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Neurodegenerative Diseases
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ALX-430-156 Revised 21-Apr-08
6BIO
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SYNONYMS (2’Z,3’E)-6-Bromoindirubin-3’-oxime
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY GSK-3 Inhibitors
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ALX-430-156-M001   1 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C16H10BrN3O2
MW: 356.2
CAS NUMBER: 667463-62-9
PURITY: ≥98%
APPEARANCE: Dark red solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Inhibitor of phosphoinositide-dependent kinase 1 (PDK1). Potent, reversible and ATP-competitive inhibitor of glycogen synthase kinase-3α/β (GSK-3α/β).
Product Specific Literature References
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases: P. Polychronopoulos, et al.; J. Med. Chem. 47, 935 (2004) Abstract
7-Bromoindirubin-3’-oxime induces caspase-independent cell death: J. Ribas, et al.; Oncogene 25, 6304 (2006) Abstract
Inverse in silico screening for identification of kinase inhibitor targets: S. Zahler, et al.; Chem. Biol. 14, 1207 (2007) Abstract
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins: V. Myrianthopoulos, et al.; J. Med. Chem. 50, 4027 (2007) Abstract
Related Products
Further Categories Containing This Product:
PI(3)K-Akt-mTOR Pathway Other Products
 
 
ALX-151-026 Revised 20-Jun-08
N-Acetyl-Asp-Tyr(2-malonyl)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-026-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C39H57N7O14S
MW: 880.0
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Peptide is very unstable.
Product Description
Peptide containing a phosphotyrosyl mimetic. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides: B. Ye, et al.; J. Med. Chem. 38, 4270 (1995) Abstract
Further Categories Containing This Product:
Peptides • Phosphoinositide 3-kinase [PI(3)K] / Related Products
 
 
ALX-151-027 Revised 17-Jan-05
N-Acetyl-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-027-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C36H57N7O13SP
MW: 858.9
PURITY: ≥96%
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Phosphotyrosine containing peptide. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides: B. Ye, et al.; J. Med. Chem. 38, 4270 (1995) Abstract
Further Categories Containing This Product:
Peptides • Phosphoinositide 3-kinase [PI(3)K] / Related Products
 
 
ALX-201-006 Revised 04-Sep-08
N-Acetyl-eglin C (recombinant)
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PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-201-006-MC01   0.1 mg 95.00 USD Add To Cart
ALX-201-006-MC05   0.5 mg 380.00 USD Add To Cart
ALX-201-006-M001   1 mg 670.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Thr-Glu-Phe-Gly-Ser-Glu-Leu-Lys-Ser-Phe-Pro-Glu-Val-Val-Gly-Lys-Thr-Val-Asp-Gln-Ala-Arg-Glu-Tyr-Phe-Thr-Leu-His-Tyr-Pro-Gln-Tyr-Asn-Val-Tyr-Phe-Leu-Pro-Glu-Gly-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-Asp-Arg-Val-Arg-Val-Phe-Tyr-Asn-Pro-Gly-Thr-Asn-Val-Val-Asn-His-Val-Pro-His-Val-Gly-OH
FORMULA: C377H552N96O107
MW: 8141.1
CAS NUMBER: 96380-69-7
SOURCE/HOST: Produced in E. coli.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
Product Description
Eglin C was originally isolated from the leech Hirudo medicinalis [1]. Recombinant N-acetyl-eglin C is a 70 amino acid peptide with identical biological activity to native eglin C. An effective inhibitor of chymotrypsin and subtilisin as well as of leukocyte elastase and cathepsin G.
Product Specific Literature References
[1] Structure of the elastase-cathepsin G inhibitor of the leech Hirudo medicinalis: U. Seemüller, et al.; Hoppe-Seyler's Z. Physiol. Chem. 361, 1841 (1980) Abstract
[2] A large fragment approach to DNA synthesis: total synthesis of a gene for the protease inhibitor eglin c from the leech Hirudo medicinalis and its expression in E. coli: H. Rink, et al.; Nucl. Acids Res. 12, 6369 (1984) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link P01051: Eglin C (Hirudo medicinalis)
Further Categories Containing This Product:
Proteases Other Products • Recombinant Proteins / Fusion Proteins
 
 
ALX-270-484 Revised 07-Apr-08
AGK2
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SYNONYMS 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Sirtuins / Related Products
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ALX-270-484-M001   1 mg 40.00 USD Add To Cart
ALX-270-484-M005   5 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C23H13Cl2N3O2
MW: 434.3
CAS NUMBER: 304896-28-4
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Potent, selective and cell permeable inhibitor of sirtuin 2 (SIRT2) (IC50=3.5μM). Rescues α-synuclein-mediated toxicity. Modifies inclusion morphology in a cellular model of Parkinson’s disease. Protects against dopaminergic cell death. Leads to an increase in acetylated tubulin.
Product Specific Literature References
Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson’s disease: T.F. Outeiro, et al.; Science 317, 516 (2007) Abstract
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Further Categories Containing This Product:
Parkinson's Disease Other Products
 
 
ALX-270-386 Revised 24-Feb-05
Aloisine
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SYNONYMS RP106
7-n-Butyl-6-(4-methoxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-386-M001   1 mg 25.00 USD Add To Cart
Product Specification
FORMULA: C17H19N3O
MW: 281.4
PURITY: ≥95%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Potent, cell permeable, selective ATP-competitive inhibitor of CDK1/cyclin B (IC50=700nM), CDK5/p25 (IC50=1.5µM), and GSK-3 (IC50=920nM).
Product Specific Literature References
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects: Y. Mettey, et al.; J. Med. Chem. 46, 222 (2003) Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-385 Revised 17-Jul-07
Aloisine A
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SYNONYMS RP107
7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-385-M001   1 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C16H17N3O
MW: 267.3
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Cell permeable, potent, selective, reversible and ATP-competitive inhibitor of CDK1/cyclin B (IC50=150nM), CDK2/cyclin A (IC50=120nM), CDK2/cyclin E (IC50=400nM), CDK5/p25
(IC50=200nM), CDK5/p35 (IC50=160nM) and GSK-3α (IC50=500nM). Also inhibits GSK-3β (IC50=650nM) and c-Jun N-terminal kinase (JNK) (IC50~3-10µM). Poor inhibitor of CK1, CK2, CDK4/cyclin D1, MAPKK, PKA, PKG, PKCs and c-raf (IC50≥100µM). Blocks cell cycle in both G1 and G2 phase.
Product Specific Literature References
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects: Y. Mettey, et al.; J. Med. Chem. 46, 222 (2003) Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors • JNK [SAPK1] / Related Products • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-275 Revised 11-Sep-08
Alsterpaullone
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SYNONYMS 9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-275-M001   1 mg 60.00 USD Add To Cart
ALX-270-275-M005   5 mg 270.00 USD Add To Cart
Product Specification
FORMULA: C16H11N3O3
MW: 293.3
CAS NUMBER: 237430-03-4
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow to brown powder.
SOLUBILITY: Soluble in DMSO; insoluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Identity determined by IR, 1H-NMR and 13C-NMR.

Product Description
Potent inhibitor of CDK1/cyclin B (IC50=35nM). Potent and selective inhibitor of CDK2/cyclin A, CDK2/cyclin E (IC50=200nM), CDK5/p25 (IC50=40nM), CDK5/p35 (IC50=40nM) and GSK-3β . Induces apoptosis by activation of caspase-8 and caspase-9 followed by disruption of the mitochondrial potential.

Licensed from NCI.
Product Specific Literature References
ATP-site directed inhibitors of cyclin-dependent kinases: N. Gray, et al.; Curr. Med. Chem. 6, 859 (1999) Abstract
Fused azepinones with antitumor activity: C. Kunick; Curr. Pharm. Des. 5, 181 (1999), (Review) Abstract
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity: C. Schultz, et al.; J. Med. Chem. 42, 2909 (1999) Abstract
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases: D.W. Zaharevitz, et al.; Cancer Res. 59, 2566 (1999) Abstract
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity: C. Kunick, et al.; Bioorg. Med. Chem. Lett. 10, 567 (2000) Abstract
Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25: M. Leost, et al.; Eur. J. Biochem. 267, 5983 (2000) Abstract
Inhibition of CDKs as a therapeutic modality: E.A. Sausville, et al.; Ann. NY Acad. Sci. 910, 207 (2000) Abstract
A novel, extraneuronal role for cyclin-dependent protein kinase 5 (CDK5): modulation of cAMP-induced apoptosis in rat leukemia cells: T. Sandal, et al.; J. Biol. Chem. 277, 20783 (2002) Abstract; Full Text
Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor: M. Knockaert, et al.; J. Biol. Chem. 277, 25493 (2002) Abstract; Full Text
Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential: T. Lahusen, et al.; Mol Carcinog 36, 183 (2003) Abstract
The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products • GSK-3 Inhibitors
 
 
ALX-270-387 Revised 18-Jul-07
3-Amino-1H-pyrazolo[3,4-b]quinoxaline
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-387-M001   1 mg 40.00 USD Add To Cart
ALX-270-387-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C9H7N5
MW: 185.2
CAS NUMBER: 40254-90-8
PURITY: ≥98% (HPLC)
APPEARANCE: Red solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Selective inhibitor of CDK1/cyclin B (IC50=600nM), CDK5/p25 (IC50=400nM) and GSK-3β (IC50=1µM). Does not inhibit Cdc25 phosphatase activity (IC50>10µM).
Product Specific Literature References
Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-dependent kinases inhibitors: M.A. Ortega, et al.; Bioorg. Med. Chem. 10, 2177 (2002) Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors
 
 
ALX-350-106 Revised 29-Nov-07
Ampullosporin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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ALX-350-106-M001   1 mg 50.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Trp-Ala-Aib-Aib-Leu-Aib-Gln-Aib-Aib-Aib-Gln-Leu-Aib-Gln-Leucinol
FORMULA: C77H127N19O19
MW: 1623.0
SOURCE/HOST: Antibiotic isolated from Sepedonium ampullosporum.
PURITY: ≥98% (HPLC)
SOLUBILITY: Soluble in alcohols, chloroform or dichloromethane. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: TOXIC.
Product Description
Peptaibol-type polypeptide. Induces pigment formation by the fungus Phoma destructiva, causes hypothermia in mice, displays neuroleptic activity in rats and forms instable pores in artificial bilayer membranes.
Product Specific Literature References
Ampullosporin, a new peptaibol-type antibiotic from Sepedonium ampullosporum HKI-0053 with neuroleptic activity in mice: M. Ritzau, et al.; J. Antibiot. 50, 722 (1997) Abstract
Differences in ion permeability of an artificial bilayer membrane caused by ampullosporin and bergofungin, new 15-membered peptaibol-type antibiotics: P. Grigoriev, et al.; Bioelectrochemistry 44, 155 (1997)
Differences in ion-channel formation by ampullosporins B, C, D and semisynthetic desacetyltryptophanyl ampullosporin A: P. Grigoriev, et al.; Bioelectrochemistry 57, 119 (2002) Abstract
Synthesis and biological evaluation of analogues of the peptaibol ampullosporin A: H.H. Nguyen, et al.; J. Med. Chem. 45, 2781 (2002) Abstract
Crystal structure and conformational analysis of ampullosporin A: M. Kronen, et al.; J. Pept. Sci. 9, 729 (2003) Abstract
Membrane association and activity of 15/16-membered peptide antibiotics: zervamicin IIB, ampullosporin A and antiamoebin I: T.N. Kropacheva, et al.; Biochim. Biophys. Acta 1715, 6 (2005) Abstract
Transcriptional response to the neuroleptic-like compound Ampullosporin A in the rat ketamine model: H. Krugel, et al.; J. Neurochem. 97, Suppl. 1, 74 (2006) Abstract
Further Categories Containing This Product:
Peptides • Alzheimer Research Other Products • Ion Channels & Transporters Other Products