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Cell Cycle
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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:
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:
GSK-3 Inhibitors • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-270-249 Revised 11-Sep-08
Aminopurvalanol A
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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
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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-270-387 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-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:
Natural Products - Other Tumor Promoters • Cell Cycle Blockers & Inhibitors / Related Products • Carcinogens & Tumor Promoters Other Products • Natural Products - DNA Replication Inhibitors • 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 • Natural Products for Cell Cycle Research • Natural Products - Other Anti-infective Agents • Parasitic Diseases Other Products • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-350-375 Revised 22-Jul-08 New product
Arcyriaflavin A
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-375-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H11N3O2
MW: 325.3
CAS NUMBER: 118458-54-1
SOURCE/HOST: Synthetic. Originally isolated from the marine ascidian Eudistoma sp.
PURITY: ≥95% (HPLC)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in DMSO (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light. Packaged under inert gas.

Product Description
Potent inhibitor of CDK4 / cyclin D1 (IC50 = 59nM). Inhibits human cytomegalovirus (HCMV) replication in cell culture (IC50 = 200nM).
Product Specific Literature References
Staurosporine aglycone (K252-c) and arcyriaflavin A from the marine ascidian, Eudistoma sp: P.A. Horton, et al.; Experientia 50, 843 (1994) Abstract
Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication: M.J. Slater, et al.; Bioorg. Med. Chem. 7, 1067 (1999) Abstract
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors: C. Sanchez-Martinez, et al.; Bioorg. Med. Chem. Lett. 13, 3835 (2003) Abstract
Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors: G. Zhu, et al.; Bioorg. Med. Chem. Lett. 13, 1231 (2003) Abstract
Two indolocarbazole alkaloids with apoptosis activity from a marine-derived actinomycete Z(2)039-2: R. Liu, et al.; Arch. Pharm. Res. 30, 270 (2007) Abstract
Further Categories Containing This Product:
Natural Products for Cell Cycle Research • Antiviral Agents Other Products
 
 
ALX-350-273 Revised 03-Apr-08
3-ATA
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SYNONYMS 3-Amino-9-thio(10H)-acridone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-273-M001   1 mg 60.00 USD Add To Cart
ALX-350-273-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C13H10N2S
MW: 226.3
CAS NUMBER: 12982-10-85
PURITY: ≥95%
APPEARANCE: White solid powder.
SOLUBILITY: Soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Specific CDK4 inhibitor (IC50=3.1µM) inducing growth inhibition of p16-altered tumors.
Product Specific Literature References
The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4: A. Kubo, et al.; Clin. Cancer Res. 5, 4279 (1999) Abstract
3-Amino thioacridone, a selective cyclin-dependent kinase 4 inhibitor, attenuates kainic acid-induced apoptosis in neurons: E. Verdaguer, et al.; Neuroscience 120, 599 (2003) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors
 
 
ALX-385-022 Revised 07-Oct-08
Baicalein
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SYNONYMS 5,6,7-Trihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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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 - Protein Kinase Inhibitors • Tyrosine Kinase Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products for Angiogenesis Research • Lipoxygenases / Related Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antioxidants • Natural Products - Antiviral / anti-HIV Agents • Cell Cycle Blockers & Inhibitors / Related Products • Natural Products for Cell Cycle Research
 
 
ALX-270-388 Revised 18-Jul-07
Benfluorene