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Circadian Clock / Related Products
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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
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Further Categories Containing This Product:
PI(3)K-Akt-mTOR Pathway Other Products
 
 
ALX-270-039 Revised 15-Nov-06
A-3 . hydrochloride
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SYNONYMS N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-039-M010   10 mg 65.00 USD Add To Cart
ALX-270-039-M050   50 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C12H13ClN2O2S . HCl
MW: 284.8 . 36.5
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of cAMP- and cGMP-dependent protein kinase (PKA and PKG), protein kinase C (PKC), casein kinase I and II, and myosin light chain kinase.
Product Specific Literature References
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Casein Kinase Inhibitors
 
 
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-270-468 Revised 02-Oct-07
AR-A014418
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SYNONYMS N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY GSK-3 Inhibitors
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ALX-270-468-M001   1 mg 55.00 USD Add To Cart
Product Specification
FORMULA: C12H12N4O4S
MW: 308.3
CAS NUMBER: 487021-52-3
SOURCE/HOST: Synthetic.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, methanol, 100% ethanol or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL. MAY BE CARCINOGENIC.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Cell permeable, specific and potent inhibitor of glycogen synthase kinase-3 (GSK-3) (IC50=104nM). Inhibition is competitive with respect to ATP (Ki=38nM).
Product Specific Literature References
Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418: R. Bhat, et al.; J. Biol. Chem. 278, 45937 (2003) Abstract; Full Text
AR-A014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test: T.D. Gould, et al.; Int. J. Neuropsychopharmacol. 7, 387 (2004) Abstract
Inhibition of glycogen synthase kinase-3 by lithium correlates with reduced tauopathy and degeneration in vivo: W. Noble, et al.; PNAS 102, 6990 (2005) Abstract; Full Text
 
 
ALX-270-430 Revised 23-Mar-06
1-Azakenpaullone
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SYNONYMS 9-Bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY GSK-3 Inhibitors
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ALX-270-430-M001   1 mg 95.00 USD Add To Cart
ALX-270-430-M005   5 mg 380.00 USD Add To Cart
Product Specification
FORMULA: C15H10BrN3O
MW: 328.2
PURITY: ≥95% (HPLC)
APPEARANCE: Off-white to tan powder.
SOLUBILITY: Soluble in DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING: Protect from light.

Product Description
Analog of kenpaullone (Prod. No. ALX-270-274) acting as a potent and ATP-competitive inhibitor of GSK-3β (IC50=18nM). Displays ~100-200 fold greater selectivity on
GSK-3β than over CDK1/cyclin B and CDK5/p25 (IC50=2.0µM and 4.2µM, respectively).
Product Specific Literature References
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta: C. Kunick, et al.; Bioorg. Med. Chem. Lett. 14, 413 (2004) Abstract
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes: B. Voigt, et al.; Bioorg. Med. Chem. Lett. 15, 823 (2005) Abstract
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ALX-350-014 Revised 03-Apr-08
Calyculin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-014-C010   10 µg 65.00 USD Add To Cart
ALX-350-014-C025   25 µg 110.00 USD Add To Cart
ALX-350-014-C050   50 µg 190.00 USD Add To Cart
ALX-350-014-C100   100 µg 320.00 USD Add To Cart
Product Specification
FORMULA: C50H81N4O15P
MW: 1009.2
CAS NUMBER: 101932-71-2
SOURCE/HOST: Isolated from Discodermia calyx.
PURITY: ≥95%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetonitrile, chloroform, methylene chloride or benzene. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: May by subject to isomerization when in solution. Biological activity is not affected by isomerization.
HANDLING: Protect from light and moisture.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Potent cell permeable inhibitor with high specificity for protein phosphatase 1 (PP1) and 2A (PP2A). Inhibits p130cas tyrosine phosphorylation. Enhances the phosphorylation level of NF-κB. Affects intracellular signalling processes that require 14-3-3. Potent non-phorbol type tumor promoter. Prevents γ-radiation induced apoptosis.
Product Specific Literature References
Okadaic acid: an additional non-phorbol-12-tetradecanoate-13-acetate- type tumor promoter: M. Suganuma, et al.; PNAS 85, 1768 (1988) Abstract
Protein phosphatases come of age: P.Cohen & P.T. Cohen; J. Biol. Chem. 264, 21435 (1989) Abstract; Full Text
Calyculin A and okadaic acid: inhibitors of protein phosphatase activity: H. Ishihara, et al.; BBRC 159, 871 (1989) Abstract
The structure and regulation of protein phosphatases: P. Cohen; Ann. Rev. Biochem. 58, 453 (1989) Abstract
Calyculin A, an inhibitor of protein phosphatases, a potent tumor promoter on CD-1 mouse skin: M. Suganuma, et al.; Cancer Res. 50, 3521 (1990) Abstract
Nonphorbol tumor promoters okadaic acid and calyculin-A induce membrane translocation of protein kinase C: R. Gopalakrishna; BBRC 189, 950 (1992) Abstract
Comparative effects of protein phosphatase inhibitors (okadaic acid and calyculin A) on human leukemia HL60, HL60/ADR and K562 cells: K. Sakurada, et al.; BBRC 187, 488 (1992) Abstract
Calyculin A, a potent inhibitor of phosphatases-1 and -2A, prevents apoptosis: Q. Song & M.F. Lavin; BBRC 190, 47 (1993) Abstract
Enhancement of AMPA-mediated synaptic transmission by the protein phosphatase inhibitor calyculin A in rat hippocampal slices: A. Figurov, et al.; Eur. J. Neurosci. 5, 1035 (1993) Abstract
Calyculin A, a non-phorbol ester type tumor promotor, induced oxidative DNA damage in stimulated human neutrophil-like cells: T. Takeuchi, et al.; BBRC 205, 1803 (1994) Abstract
Potassium and calcium channel involvement in induction of long-lasting synaptic enhancement by calyculin A, a protein phosphatase inhibitor, in rat hippocampal CA1 region: N. Murakami, et al.; Neurosci. Lett. 176, 181 (1994) Abstract
Differential toxicity of the protein phosphatase inhibitors microcystin and calyculin A: M.T. Runnegar, et al.; J. Pharmacol. Exp. Ther. 273, 545 (1995) Abstract
Inhibition of p130cas tyrosine phosphorylation by calyculin A: W. Qiu, et al.; J. Leukoc. Biol. 63, 631 (1998) Abstract
Unique features of the okadaic acid activity class of tumor promoters: H. Fujiki & M. Suganuma; J. Cancer Res. Clin. Oncol. 125, 150 (1999), Review Abstract
Calyculin A-induced vimentin phosphorylation sequesters 14-3-3 and displaces other 14-3-3 partners in vivo: G. Tzivion, et al.; J. Biol. Chem. 275, 29772 (2000) Abstract
Calyculin A induces apoptosis and stimulates phosphorylation of p65NF-kappaB in human osteoblastic osteosarcoma MG63 cells: H. Tanaka, et al.; Int. J. Oncol. 31, 389 (2007) Abstract
Further Categories Containing This Product:
PP2A / Related Products • PP1 / Related Products • Natural Products - Other Tumor Promoters • 14-3-3 Proteins / Related Products • Carcinogens & Tumor Promoters Other Products • NF-kB Pathway Modulators • Natural Products - Apoptosis Inducers & Inhibitors • Marine Natural Products
 
 
ALX-270-062 Revised 03-Feb-05
Cantharidic acid . disodium salt
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PP2A / Related Products
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ALX-270-062-M010   10 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C10H12O5 . 2Na
MW: 212.2 . 46.0
CAS NUMBER: 28874-45-5
PURITY: ≥95%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water; slightly soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent protein phosphatase 2A inhibitor.
Product Specific Literature References
M. Matsuzawa, et al.; J. Agric. Food Chem. 35, 823 (1987)
Partial characterization of specific cantharidin binding sites in mouse tissues: M.J. Graziano, et al.; Mol. Pharmacol. 33, 706 (1989) Abstract
Cantharidin-binding protein: identification as protein phosphatase 2A: Y.-M. Li & J.E. Casida; PNAS 89, 11867 (1992) Abstract
 
 
ALX-270-063 Revised 03-Apr-08
Cantharidin
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SYNONYMS Hexahydro-3a,7a-dimethyl-4,7-epoxyisobenzo-furan-1,3-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-270-063-M025   25 mg 50.00 USD Add To Cart
ALX-270-063-M100   100 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C10H12O4
MW: 196.2
CAS NUMBER: 56-25-7
MERCK INDEX: 14: 1752
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetone, DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Protect from light.
HAZARD: TOXIC.