06
Histone H1-7 Substrate
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-158-001-M001   1 mg 70.00 USD Add To Cart
ALX-158-001-M005   5 mg 280.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Arg-Lys-Ala-Ser-Gly-Pro-OH
FORMULA: C31H58N14O9
MW: 770.9
PURITY: ≥98%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cAMP-dependent protein kinase (PKA). The peptide is derived from the phosphorylation site (Ser38) in calf thymus histone H1.
Product Specific Literature References
Studies on the mechanism of phosphorylation of synthetic polypeptides by a calf thymus cyclic AMP-dependent protein kinase: A.H. Pomerantz, et al.; PNAS 74, 4261 (1977) Abstract
Further Categories Containing This Product:
Peptides • PKA Substrates
 
 
ALX-158-003 Revised 04-Jul-03
Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-158-003-M001   1 mg 50.00 USD Add To Cart
ALX-158-003-M005   5 mg 200.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ser-Arg-Lys-Glu-OH
FORMULA: C38H74N18O11
MW: 959.1
PURITY: ≥97%
APPEARANCE: White powder.
FORMULATION: Lyophilized.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cGMP-dependent protein kinase corresponding to residues 29-35 of histone H2B. For the corresponding alanine-for-serine substituted peptides see Prod. No. ALX-158-002 and Prod. No. ALX-158-004.
Product Specific Literature References
Comparison of the substrate specificity of adenosine 3':5'- monophosphate- and guanosine 3':5'-monophosphate-dependent protein kinases. Kinetic studies using synthetic peptides corresponding to phosphorylation sites in histone H2B: D.B. Glass & E.G. Krebs; J. Biol. Chem. 254, 9728 (1979) Abstract; Full Text
Further Categories Containing This Product:
PKG Substrates • Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products • Peptides
 
 
ALX-158-002 Revised 28-Feb-06
[Ala32]-Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-158-002-M001   1 mg 75.00 USD Add To Cart
ALX-158-002-M005   5 mg 300.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ala-Arg-Lys-Glu-OH
FORMULA: C38H74N18O10
MW: 943.1
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Inhibitor of cGMP-dependent protein kinase, derived by a serine-to-alanine substitution at position 32 of histone H2B (29-35). For the corresponding unsubstituted histone fragment see Prod. No. ALX-158-003.
Product Specific Literature References
D.B. Glass & M.D. Miller; Fed. Proc. 39, 867 (1980)
Differential responses of cyclic GMP-dependent and cyclic AMP-dependent protein kinases to synthetic peptide inhibitors: D.B. Glass; Biochem. J. 213, 159 (1983) Abstract
Further Categories Containing This Product:
Peptides • PKG Inhibitors
 
 
ALX-158-004 Revised 13-Jan-05
[Ala34]-Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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ALX-158-004-M001   1 mg 60.00 USD Add To Cart
ALX-158-004-M005   5 mg 240.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ser-Arg-Ala-Glu-OH
FORMULA: C35H67N17O11
MW: 902.0
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cGMP-dependent protein kinase. For the corresponding unsubstituted histone fragment see Prod. No. ALX-158-003.
Product Specific Literature References
Phosphorylation by guanosine 3':5'-monophosphate-dependent protein kinase of synthetic peptide analogs of a site phosphorylated in histone H2B: D.B. Glass & E.G. Krebs; J. Biol. Chem. 257, 1196 (1982) Abstract; Full Text
Further Categories Containing This Product:
PKG Substrates • Peptides
 
 
ALX-260-164 Revised 24-Sep-07
H-LVK-CHO
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SYNONYMS H-Leu-Val-Lys-CHO
Cathepsin B Inhibitor (Aldehyde)
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-164-M001   1 mg 70.00 USD Add To Cart
ALX-260-164-M005   5 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C19H36N4O4
MW: 384.5
PURITY: ≥95%
APPEARANCE: White to beige solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: May form cyclic isomers.
Product Description
Inhibitor of cathepsin B (IC50=4nM). More potent than to leupeptin (IC50=310nM) (Prod. No. ALX-260-009).
Product Specific Literature References
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues: R.M. McConnell, et al.; J. Med. Chem. 36, 1084 (1993) Abstract
 
 
ALX-430-035 Revised 05-Feb-08
HNMPA-(AM)3
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SYNONYMS Hydroxy-2-naphthalenylmethylphosphonic acid tris acetoxymethyl ester
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-430-035-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C20H23O10P
MW: 454.4
PURITY: ≥98%
APPEARANCE: Colorless oil.
SOLUBILITY: >20mg/ml soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions are stable for up to 3 months when stored at -20 °C. Avoid alkaline medium, pH>8.0.

Product Description
Cell permeable inhibitor of insulin receptor tyrosine kinase activity and insulin-stimulated rat adipocyte glucose oxidation. Inhibits both serine and tyrosine autophosphorylation by the human insulin receptor. Does not affect protein kinase C (PKC) or cAMP-dependent protein kinase (PKA).
Product Specific Literature References
Design of a selective insulin receptor tyrosine kinase inhibitor and its effect on glucose uptake and metabolism in intact cells: R. Saperstein, et al.; Biochemistry 28, 5694 (1989) Abstract
Catalysis of serine and tyrosine autophosphorylation by the human insulin receptor: K. Baltensperger, et al.; PNAS 89, 7885 (1992) Abstract
 
 
ALX-270-363 Revised 04-Mar-05
3-(4-Hydroxybenzylidenyl)indolin-2-one
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-270-363-M001   1 mg 50.00 USD Add To Cart
ALX-270-363-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C15H11NO2
MW: 237.3
CAS NUMBER: 293302-14-4
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Yellow crystals.
SOLUBILITY: Soluble in DMSO (> 50 mg/ml) or methanol (0.5mg/ml). Sparingly soluble in aqueous buffers (5µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable as a powder for at least 2 years when stored at +4°C in the dark. Stock solutions made in DMSO should be stored in the dark and used within one month.
HANDLING: Keep cool and dry. Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR, IR, ESI-MS and UV.

Product Description
Selective receptor tyrosine kinase (RTK) inhibitor. Inhibits FLK-1 RTK (IC50 ~3µM) [1]. Consists predominantly of the E-isomer, contains ~10% of the Z-isomer [1].
Product Specific Literature References
[1] Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases: L. Sun, et al.; J. Med. Chem. 41, 2588 (1998) Abstract
 
 
ALX-270-395 Revised 08-Dec-04
2-Hydroxybohemine
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SYNONYMS 6-(2-Hydroxybenzylamino)-2-(3-hydroxypropylamino)-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-395-M001   1 mg 60.00 USD Add To Cart
ALX-270-395-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C18H24N6O2
MW: 356.4
PURITY: ≥95%
FORMULATION: Off-white solid.
SOLUBILITY: 100µM soluble in DMSO, dimethyl formamide or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of CDK1 (IC50=100nM) and CDK2 (IC50=80nM).
Product Specific Literature References
Antiproliferative effect of plant cytokinin analogues with an inhibitory activity on cyclin-dependent kinases: K. Vermeulen, et al.; Leukemia 16, 299 (2002) Abstract
 
 
ALX-270-292 Revised 09-Feb-05
1L-6-Hydroxymethyl-chiro-inositol-2-[(R)-2-O-methyl-3-O-octadecylcarbonate]
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-292-M001   1 mg 85.00 USD Add To Cart
ALX-270-292-M005   5 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C30H58O10
MW: 578.8
PURITY: >98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.

Product Description
Potent inhibitor of Akt (PKB) (IC50=2.0µM). Weak inhibitor of PI(3)K (phosphoinositide 3-kinase) (IC50=83µM). Has been shown to inhibit the growth of the following cancer cell lines: HeLa (IC50=2.5µM), HT-29 (IC50=10µM), MCF-7 (IC50=1.2µM) and PC-3 (IC50=2.0µM).
Product Specific Literature References
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth: Y. Hu, et al.; J. Med. Chem. 43, 3045 (2000) Abstract
Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products • Akt [PKB] / Related Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-350-289 Revised 18-Nov-08
10Z-Hymenialdisine
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SYNONYMS 4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-289-C500   500 µg 190.00 USD Add To Cart
ALX-350-289-M001   1 mg 340.00 USD Add To Cart
Product Specification
FORMULA: C11H10BrN5O2
MW: 324.1
CAS NUMBER: 82005-12-7
SOURCE/HOST: Isolated from sponge Axinella damicornis (Stylissa damicornis).
PURITY: ≥97%
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.
IDENTITY: Identity determined by 1H- NMR, 13C-NMR and MS.

Product Description
Originally isolated from the sponges Axinella verrucosa and Acantella aurantiaca. Potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-β (GSK-3β) and CDK5/p35 in Alzheimer’s disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6µM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nM), CDK2/cyclin A (IC50=70nM), CDK2/cyclin E (IC50=40nM), CDK4/cyclin D1 (IC50=600nM), CDK5/p25 (IC50=28nM), GSK-3β (IC50=10nM), and casein kinase 1 (CK1) (IC50=35nM). Inhibitor of NF-κB activation and of various pro-inflammatory cytokines such as IL-1, IL-2 (IC50=2.4µM), IL-6, IL-8, TNF-α (IC50=1.4µM) and nitric oxide (NO) (IC50=0.8µM) in a variety of cell lines.
Product Specific Literature References
Isolation and x-ray crystal structure of a novel bromo-compound from two marine sponges: G. Cimino, et al.; Tetrahedron Lett. 23, 767 (1982)
Bioactive alkaloids from the tropical marine sponge Axinella carteri: A. Supriyono, et al.; Z. Naturforsch. [C] 50, 669 (1995) Abstract
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kappaB: J.J. Breton & M.C. Chabot-Fletcher; J. Pharmacol. Exp. Ther. 282, 459 (1997) Abstract; Full Text
Inhibition of NFkappaB-mediated interleukin-1beta-stimulated prostaglandin E2 formation by the marine natural product hymenialdisine: A. Roshak, et al.; J. Pharmacol. Exp. Ther. 283, 955 (1997) Abstract; Full Text
Inhibition of interleukin-1-induced proteoglycan degradation and nitric oxide production in bovine articular cartilage/chondrocyte cultures by the natural product, hymenialdisine: A.M. Badger, et al.; J. Pharmacol. Exp. Ther. 290, 587 (1999) Abstract; Full Text
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000) Abstract
Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001) Abstract; Full Text
An investigation of cell proliferation and soluble mediators induced by interleukin 1beta in human synovial fibroblasts: comparative response in osteoarthritis and rheumatoid arthritis: H. Inoue, et al.; Inflamm. Res. 50, 65 (2001) Abstract
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002) Abstract
Inhibition of cytokine production by hymenialdisine derivatives: V. Sharma, et al.; J. Med. Chem. 47, 3700 (2004) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • MAPK Pathway Inhibitors • Natural Products - NF-kB Pathway Inhibitors • NF-kB Pathway Inhibitors • Natural Products for Cell Cycle Research • Natural Products - Nitric Oxide Pathway Modulators • DNA Damage Checkpoint Other Products • GSK-3 Inhibitors • Alkaloids • Marine Natural Products
 
 
ALX-350-291 Revised 19-Oct-07
Hymenidin
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SYNONYMS 2-Debromooroidin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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