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GSK-3 Inhibitors
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ALX-270-271 Revised 17-Jul-07
Indirubin-3'-monoxime
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-271-M001   1 mg 50.00 USD Add To Cart
ALX-270-271-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C16H11N3O2
MW: 277.3
PURITY: ≥98% (1H-NMR)
APPEARANCE: Dark red powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Selective and strong inhibitor of cyclin-dependent kinases (CDKs). Inhibits CDK1/cyclin B (IC50=180nM), CDK2/cyclin A (IC50~500nM), CDK2/cyclin E (IC50=250nM), CDK4/cyclin D1 (IC50=3.3µM) and CDK5/p35 (IC50=100nM).  Inhibits the proliferation of a large range of cells, mainly through arresting the cells in the G2/M phase of the cell cycle. Powerful inhibitor of GSK-3β (IC50~100nM) and tau phosphorylation in vitro and in vivo at Alzheimer’s disease-specific sites.
Product Specific Literature References
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nature Cell Biol. 1, 60 (1999) Abstract; Full Text
Anti-mitotic properties of indirubin-3'-monoxime, a CDK/GSK-3 inhibitor: induction of endoreplication following prophase arrest: E. Damiens, et al.; Oncogene 20, 3786 (2001) Abstract; Full Text
Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?: S. Leclerc, et al.; J. Biol. Chem. 276, 251 (2001) Abstract; Full Text
Inhibition of cyclin-dependent kinase 1 (CDK1) by indirubin derivatives in human tumour cells: D. Marko, et al.; Br. J. Cancer 84, 283 (2001) Abstract; Full Text
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Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products • GSK-3 Inhibitors • Tau / Related Products
 
 
ALX-270-275 Revised 07-Dec-07
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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:
GSK-3 Inhibitors • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-270-296 Revised 15-Aug-08
Indirubin-5-sulfonic acid . sodium salt
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SYNONYMS E226
Indirubin-5-sulphonate . Na
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-296-M001   1 mg 75.00 USD Add To Cart
ALX-270-296-M005   5 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C16H9N2O5S . Na
MW: 341.3 . 23.0
PURITY: ≥95% (1H-NMR)
APPEARANCE: Black powder.
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of cyclin-dependent kinases (CDKs), with selectivity for CDK1/cyclin B (IC50=55nM), CDK2/cyclin A (IC50=35nM), CDK2/cyclin E (IC50=150nM), CDK4/cyclin D1 (IC50=300nM), CDK5/p35 (IC50=65nM) and GSK-3β (IC50=280nM).
Product Specific Literature References
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nat. Cell. Biol. 1, 60 (1999)
Inhibitor binding to active and inactive cdk2. the crystal structure of cdk2-cyclin a/indirubin-5-sulphonate: T.G. Davies, et al.; Structure (Camb) 9, 389 (2001) Abstract
Inhibition of cyclin-dependent kinase 1 (CDK1) by indirubin derivatives in human tumour cells: D. Marko, et al.; Br. J. Cancer 84, 283 (2001) Abstract
Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?: S. Leclerc, et al.; J. Biol. Chem. 276, 251 (2001) Abstract; Full Text
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Further Categories Containing This Product:
GSK-3 Inhibitors
 
 
ALX-270-354 Revised 03-Jul-08
TDZD-8
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SYNONYMS 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY GSK-3 Inhibitors
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ALX-270-354-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C10H10N2SO2
MW: 222.3
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Highly selective, non-ATP competitive inhibitor of GSK-3β (IC50=2µM). Binds to the active site of GSK-3β. Does not significantly affect the activities of Cdk-1/cyclin B, CK-II, PKA, and PKC (IC50>100µM).
Product Specific Literature References
First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease: A. Martinez, et al.; J. Med. Chem. 45, 1292 (2002) Abstract; Full Text
 
 
ALX-270-358 Revised 21-Sep-04
2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole
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SYNONYMS TIBPO
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY GSK-3 Inhibitors
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ALX-270-358-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C14H10IN3OS
MW: 395.2
PURITY: ≥95%
FORMULATION: Lyophilized.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light and moisture.

Product Description
Potent inhibitor of glycogen synthase kinase-3β (GSK-3β) (IC50=390nM).
Product Specific Literature References
Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors: L. Naerum, et al.; Bioorg. Med. Chem. Lett. 12, 1525 (2002) Abstract
 
 
ALX-270-361 Revised 28-Sep-07
Indirubin
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-361-M001   1 mg 50.00 USD Add To Cart
ALX-270-361-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C16H10N2O2
MW: 262.3
CAS NUMBER: 479-41-4
SOURCE/HOST: Synthetic.
PURITY: ≥98% (1H-NMR, HPLC)
APPEARANCE: Purple powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (0.3mg/ml). Sparingly soluble in aqueous buffers (12.5µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years when stored at +4°C in the dark. Stock solutions should be stored in the dark and used within 1 month.
HANDLING: Keep cool and dry. Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR, IR, ESI-MS and UV.

Product Description
Inhibitor of cyclin-dependent kinases (CDK1/cyclin B (IC50=10µM), CDK2/cyclin A (IC50=2.2µM), CDK2/cyclin E (IC50=7.5µM), CDK4/cyclin D1 (IC50=12µM), CDK5/p35 (IC50=5.5µM)) [1] and of GSK-3β (IC50=600nM) [2]. Inhibits inflammatory reaction in delayed-type hypersensitivity in mice [3]. Ligand of human aryl hydrocarbon receptor [4]. Exhibits anti-cancer activity [5] [6].
Product Specific Literature References
[1] Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nature Cell Biol. 1, 60 (1999) Abstract
[2] Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors?: S. Leclerc, et al.; J. Biol. Chem. 276, 251 (2001) Abstract; Full Text
[3] Indirubin inhibits inflammatory reactions in delayed-type hypersensitivity: T. Kunikata, et al.; Eur. J. Pharmacol. 410, 93 (2000) Abstract
[4] Indirubin and indigo are potent aryl hydrocarbon receptor ligands present in human urine: J. Adachi, et al.; J. Biol. Chem. 276, 31475 (2001) Abstract; Full Text
[5] Molecular mechanisms of indirubin and its derivatives: novel anticancer molecules with their origin in traditional Chinese phytomedicine: G. Eisenbrand, et al.; J. Cancer Res. Clin. Oncol. 130, 627 (2004) Abstract
[6] Indirubin enhances tumor necrosis factor-induced apoptosis through modulation of nuclear factor-kappa B signaling pathway: G. Sethi, et al.; J. Biol. Chem. 281, 23425 (2006) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Indirubin is derived from various natural sources, such as Indigofera indica, Isatis tinctoria and I. indigotica by fermentation, oxidation and the presence of light as a by product of indigo formation. Indirubin is also present in human urine and fetal bovine serum [4]. Preclinical studies of indirubin its confirmed anti-tumor activity. Efficacy against chronic myelocytic leukemia was demonstrated in clinical trials in China [2].
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Further Categories Containing This Product:
GSK-3 Inhibitors • Antitumor Reagents Other Products • Anti-inflammatory Agents Other 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:
Cell Cycle Blockers & Inhibitors / Related Products • GSK-3 Inhibitors • JNK [SAPK1] / Related 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:
Cell Cycle Blockers & Inhibitors / Related 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-270-424 Revised 13-Feb-07
5-Iodo-indirubin-3'-monoxime
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-424-M001   1 mg 90.00 USD Add To Cart
Product Specification