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ALX-385-016 Revised 02-Jun-08
Morin
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SYNONYMS 2’,3,4’,5,7-Pentahydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonols
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-385-016-G001   1 g 16.00 USD Add To Cart
Product Specification
FORMULA: C15H10O7
MW: 302.2
CAS NUMBER: 480-16-0
MERCK INDEX: 14: 6269
RTECS: LK8749000
PURITY: ≥85%
APPEARANCE: White to brown powder.
SOLUBILITY: Soluble in methanol or 100% ethanol; slightly soluble in ether or acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: IRRITANT.

Product Description
Antioxidant flavonoid. Shows anti-proliferative and antitumor properties. Induces apoptosis. Induces cell cycle arrest at the G2/M phase. Anti-inflammatory compound. Suppresses NF-κB activation. Induces lipid peroxidation and DNA strand breaks.
Product Specific Literature References
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Lipid peroxidation and DNA damage induced by morin and naringenin in isolated rat liver nuclei: S. C. Sahu & G. C. Gray; Food Chem. Toxicol. 35, 443 (1997) Abstract
Morin inhibits the growth of human leukemia HL-60 cells via cell cycle arrest and induction of apoptosis through mitochondria dependent pathway: H.M. Kuo, et al.; Anticancer Res. 27, 395 (2007) Abstract
Morin (3,5,7,2’,4’-Pentahydroxyflavone) abolishes nuclear factor-kappaB activation induced by various carcinogens and inflammatory stimuli, leading to suppression of nuclear factor-kappaB-regulated gene expression and up-regulation of apoptosi: S.K. Manna, et al.; Clin. Cancer Res. 13, 2290 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative) • NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Antitumor Reagents • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antioxidants • Cell Cycle Blockers & Inhibitors / Related Products • Natural Products for Cell Cycle Research • Lipid Peroxidation
 
 
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
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-385-027 Revised 08-Feb-08
Tangeretin
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SYNONYMS 2-(4-Methoxyphenyl)-5,6,7,8-tetramethoxy-4H-1-benz-1-benzopyran-4-one
4’,5,6,7,8-Pentamethoxyflavone
Ponkanetin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-385-027-M010   10 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C20H20O7
MW: 372.4
CAS NUMBER: 481-53-8
RTECS: DJ3102725
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol or ethyl acetate; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Flavonoid found in the peel of citrus fruits where it provides natural resistance to fungi. Induces G1 cell cycle arrest in cancer cells. Counteracts tumor promoter-induced inhibition of intercellular communication and inhibits cell proliferation in several cancer lines. Reduces elevation of blood pressure and plasma glucose levels.
Product Specific Literature References
Nobiletin Is Main Fungistat in Tangerines Resistant to Mal Secco: A. Ben-Aziz; Science 155, 1026 (1967) Abstract
Flavonoids (apigenin, tangeretin) counteract tumor promoter-induced inhibition of intercellular communication of rat liver epithelial cells: C. Chaumontet, et al.; Cancer Lett. 114, 207 (1997) Abstract
Antiproliferative activity of flavonoids on several cancer cell lines: S. Kawaii; Biosci. Biotechnol. Biochem. 63, 896 (1999) Abstract
Tangeretin inhibits extracellular-signal-regulated kinase (ERK) phosphorylation: S. Van Slambrouck, et al.; FEBS Lett. 579, 1665 (2005) Abstract
Tangeretin and nobiletin induce G1 cell cycle arrest but not apoptosis in human breast and colon cancer cells: K.L. Morley, et al.; Cancer Lett. 251, 168 (2007) Abstract
Tangeretin suppresses IL-1beta-induced cyclooxygenase (COX)-2 expression through inhibition of p38 MAPK, JNK, and AKT activation in human lung carcinoma cells: K.H. Chen, et al.; Biochem. Pharmacol. 73, 215 (2007) Abstract
Further Categories Containing This Product:
Active Substances from Fruit and Vegetables • Natural Products - Antitumor Reagents • Cell Cycle Blockers & Inhibitors / Related Products • Natural Products for Cell Cycle Research • Natural Products - Antifungal Agents
 
 
ALX-430-094 Revised 04-Jul-07
Monastrol
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SYNONYMS 4-(3-Hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydro-4H-pyrimidin-5-carboxylic acid ethyl ester
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-094-M001   1 mg 60.00 USD Add To Cart
ALX-430-094-M005   5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C14H16N2O3S
MW: 292.4
CAS NUMBER: 329689-23-8
PURITY: ≥95%
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cell permeable non-tubulin-interacting mitosis inhibitor. Blocks mitosis (IC50=14µM) by binding to the mitotic kinesin Eg5.
Product Specific Literature References
Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen: T.U. Mayer, et al.; Science 286, 971 (1999) Abstract
A combinatorial approach to recognition of chirality: preparation of highly enantioselective aryl-dihydropyrimidine selectors for chiral HPLC: K. Lewandowski, et al.; J. Comb. Chem. 1, 105 (1999) Abstract
Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5: Z. Maliga, et al.; Chem. Biol. 9, 989 (2002) Abstract
Inhibition of a mitotic motor protein: where, how, and conformational consequences: Y. Yan, et al.; J. Mol. Biol. 335, 547 (2004) Abstract
Monastrol, a selective inhibitor of the mitotic kinesin Eg5, induces a distinctive growth profile of dendrites and axons in primary cortical neuron cultures: S.Y. Yoon, et al.; Cell Motil. Cytoskeleton 60, 181 (2005) Abstract
Interaction of the mitotic kinesin Eg5 inhibitor monastrol with P-glycoprotein: T. Peters, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 372, 291 (2006) Abstract
A pathway of structural changes produced by monastrol binding to Eg5: Z. Maliga, et al.; J. Biol. Chem. 281, 7977 (2006) Abstract
Allosteric inhibition of kinesin-5 modulates its processive directional motility: B.H. Kwok, et al.; Nat. Chem. Biol. 2, 480 (2006) Abstract
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins / Related Products
 
 
ALX-430-128 Revised 21-Feb-08
Nutlin-3
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SYNONYMS (±)-4-[4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-piperazin-2-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-128-M001   1 mg 35.00 USD Add To Cart
ALX-430-128-M005   5 mg 160.00 USD Add To Cart
ALX-430-128-M025   25 mg 560.00 USD Add To Cart
Product Specification
FORMULA: C30H30Cl2N4O4
MW: 581.5
CAS NUMBER: 548472-68-0
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, DMSO, dimethyl formamide or acetonitrile; sparingly soluble in a 1:10 solution of ethanol:PBS, pH 7.2.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at -20°C.

We do not recommend storing the aqueous solution for more than one day.
HAZARD: IRRITANT.

Product Description
Inhibitor of p53/MDM2 interaction (IC50=0.09µM).
Product Specific Literature References
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2: L.T. Vassilev, et al.; Science 303, 844 (2004) Abstract
Reactivation of the p53 pathway as a treatment modality for KSHV-induced lymphomas: G. Sarek, et al.; J. Clin. Invest. 117, 1019 (2007) Abstract; Full Text
General Literature References
Drug discovery and p53: D.P. Lane, et al.; Drug Discov. Today 8, 347 (2003) Abstract
Further Categories Containing This Product:
Ubiquitin Ligases [E3]
 
 
ALX-430-151 Revised 22-Jul-08
RITA
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SYNONYMS Reactivation of p53 and Induction of Tumor Cell Apoptosis
2,5-bis(5-Hydroxymethyl-2-thienyl)furan
NSC652287
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-151-M001   1 mg 75.00 USD Add To Cart
ALX-430-151-M005   5 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C14H12O3S2
MW: 292.4
CAS NUMBER: 213261-59-7
PURITY: ≥98%
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Soluble in 100% ethanol (1mg/ml), DMSO (20mg/ml), dimethyl formamide (30mg/ml); 0.5mg/ml soluble in a 1:1 solution of dimethyl formamide: PBS (pH 7.2) (dilute the dimethyl formamide solution with PBS).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least two years after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Inhibitor of p53/HDM2 interaction. Activator of p53 function in tumors. Potently inhibits the growth of a variety of  cancer cell lines in the submicromolar range. It has been suggested that RITA selectively targets cells expressing p53 by other mechanisms than direct binding to the N-terminal domain of p53 [4].
Product Specific Literature References
[1] DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells: W. Nieves-Neira, et al.; Mol. Pharmacol. 56, 478 (1999) Abstract; Full Text
[2] Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism: M.I. Rivera, et al.; Biochem. Pharmacol. 57, 1283 (1999) Abstract
[3] Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors: N. Issaeva, et al.; Nat. Med. 10, 1321 (2004) Abstract
[4] NMR indicates that the small molecule RITA does not block p53-MDM2 binding in vitro: M. Krajewski, et al.; Nat. Med. 11, 1135 (2005) Abstract
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers)
 
 
ALX-430-161 Revised 15-Sep-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
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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) • Flavones • MDR Other Products
 
 
ALX-440-045 Revised 17-Jul-07
Methotrexate
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SYNONYMS (+)-Amethopterin
4-Amino-10-methylfolic acid
Methylaminopterin
MTX
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Enzyme Inhibitors)
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-440-045-M050   50 mg 25.00 USD Add To Cart
ALX-440-045-M100   100 mg 45.00 USD Add To Cart
ALX-440-045-M500   500 mg 135.00 USD Add To Cart
ALX-440-045-G001   1 g 240.00 USD Add To Cart
Product Specification
FORMULA: C20H22N8O5
MW: 454.5
CAS NUMBER: 59-05-2
MERCK INDEX: 14: 5985
PURITY: ≥98%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in alkaline solution; insoluble in water, 100% ethanol or ether.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: TOXIC. MAY BE CARCINOGENIC. MAY BE TERATOGENIC.

Product Description
Folic acid antagonist. Potent inhibitor of dihydrofolate reductase. Induces apoptosis. Inhibits DNA synthesis. Anticancer agent.
Product Specific Literature References
Immunosuppressive properties of methotrexate: apoptosis and clonal deletion of activated peripheral T cells: L. Genestier, et al.; J. Clin. Invest. 102, 322 (1998) Abstract
Methotrexate induces apoptotic cell death in human keratinocytes: M. Heenen, et al.; Arch. Dermatol. Res. 290, 240 (1998) Abstract
Activation-dependent lymphocyte apoptosis induced by methotrexate: R. Paillot, et al.; Transplant. Proc. 30, 2348 (1998) Abstract
Methotrexate inhibits the first committed step of purine biosynthesis in mitogen-stimulated human T-lymphocytes: a metabolic basis for efficacy in rheumatoid arthritis?: L.D. Fairbanks, et al.; Biochem. J. 342, 143 (1999)