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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 • Casein Kinase Inhibitors • PKG 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:
Cell Cycle Blockers & Inhibitors/Related Products • GSK-3 Inhibitors
 
 
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-270-275 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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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-270-387 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
Related Products
 
 
ALX-153-003 Revised 03-Feb-05
Casein Kinase II Substrate
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Casein Kinase Substrates
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ALX-153-003-M001   1 mg 70.00 USD Add To Cart
ALX-153-003-M005   5 mg 280.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Arg-Arg-Glu-Glu-Glu-Thr-Glu-Glu-Glu-OH
FORMULA: C52H87N19O24
MW: 1362.4
PURITY: ≥96%
APPEARANCE: White lyophilized powder.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Specific substrate for casein kinase II, derived from the kinase II phosphorylation site found in casein. Is not being phosphorylated by casein kinase I, cAMP-dependent protein kinase, protein kinase G, myosin light chain kinase, phosphorylase kinase and EGF receptor kinase.
Product Specific Literature References
A synthetic peptide substrate specific for casein kinase II: E.A. Kuenzel & E.D. Krebs; PNAS 82, 737 (1985) Abstract
Further Categories Containing This Product:
Peptides
 
 
ALX-270-442 Revised 12-Jun-08
CDK1/2 Inhibitor III
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SYNONYMS 5-Amino-3-((4-(aminosulfonyl)phenyl)amino)-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-442-M001   1 mg 118.00 USD Add To Cart
Product Specification
FORMULA: C15H13F2N7O2S2
MW: 425.4
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
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.
HAZARD: HARMFUL.
IDENTITY: Identity determined by NMR.

Product Description
Cell permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC50=20nM, 35nM and 92nM in HCT-116, HeLa, and A375 cells). Acts as a highly potent, ATP-competitive inhibitor of CDK1/cyclin B and CDK2/cyclin A (IC50=600pM and 500pM) with selectivity over VEGF-R2 and GSK-3β (IC50=32nM and 140nM).
Product Specific Literature References
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities: R. Lin, et al.; J. Med. Chem. 48, 4208 (2005) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Antitumor Agents (Anti-proliferative) • VEGFs & VEGF-Rs Other Products • GSK-3 Inhibitors
 
 
ALX-270-095 Revised 07-May-08
5,6-Dichloro-1-β-D-ribofuranosyl benzimidazole
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SYNONYMS DRB
5,6-Dichlorobenzimidazole riboside
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Adenosine Derivatives Other Products
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ALX-270-095-M005   5 mg 20.00 USD Add To Cart
ALX-270-095-M025   25 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C12H12Cl2N2O4
MW: 319.1
CAS NUMBER: 53-85-0
RTECS: DD7310000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO (100mM) or dimethyl formamide (100mM).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions should be stored in the refrigerator and should be lyophilized and frozen for longer storage periods.
IDENTITY: Identity determined by 1H-NMR, MS and UV.

Product Description
Selective casein kinase II inhibitor. Inhibitor of RNA synthesis in eukaryotic cells.
Product Specific Literature References
Halobenzimidazole ribosides and RNA synthesis of cells and viruses: I. Tamm & P. Sehgal; Adv. Virus Res. 22, 187 (1978) Abstract
Mechanism of action of 5,6-dichloro-1-beta-D- ribofuranosylbenzimidazole. II. A resistant human cell mutant with an altered transcriptional machinery: B. Mittleman, et al.; J. Mol. Biol. 165, 461 (1983) Abstract
Mechanism of action of DRB. III. Effect on specific in vitro initiation of transcription: R. Zandomeni, et al.; J. Mol. Biol. 167, 561 (1983) Abstract
Casein kinase type II is involved in the inhibition by 5,6-dichloro-1- beta-D-ribofuranosylbenzimidazole of specific RNA polymerase II transcription: R. Zandomeni, et al.; J. Biol. Chem. 261, 3414 (1986) Abstract; Full Text
Inhibition of germinal vesicle breakdown in bovine oocytes by 5,6- dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB): C.E. Farin & L. Yang; Mol. Reprod. Dev. 37, 284 (1994) Abstract
Further Categories Containing This Product:
Casein Kinase Inhibitors
 
 
ALX-270-017 Revised 27-Apr-06