• Home
  • Sitemap
  • Help
  • Technical Support
  • Contact
Cyclin-dependent Kinases [CDKs] & Cyclins / Related Products
You are here: Product Lines > Cell Cycle > Cyclin-dependent Kinases [CDKs] & Cyclins / Related Products
Toolbar - View Selection
 
Items 68 of 68
ALX-270-143 Revised 20-Feb-08
Tyrphostin AG 494
Add to Clipboard
SYNONYMS Tyrphostin B48
N-Phenyl-3,4-dihydroxybenzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-N-phenylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-143-M005   5 mg 25.00 USD Add To Cart
ALX-270-143-M025   25 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C16H12N2O3
MW: 280.3
CAS NUMBER: 133550-35-3
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Blocks CDK2 activation and causes cells to arrest at late G1 and during S phase.
Product Specific Literature References
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases: A. Gazit, et al.; J. Med. Chem. 34, 1896 (1991) Abstract
Tyrphostin AG 494 blocks Cdk2 activation: N. Osherov & A. Levitzki; FEBS Lett. 410, 187 (1997) Abstract
Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase: N. Kleinberger-Doron, et al.; Exp. Cell Res. 241, 340 (1998) Abstract
 
 
ALX-270-168 Revised 18-May-06
Tyrphostin AG 490
Add to Clipboard
SYNONYMS Tyrphostin B42
N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-]N-benzylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-168-M005   5 mg 45.00 USD Add To Cart
ALX-270-168-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C17H14N2O3
MW: 294.3
CAS NUMBER: 133550-30-8
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO and acetone; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selectively inhibits CDK2 activation leading to a potent cell cycle arrest at late G1 and S phase. Cell permeable inhibitor of JAK-2 tyrosine kinase. Does not significantly inhibit other kinases, such as Lck, Lyn, Btk, Syk or Src. Blocks IL-7 induced JAK kinase activity in T cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. Valuable tool for studying the cellular role of JAK kinases in signal transduction.
Product Specific Literature References
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors: A. Gazit, et al.; J. Med. Chem. 32, 2344 (1989) Abstract
Tyrosine phosphorylation is an obligatory event in IL-2 secretion [published erratum appears in J Immunol 1991 May 1;146(9):3260]: A. Levitzki; Biochem. Pharmacol. 40, 913 (1990) Abstract
Activation of phosphatidylinositol-3 kinase by ligation of the interleukin-7 receptor is dependent on protein tyrosine kinase activity: H. Dadi, et al.; Blood 84, 1579 (1994) Abstract; Full Text
JAK3 protein tyrosine kinase mediates interleukin-7-induced activation of phosphatidylinositol-3’ kinase: N. Sharfe, et al.; Blood 86, 2077 (1995) Abstract; Full Text
Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor: N. Meydan, et al.; Nature 379, 645 (1996) Abstract
Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells: R.A. Kirken, et al.; J. Leukoc. Biol. 65, 891 (1999) Abstract
JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response: L.H. Wang, et al.; J. Immunol. 162, 3897 (1999) Abstract
JAK2 tyrosine kinase inhibitor tyrphostin AG490 downregulates the mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) pathways and induces apoptosis in myeloma cells: J. De Vos, et al.; Br. J. Haematol. 109, 823 (2000) Abstract
 
 
ALX-270-246 Revised 28-Sep-07
Purvalanol A
Add to Clipboard
SYNONYMS 6-[(3-Chloro)anilino]-2(1R)-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-246-M001   1 mg 55.00 USD Add To Cart
ALX-270-246-M005   5 mg 220.00 USD Add To Cart
Product Specification
FORMULA: C19H25N6OCl
MW: 388.9
PURITY: ≥99%
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: Soluble in DMSO, methanol or dichloromethane.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry. Keep under inert gas.

Product Description
Inhibitor of human CDK1 (IC50=4nM), CDK2/cyclin A (IC50=70nM), Cdc2/cyclin B, CDK2/cyclin E (IC50=35nM), CDK4/cyclin D1 (IC50=850nM) as well as CDK5/p35 (IC50=75nM). More membrane permeable than purvalanol B.
Product Specific Literature References
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors: N.S. Gray, et al.; Science 281, 533 (1998) Abstract
Up-regulation of cdc2 protein during paclitaxel-induced apoptosis: P. Chadebech, et al.; Int. J. Cancer 87, 779 (2000) Abstract
Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004) Abstract
 
 
ALX-270-248 Revised 17-Jul-07
Compound 52
Add to Clipboard
SYNONYMS 2-(2-Hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-248-M001   1 mg 55.00 USD Add To Cart
Product Specification
FORMULA: C16H19ClN6O
MW: 346.8
PURITY: ≥99%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent, cell permeable and selective inhibitor of CDK1 (IC50=340nM) the cell cycle-regulating kinase Cdc28p (IC50=7µM) and the related Pho85p kinase (IC50=2µM).
Product Specific Literature References
Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors: N.S. Gray, et al.; Science 281, 533 (1998) Abstract
 
 
ALX-270-249 Revised 11-Sep-08
Aminopurvalanol A
Add to Clipboard
SYNONYMS (2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-
9H-purin-2-yl)amino)-3-methyl-1-butanol
NG-97
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-249-M001   1 mg 45.00 USD Add To Cart
ALX-270-249-M005   5 mg 135.00 USD Add To Cart
Product Specification
FORMULA: C19H26N7OCl
MW: 403.9
CAS NUMBER: 220792-57-4
PURITY: ≥97% (1H-NMR)
APPEARANCE: White to brownish solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Packaged under inert gas. Protect from light.
HAZARD: IRRITANT.

Product Description
Cell permeable, reversible and competitive inhibitor of CDK1/cyclin B (IC50=33nM), CDK2/cyclin A (IC50=33nM), CDK2/cyclin E (IC50=28nM) and CDK5/p35 (IC50=20nM).
Product Specific Literature References
Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors: Y.T. Chang, et al.; Chem. Biol. 6, 361 (1999) Abstract
A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts: G.R. Rosania, et al.; PNAS 96, 4797 (1999) Abstract; Full Text
M-phase regulation of the recruitment of mRNAs onto polysomes using the CDK1/cyclin B inhibitor aminopurvalanol: M. Le Breton, et al.; BBRC 306, 880 (2003) Abstract
 
 
ALX-270-271 Revised 17-Jul-07
Indirubin-3'-monoxime
Add to Clipboard
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
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
 
 
ALX-270-274 Revised 13-Sep-07
Kenpaullone
Add to Clipboard
SYNONYMS 9-Bromo-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-274-M001   1 mg 60.00 USD Add To Cart
ALX-270-274-M005   5 mg 270.00 USD Add To Cart
Product Specification
FORMULA: C16H11BrN2O
MW: 327.2
CAS NUMBER: 142273-20-9
PURITY: ≥95%
APPEARANCE: Brown powder.
SOLUBILITY: Soluble in DMSO; insoluble in water or ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent inhibitor of CDK1/cyclin B (IC50=400nM). Also inhibits CDK2/cyclin A (IC50=680nM) , CDK5 (IC50=850nM) and with much less effect other kinases.
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
Structure-based design modifications of the paullone molecular scaffold for cyclin-dependent kinase inhibition: R. Gussio; Anticancer Drug Des. 15, 53 (2000) 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
 
 
ALX-270-275 Revised 11-Sep-08
Alsterpaullone
Add to Clipboard
SYNONYMS 9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
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:
Apoptosis Inducers & Inhibitors Other ProductsGSK-3 Inhibitors
 
 
ALX-270-282 Revised 18-Jul-07
9-Cyanopaullone
Add to Clipboard
SYNONYMS 9-Cyano-7,12-dihydroindolo-[3,2-d][1]benzazepin-6[5H]-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-282-M001   1 mg 70.00 USD Add To Cart
ALX-270-282-M005   5 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C17H11N3O
MW: 273.3
PURITY: ≥95%
SOLUBILITY: Soluble in DMSO; insoluble in water or ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Very potent inhibitor of CDK1/cyclin B (IC50=25nM). Also inhibits CDK5/p25 (IC50=44nM ) and GSK-3β (IC50=10nM).
 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) 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, 2609 (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
Structure-based design modifications of the paullone molecular scaffold for cyclin-dependent kinase inhibition: R. Gussio, et al.; Anticancer Drug Des. 15, 53 (2000) 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
 
 
ALX-270-296 Revised 15-Aug-08
Indirubin-5-sulfonic acid . sodium salt
Add to Clipboard
SYNONYMS E226
Indirubin-5-sulphonate . Na
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: