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Cell Cycle Blockers & Inhibitors/Related Products
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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-350-016 Revised 31-Jul-08
(+)-Aphidicolin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-016-M001   1 mg 65.00 USD Add To Cart
ALX-350-016-M005   5 mg 260.00 USD Add To Cart
ALX-350-016-M025   25 mg 890.00 USD Add To Cart
Product Specification
FORMULA: C20H34O4
MW: 338.5
CAS NUMBER: 38966-21-1
MERCK INDEX: 14: 727
RTECS: PB9185000
SOURCE/HOST: Isolated from Nigrospora oryzae.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (50mg/ml), methanol (10mg/ml) or 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Reversible inhibitor of eukaryotic nuclear DNA replication. Useful for cell synchronization. Blocks the cell cycle at early S phase. Prolongs the half life of DNA methyltransferase. Specific inhibitor of DNA polymerase α and δ in eukaryotic cells and in some viruses of animal origin. Acts synergistically with vincristine and doxorubicin. Apoptosis inhibitor/inducer.
Product Specific Literature References
X-Ray crystallographic determination of the structure of the antibiotic aphidicolin: a tetracyclic diterpenoid containing a new ring system: K.M. Brundret, et al.; J. C. S. Chem. Commun. 1027 (1972)
The production of aphidicolin by Nigrospora sphaerica: A.N. Starratt and S.R Loschiavo; Can. J. Microbiol. 20, 416 (1974)
Aphidicolin prevents mitotic cell division by interfering with the activity of DNA polymerase-alpha: S. Ikegami, et al.; Nature 275, 458 (1978) Abstract
Inhibition by aphidicolin of cell cycle progression and DNA replication in sea urchin embryos: S. Ikegami, et al.; J. Cell. Physiol. 100, 439 (1979) Abstract
New views of the biochemistry of eucaryotic DNA replication revealed by aphidicolin, an unusual inhibitor of DNA polymerase alpha: J.A. Huberman; Cell 23, 647 (1981) Abstract
Aphidicolin: a specific inhibitor of nuclear DNA replication in eukaryotes: S. Spadari, et al.; TIBS 7, 29 (1982)
Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in human myeloid leukemia cell lines: K. Kuwakado, et al.; Biochem. Pharmacol. 46, 1909 (1993) Abstract
Life, death and genomic change in perturbed cell cycles: R.T. Schimke, et al.; Philos. Trans. R. Soc. London B Biol. Sci. 345, 311 (1994) Abstract
Dissociation of nuclear and cytoplasmic cell cycle progression by drugs employed in cell synchronization: L. Urbani, et al.; Exp. Cell. Res. 219, 159 (1995) Abstract
Drug-induced apoptosis is not necessarily dependent on macromolecular synthesis or proliferation in the p53-negative human prostate cancer cell line PC-3: M.M. Borner, et al.; Cancer Res. 55, 2122 (1995) Abstract
TrkA neurogenic receptor regulates differentiation of neuroblastoma cells: W. Poluha, et al.; Oncogene 10, 185 (1995) Abstract
Coordinate regulation of G- and C strand length during new telomere synthesis: X. Fan and C.M. Price; Mol. Biol. Cell 8, 2145 (1997) Abstract; Full Text
Effect of aphidicolin on DNA methyltransferase in the nucleus: I. Suetake, et al.; Cell Struct. Funct. 23, 137 (1998) Abstract
Cytotoxicity of aphidicolin and its derivatives against neuroblastoma cells in vitro: synergism with doxorubicin and vincristine: M. Michaelis, et al.; Anticancer Drugs 11, 479 (2000) Abstract
Aphidicolin and bleomycin induced chromosome damage as biomarker of mutagen sensitivity: a twin study: B. Tedeschi, et al.; Mutat. Res. 546, 55 (2004) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products • Natural Products - Other Tumor Promoters • DNA Replication Inhibitors • Carcinogens & Tumor Promoters Other Products • Natural Products - DNA Replication Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-350-095 Revised 03-Apr-08
Apicidin
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SYNONYMS cyclo-L-(2-Amino-8-oxodecanoyl)-L-(N-methoxy-tryptophan)-L-isoleucyl-D-pipecolinyl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation/Transcription
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ALX-350-095-M001   1 mg 50.00 USD Add To Cart
ALX-350-095-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C34H49N5O6
MW: 623.8
CAS NUMBER: 183506-66-3
SOURCE/HOST: Isolated from Fusarium sp.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC.

Product Description
Potent inhibitor of histone deacetylase (HDAC). Inhibits proliferation. Induces cell cycle arrest. Stimulates apoptosis of cancer cells. Antiprotozoal.
Product Specific Literature References
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase: S.J. Darkin-Rattray, et al.; PNAS 93, 13143 (1996) Abstract
Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin: J.W. Han, et al.; Cancer Res. 60, 6068 (2000) Abstract
Transcriptional activation of p21(WAF1/CIP1) by apicidin, a novel histone deacetylase inhibitor: J.S. Kim, et al.; BBRC 281, 866 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 107 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 113 (2001) Abstract
Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities: S.B. Singh, et al.; J. Org. Chem. 67, 815 (2002) Abstract
Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells: J. Hong, et al.; Cancer Lett. 189, 197 (2003) Abstract
Activation of NF-kappaB by HDAC inhibitor apicidin through Sp1-dependent de novo protein synthesis: its implication for resistance to apoptosis: Y.K. Kim, et al.; Cell Death Differ. 13, 2033 (2006) Abstract
Apicidin, a novel histone deacetylase inhibitor, has profound anti-growth activity in human endometrial and ovarian cancer cells: T. Ueda, et al.; Int. J. Mol. Med. 19, 301 (2007) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products • HDAC Inhibitors • Parasitic Diseases Other Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Other Anti-infective Agents • Natural Products for Cell Cycle Research
 
 
ALX-385-022 Revised 19-Nov-07
Baicalein
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SYNONYMS 5,6,7-Trihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonoids/Related Products
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ALX-385-022-M005   5 mg 25.00 USD Add To Cart
ALX-385-022-M025   25 mg 100.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 491-67-8
MERCK INDEX: 14: 942
PURITY: ≥97%
APPEARANCE: Yellow to yellow-green crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Inhibitor of 12-lipoxygenase, leukotriene biosynthesis and the release of lysosomal enzymes. Inhibits cellular Ca2+ uptake and calcium mobilization. Inhibitor of protein tyrosine kinase in leukemia (CEM) cells. Induces cell cycle arrest and apoptosis. Anti-inflammatory compound. Has anti-thrombotic, anti-proliferative and anti-mitogenic effects.
Product Specific Literature References
Specific action of the lipoxygenase pathway in mediating angiotensin II- induced aldosterone synthesis in isolated adrenal glomerulosa cells: J.L. Nadler, et al.; J. Clin. Invest. 80, 1763 (1987) Abstract
Inhibition of reverse transcriptase activity by a flavonoid compound, 5,6,7-trihydroxyflavone: K. Ono, et al.; BBRC 160, 982 (1989) Abstract
Biliary excretion of metabolites of baicalin and baicalein in rats: K. Abe, et al.; Chem. Pharm. Bull. 38, 209 (1990) Abstract
Effects of baicalein and esculetin on transduction signals and growth factors expression in T-lymphoid leukemia cells: H.C. Huang, et al.; Eur. J. Pharmacol. 268, 73 (1994) Abstract
Protective effects of baicalein against cell damage by reactive oxygen species: D. Gao, et al.; Chem. Pharm. Bull. (Tokyo) 46, 1383 (1998) Abstract
Baicalein induces a dual growth arrest by modulating multiple cell cycle regulatory molecules
: S.L. Hsu, et al.; Eur. J. Pharmacol. 425, 165 (2001) Abstract
Mechanisms in mediating the anti-inflammatory effects of baicalin and baicalein in human leukocytes: Y.C. Shen, et al.; Eur. J. Pharmacol. 465, 171 (2003) Abstract
Baicalein induced cell cycle arrest and apoptosis in human lung squamous carcinoma CH27 cells: H.Z. Lee, et al.; Anticancer Res. 25, 959 (2005) Abstract
Biological properties of baicalein in cardiovascular system: Y. Huang, et al.; Curr. Drug Targets Cardiovasc. Haematol. Disord. 5, 177 (2005), (Review) Abstract
Baicalein inhibition of hydrogen peroxide-induced apoptosis via ROS-dependent heme oxygenase 1 gene expression: H.Y. Lin, et al.; Biochim. Biophys. Acta 1773, 1073 (2007) Abstract
Further Categories Containing This Product:
Leukotrienes Other Products • Natural Products for Angiogenesis Research • Tyrosine Kinase Inhibitors • Natural Products - Protein Kinase Inhibitors • Natural Products - Antiviral/anti-HIV Agents • Lipoxygenases/Related Products • Cell Cycle Blockers & Inhibitors/Related Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products for Cell Cycle Research • Natural Products - Antioxidants
 
 
ALX-270-390 Revised 09-Jan-08
Bohemine
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SYNONYMS 6-Benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-390-M001   1 mg 40.00 USD Add To Cart
ALX-270-390-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C18H24N6O
MW: 340.4
CAS NUMBER: 189232-42-6
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from moisture.

Product Description
Cell permeable inhibitor of CDK1 (IC50=1.1µM) and CD2 (IC50=600nM). Arrests cell cycle in the G1/S boundary and activates mature bovine oocytes.
Product Specific Literature References
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds: L. Havlicek, et al.; J. Med. Chem. 40, 408 (1997) Abstract
Treatment of Vicia faba root tip cells with specific inhibitors to cyclin-dependent kinases leads to abnormal spindle formation: P. Binarova, et al.; Plant J. 16, 697 (1998) Abstract
Activation of bovine oocytes by specific inhibition of cyclin-dependent kinases: R. Alberio, et al.; Mol. Reprod. Dev. 55, 422 (2000) Abstract
Proteomics approach in classifying the biochemical basis of the anticancer activity of the new olomoucine-derived synthetic cyclin-dependent kinase inhibitor, bohemine: H. Kovarova, et al.; Electrophoresis 21, 3757 (2000) Abstract
In vivo metabolism of 2,6,9-trisubstituted purine-derived cyclin-dependent kinase inhibitor bohemine in mice: glucosidation as the principal metabolic route: Z. Chmela, et al.; Drug. Metab. Dispos. 29, 326 (2001) Abstract; Full Text
Antiproliferative effect of plant cytokinin analogues with an inhibitory activity on cyclin-dependent kinases: K. Vermeulen, et al.; Leukemia 16, 299 (2002)
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products
 
 
ALX-105-011 Revised 18-Sep-06
S-Trityl-L-cysteine
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SYNONYMS NSC 83265
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors/Related Products
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ALX-105-011-M100   100 mg 20.00 USD Add To Cart
ALX-105-011-M500   500 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C22H21NO2S
MW: 363.5
CAS NUMBER: 2799-07-7
RTECS: AY7710000
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or acetic acid
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Potent, cell permeable cysteine thioether displaying anti-mitotic and anti-tumor properties. Inhibits mitosis by blocking basal and microtubule-activated ATPase activities of the mitotic kinesin Eg5 (IC50=1µM and 140nm). Induces mitotic arrest in HeLa cells (IC50=700nM) and inhibits the growth of NCI tumor cell line panel (GI50=1.31µM).
Product Specific Literature References
In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities: S. DeBonis, et al.; Mol. Cancer Ther. 3, 1079 (2004) Abstract; Full Text
S-trityl-l-cysteine is a reversible, tight-binding inhibitor of the human kinesin eg5 that specifically blocks mitotic progression: D.A. Skoufias, et al.; J. Biol. Chem. 281, 17559 (2006) Abstract; Full Text
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins/Related Products • Antitumor Agents (Anti-proliferative)
 
 
ALX-270-438 Revised 06-Dec-06
Dimethylenastron
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SYNONYMS 7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors/Related Products
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ALX-270-438-M001   1 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C16H18N2O2S
MW: 302.4
CAS NUMBER: 863774-58-7
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 6 months when stored at -20°C in the dark.
HANDLING: Protect from light.
HAZARD: HARMFUL.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Potent, cell permeable non-tubulin-interacting mitosis inhibitor. Blocks mitosis (IC50=200nM) by binding to the mitotic kinesin Eg5.
Product Specific Literature References
Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5: M. Gartner, et al.; ChemBioChem. 6, 1173 (2005) Abstract
Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5: N. Sunder-Plassmann, et al.; Bioorg. Med. Chem. 13, 6094 (2005) Abstract
Inhibitors of kinesin Eg5: antiproliferative activity of monastrol analogues against human glioblastoma cells: C. Muller, et al.; Cancer Chemother. Pharmacol. 59, 157 (2007) Abstract
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins/Related Products
 
 
ALX-350-006 Revised 05-Apr-08
Genistein (synthetic)
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SYNONYMS 4',5,7-Trihydroxyisoflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-006-M010   10 mg 25.00 USD Add To Cart
ALX-350-006-M025   25 mg 50.00 USD Add To Cart
ALX-350-006-M050   50 mg 90.00 USD Add To Cart
ALX-350-006-M100   100 mg 150.00 USD Add To Cart
ALX-350-006-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 446-72-0
MERCK INDEX: 14: 4391
RTECS: NR2392000
SOURCE/HOST: Synthetic.