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Kinases in Cell Cycle Regulation
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ALX-153-012 Revised 04-Mar-05
Cyclin-dependent Kinase 2 Inhibitor
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SYNONYMS CDK2/Cyclin Inhibitor
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-153-012-M001   1 mg 120.00 USD Add To Cart
ALX-153-012-M005   5 mg 480.00 USD Add To Cart
Product Specification
SEQUENCE: H-Tyr-Ser-Phe-Val-His-His-Gly-Phe-Phe-Asn-Phe-Arg-Val-Ser-Trp-Arg-Glu-Met-Leu-Ala-OH
FORMULA: C121H164N32O27S
MW: 2530.9
PEPTIDE CONTENT: 75-95%
PURITY: ≥97%
APPEARANCE: White to off-white lyophilized solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.
Product Description
Inhibitor of cyclin-dependent kinase 2 (CDK2).
Product Specific Literature References
Genetic selection of peptide aptamers that recognize and inhibit cyclin- dependent kinase 2: P. Colas, et al.; Nature 380, 548 (1996) Abstract
Further Categories Containing This Product:
Peptides
 
 
ALX-153-041 Revised 04-Mar-05
Cyclin-dependent Kinase 2 Inhibitory Peptide I
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SYNONYMS CDK2/Cyclin Inhibitory Peptide I
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-153-041-C500   500 µg 145.00 USD Add To Cart
Product Specification
SEQUENCE: H-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Pro-Val-Lys-Arg-Arg-Leu-Phe-Gly-OH
FORMULA: C111H196N48O23
MW: 2571.1
PURITY: ≥98% (HPLC)
APPEARANCE: Solid.
FORMULATION: Lyophilized. Counter Ion: Trifluoroacetate salt.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Following reconstitution, aliquot and freeze (-20°C). Product is stable for 2 years as supplied. Stock solutions are stable for 3 months at -20°C.
HANDLING: Hygroscopic.
Product Description
Cell permeable inhibitor of CDK2/cyclin complexes. Blocks phosphorylation of substrates by CDK2/cyclin A and CDK/cyclin E complexes. Preferentially induces apoptosis only in transformed cells and not in non-transformed cells.

Chimeric peptide consisting of the N-terminal sequence of the HIV-TAT protein (directing uptake across the cell membrane) and the consensus sequence PVKRRLFG that serves as the docking site for CDK2/cyclin complexes.
Product Specific Literature References
Selective killing of transformed cells by cyclin/cyclin-dependent kinase 2 antagonists: Y.N. Chen, et al.; PNAS 96, 4325 (1999) Abstract; Full Text
Further Categories Containing This Product:
Peptides • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-153-042 Revised 04-Mar-05
Cyclin-dependent Kinase 2 Inhibitory Peptide II
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SYNONYMS CDK2/Cyclin Inhibitory Peptide II
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-153-042-C500   500 µg 145.00 USD Add To Cart
Product Specification
SEQUENCE: H-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Pro-Val-Lys-Arg-Arg-Leu-Asp-Leu-OH
FORMULA: C110H200N48O25
MW: 2595.1
PURITY: ≥98%
APPEARANCE: Lyophilized solid.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Very hygroscopic.
Product Description
Cell permeable inhibitor of CDK2/cyclin complexes. Blocks phosphorylation of substrates by CDK2/cyclin A and CDK/cyclin E complexes. Preferentially induces apoptosis only in transformed cells and not in non-transformed cells.
Product Specific Literature References
Selective killing of transformed cells by cyclin/cyclin-dependent kinase 2 antagonists: Y.N. Chen, et al.; PNAS 96, 4325 (1999) Abstract; Full Text
Further Categories Containing This Product:
Peptides • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-350-290 Revised 19-Oct-07
Debromohymenialdisine
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SYNONYMS DBH
4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-290-C100   100 µg 90.00 USD Add To Cart
Product Specification
FORMULA: C11H11N5O2
MW: 245.2
CAS NUMBER: 125118-55-0
SOURCE/HOST: Isolated from sponge Stylotella aurantium.
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Inhibitor of G2 DNA damage checkpoint (IC50=8µM) and check point kinases 1 (Chk1) (IC50=3µM) and 2 (Chk2) (IC50=3.5µM) [1,3]. Unlike other checkpoint inhibitors DBH does not inhibit ataxia-telangiectasia mutated (ATM) or ATM-Rad3-related protein. Also inhibits MAP kinase kinase 1 (MEK-1) (IC50=881nM) but is not as potent as 10Z-hymenialdisine (Prod. No. ALX-350-289) (IC50=6nM) [2].
Product Specific Literature References
[1] Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001) Abstract; Full Text
[2] Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002) Abstract
[3] G2 checkpoint abrogators as anticancer drugs: T. Kawabe; Mol. Cancer Ther. 3, 513 (2004) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Chk1 & Chk2 / Related Products • Natural Products for Cell Cycle Research • Alkaloids
 
 
ALX-480-050 Revised 17-Jul-07
6-Dimethylaminopurine
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SYNONYMS N6,N6-Dimethyladenine
6-DMAP
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-480-050-M100   100 mg 15.00 USD Add To Cart
Product Specification
FORMULA: C7H9N5
MW: 163.2
CAS NUMBER: 938-55-6
PURITY: ≥97%
APPEARANCE: Crystalline.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Non-selective inhibitor of cdc2 and other kinases.
Product Specific Literature References
Inhibition of cyclin-dependent kinases by purine analogues: J. Vesley, et al.; Eur. J. Biochem. 224, 771 (1994)
 
 
ALX-270-389 Revised 17-Jul-07
Elbfluorene
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SYNONYMS 3-Acetyl-6-hydroxy-4-phenylbenzo[4,5]furo[2,3-b]pyridine
1-Aza-9-oxafluorene 5b
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY DNA Repair Other Products
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ALX-270-389-M001   1 mg 75.00 USD Add To Cart
ALX-270-389-M005   5 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C19H13NO3
MW: 303.3
PURITY: ≥95% (HPLC)
APPEARANCE: Off-white to brownish powder.
SOLUBILITY: Soluble in DMSO. Insoluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Selective inhibitor of CDK1/cyclin B (IC50=4.2µM) with some P-glycoprotein-modulating properties (inhibitory activity ratio 1.26 at 7µM). Weakly inhibits CDK5/p25 (6% inhibition at 10µM) with no effect on CDK2/cyclin E and CDK4/cyclin D1 (IC50>100µM).
Product Specific Literature References
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties: K. Brachwitz, et al.; J. Med. Chem. 46, 876 (2003) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors
 
 
ALX-270-300 Revised 05-Apr-08
Fascaplysin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-270-300-M001   1 mg 60.00 USD Add To Cart
ALX-270-300-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C18H11N2OCl
MW: 306.8
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Brown powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.
HAZARD: TOXIC.

Product Description
Originally isolated from a marine sponge. Selective CDK4/cyclin D1 (IC50=350nM) inhibitor (in an ATP competitive manner).
Product Specific Literature References
Fascaplysin, an unusual antimicrobial pigment from the marine sponge Fascaplysinopsis sponge: D.M. Roll, et al.; J. Org. Chem. 53, 3276 (1988)
A new bioactive sesterterpene and antiplasmodial alkaloids from the marine sponge hyrtios cf. erecta: G. Kirsch, et al.; J. Nat. Prod. 63, 825 (2000) Abstract
Inhibition of cyclin-dependent kinase 4 (Cdk4) by fascaplysin, a marine natural product: R. Soni, et al.; BBRC 275, 877 (2000) Abstract
DNA binding properties of the marine sponge pigment fascaplysin: A. Hormann, et al.; Bioorg. Med. Chem. 9, 917 (2001) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • Alkaloids
 
 
ALX-430-161 Revised 21-Jul-08 New product
Flavopiridol
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SYNONYMS Alvocidib
(-)-2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(3R,4S)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1-benzopyran-4-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-430-161-M005   5 mg 60.00 USD Add To Cart
ALX-430-161-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C21H20ClNO5
MW: 401.8
CAS NUMBER: 146426-40-6
MERCK INDEX: 14: 4094
SOURCE/HOST: Synthetic.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in chloroform; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: HARMFUL.
IDENTITY: Identity determined by 1H-NMR.

Product Description

Potent inhibitor of cyclin-dependent kinases  (CDKs). Induces apoptosis in certain tumor cells. Interacts with multidrug resistance protein 1 (MRP1).
Product Specific Literature References
Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase: W.F. Jr. De Azevedo, et al.; PNAS 93, 2735 (1996) Abstract; Full Text
Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (CDK) 2 and CDK4 in human breast carcinoma cells: B.A. Carlson, et al.; Cancer Res. 56, 2973 (1996) Abstract; Full Text
Flavopiridol: a cytotoxic flavone that induces cell death in noncycling A549 human lung carcinoma cells: K.C. Bible & S.H. Kaufmann; Cancer Res. 56, 4856 (1996) Abstract; Full Text
Flavopiridol (L86-8275): selective antitumor activity in vitro and activity in vivo for prostate carcinoma cells: M. Drees, et al.; Clin. Cancer Res. 3, 273 (1997) Abstract; Full Text
The novel cyclin-dependent kinase inhibitor flavopiridol downregulates Bcl-2 and induces growth arrest and apoptosis in chronic B-cell leukemia lines: A. König, et al.; Blood 90, 4307 (1997) Abstract; Full Text
Flavopiridol induces apoptosis of normal lymphoid cells, causes immunosuppression, and has potent antitumor activity In vivo against human leukemia and lymphoma xenografts: F. Arguello, et al.; Blood 91, 2482 (1998) Abstract; Full Text
Cell cycle-independent induction of apoptosis by the anti-tumor drug Flavopiridol in endothelial cells: S. Brüsselbach, et al.; Int. J. Cancer 77, 146 (1998) Abstract
Flavopiridol induces apoptosis in chronic lymphocytic leukemia cells via activation of caspase-3 without evidence of bcl-2 modulation or dependence on functional p53: J.C. Byrd, et al.; Blood 92, 3804 (1998) Abstract; Full Text
Identification of cytosolic aldehyde dehydrogenase 1 from non-small cell lung carcinomas as a flavopiridol-binding protein: J.B. Schnier, et al.; FEBS Lett. 454, 100 (1999) Abstract
Potent interaction of flavopiridol with MRP1: J.H. Hooijberg, et al.; Br. J. Cancer 81, 269 (1999) Abstract
Flavopiridol: the first cyclin-dependent kinase inhibitor in human clinical trials: A.M. Senderowicz; Invest. New Drugs 17, 313 (1999), (Review) Abstract
Protein kinase inhibitors flavopiridol and 7-hydroxy-staurosporine down-regulate antiapoptosis proteins in B-cell chronic lymphocytic leukemia: S. Kitada, et al.; Blood 96, 393 (2000) Abstract; Full Text
Flavopiridol, a cyclin-dependent kinase inhibitor, enhances radiosensitivity of ovarian carcinoma cells: U. Raju, et al.; Cancer Res. 63, 3263 (2003) Abstract; Full Text
Potential use of pharmacological cyclin-dependent kinase inhibitors as anti-HIV therapeutics: A. Pumrery, et al.; Curr. Pharm. Des. 12, 1949 (2006) Abstract
Flavopiridol synergizes TRAIL cytotoxicity by downregulation of FLIPL: T.E. Fandy, et al.; Cancer Chemother. Pharmacol. 60, 313 (2007) Abstract
Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors: C. Sekine, et al.; J. Immunol. 180, 1954 (2008) Abstract
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • MDR Other Products
 
 
ALX-270-395 Revised 08-Dec-04
2-Hydroxybohemine
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SYNONYMS 6-(2-Hydroxybenzylamino)-2-(3-hydroxypropylamino)-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-395-M001   1 mg 60.00 USD Add To Cart
ALX-270-395-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C18H24N6O2
MW: 356.4
PURITY: ≥95%
FORMULATION: Off-white solid.
SOLUBILITY: 100µM soluble in DMSO, dimethyl formamide or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of CDK1 (IC50=100nM) and CDK2 (IC50=80nM).
Product Specific Literature References
Antiproliferative effect of plant cytokinin analogues with an inhibitory activity on cyclin-dependent kinases: K. Vermeulen, et al.; Leukemia 16, 299 (2002) Abstract
 
 
ALX-350-289 Revised 05-Apr-08
10Z-Hymenialdisine
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SYNONYMS 4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-289-C500   500 µg 190.00 USD Add To Cart
Product Specification
FORMULA: C11H10BrN5O2
MW: 324.1
CAS NUMBER: 82005-12-7
SOURCE/HOST: Isolated from sponge Axinella damicornis (Stylissa damicornis).
PURITY: ≥97%
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Originally isolated from the sponges Axinella verrucosa and Acantella aurantiaca. Potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-β (GSK-3β) and CDK5/p35 in Alzheimer’s disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6µM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nM), CDK2/cyclin A (IC50=70nM), CDK2/cyclin E (IC50=40nM), CDK4/cyclin D1 (IC50=600nM), CDK5/p25 (IC50=28nM), GSK-3β (IC50=10nM), and casein kinase 1 (CK1) (IC50=35nM). Inhibitor of NF-κB activation and of various pro-inflammatory cytokines such as IL-1, IL-2 (IC50=2.4µM), IL-6, IL-8, TNF-α (IC50=1.4µM) and nitric oxide (NO) (IC50=0.8µM) in a variety of cell lines.
Product Specific Literature References
Isolation and x-ray crystal structure of a novel bromo-compound from two marine sponges: G. Cimino, et al.; Tetrahedron Lett. 23, 767 (1982)
Bioactive alkaloids from the tropical marine sponge Axinella carteri: A. Supriyono, et al.; Z. Naturforsch. [C] 50, 669 (1995) Abstract
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kappaB: J.J. Breton & M.C. Chabot-Fletche