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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-Fletcher; J. Pharmacol. Exp. Ther. 282, 459 (1997) Abstract; Full Text
Inhibition of NFkappaB-mediated interleukin-1beta-stimulated prostaglandin E2 formation by the marine natural product hymenialdisine: A. Roshak, et al.; J. Pharmacol. Exp. Ther. 283, 955 (1997) Abstract; Full Text
Inhibition of interleukin-1-induced proteoglycan degradation and nitric oxide production in bovine articular cartilage/chondrocyte cultures by the natural product, hymenialdisine: A.M. Badger, et al.; J. Pharmacol. Exp. Ther. 290, 587 (1999) Abstract; Full Text
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000) Abstract
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
An investigation of cell proliferation and soluble mediators induced by interleukin 1beta in human synovial fibroblasts: comparative response in osteoarthritis and rheumatoid arthritis: H. Inoue, et al.; Inflamm. Res. 50, 65 (2001) Abstract
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
Inhibition of cytokine production by hymenialdisine derivatives: V. Sharma, et al.; J. Med. Chem. 47, 3700 (2004) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • CDK & Cyclin Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • NF-kB Pathway Inhibitors • DNA Damage Checkpoint Other Products • Alkaloids • Natural Products for Cell Cycle Research • GSK-3 Inhibitors
 
 
ALX-350-291 Revised 19-Oct-07
Hymenidin
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SYNONYMS 2-Debromooroidin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-291-M001   1 mg 230.00 USD Add To Cart
Product Specification
FORMULA: C11H12BrN5O
MW: 310.2
CAS NUMBER: 107019-95-4
SOURCE/HOST: Isolated from Hymeniacidon sp.
PURITY: ≥95%
APPEARANCE: Amorphous solid.
SOLUBILITY: Soluble in DMSO or 100 % ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC. CYTOTOXIC.

Product Description
Antagonist of serotonergic receptors. Inhibitor of CDK5/p25 (IC50=4µM) and GSK-3β (IC50=12µM). 
Product Specific Literature References
A novel antagonist of serotonergic receptors, hymenidin, isolated from the Okinawan marine sponge Hymeniacidon sp: J. Kobayashi, et al.; Experientia 42, 1176 (1986) Abstract
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000)
Brominated pyrrole alkaloids from marine Agelas sponges reduce depolarization-induced cellular calcium elevation: U. Bickmeyer, et al.; Toxicon. 44, 45 (2004) Abstract
Marine compounds for the therapeutic treatment of neurological disorders: D. Alonso, et al.; Expert Opininon on Therapeutic Patents 15, 1377 (2005)
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • Alkaloids • Serotonergics & Serotonin Receptors/Related Products • Natural Products for Neurological Research
 
 
ALX-380-116 Revised 07-Apr-08
Hypothemycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-116-M001   1 mg 420.00 USD Add To Cart
ALX-380-116-C250   250 µg 140.00 USD Add To Cart
Product Specification
FORMULA: C19H22O8
MW: 378.4
CAS NUMBER: 76958-67-3
SOURCE/HOST: Isolated from Phoma sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.
Product Specific Literature References
Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Antitumor Antibiotics • Antibiotics - Protein Kinase Inhibitors • CDKs & Cyclins Other Products • Tyrosine Kinase Inhibitors • Ras Signalling Pathway Other Products • Antitumor Agents (DNA Interaction & Gene Regulation) • Antibiotics - Proteasome/Ubiquitin Modulators • Ubiquitination Other Products
 
 
ALX-270-361 Revised 28-Sep-07
Indirubin
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-361-M001   1 mg 50.00 USD Add To Cart
ALX-270-361-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C16H10N2O2
MW: 262.3
CAS NUMBER: 479-41-4
SOURCE/HOST: Synthetic.
PURITY: ≥98% (1H-NMR, HPLC)
APPEARANCE: Purple powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (0.3mg/ml). Sparingly soluble in aqueous buffers (12.5µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years when stored at +4°C in the dark. Stock solutions should be stored in the dark and used within 1 month.
HANDLING: Protect from light. Keep cool and dry.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR, IR, ESI-MS and UV.

Product Description
Inhibitor of cyclin-dependent kinases (CDK1/cyclin B (IC50=10µM), CDK2/cyclin A (IC50=2.2µM), CDK2/cyclin E (IC50=7.5µM), CDK4/cyclin D1 (IC50=12µM), CDK5/p35 (IC50=5.5µM)) [1] and of GSK-3β (IC50=600nM) [2]. Inhibits inflammatory reaction in delayed-type hypersensitivity in mice [3]. Ligand of human aryl hydrocarbon receptor [4]. Exhibits anti-cancer activity [5] [6].
Product Specific Literature References
[1] Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nature Cell Biol. 1, 60 (1999) Abstract
[2] 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
[3] Indirubin inhibits inflammatory reactions in delayed-type hypersensitivity: T. Kunikata, et al.; Eur. J. Pharmacol. 410, 93 (2000) Abstract
[4] Indirubin and indigo are potent aryl hydrocarbon receptor ligands present in human urine: J. Adachi, et al.; J. Biol. Chem. 276, 31475 (2001) Abstract; Full Text
[5] Molecular mechanisms of indirubin and its derivatives: novel anticancer molecules with their origin in traditional Chinese phytomedicine: G. Eisenbrand, et al.; J. Cancer Res. Clin. Oncol. 130, 627 (2004) Abstract
[6] Indirubin enhances tumor necrosis factor-induced apoptosis through modulation of nuclear factor-kappa B signaling pathway: G. Sethi, et al.; J. Biol. Chem. 281, 23425 (2006) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Indirubin is derived from various natural sources, such as Indigofera indica, Isatis tinctoria and I. indigotica by fermentation, oxidation and the presence of light as a by product of indigo formation. Indirubin is also present in human urine and fetal bovine serum [4]. Preclinical studies of indirubin its confirmed anti-tumor activity. Efficacy against chronic myelocytic leukemia was demonstrated in clinical trials in China [2].
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Further Categories Containing This Product:
GSK-3 Inhibitors • Antitumor Reagents Other Products • Anti-inflammatory Agents Other Products
 
 
ALX-270-271 Revised 17-Jul-07
Indirubin-3'-monoxime
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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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
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Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products • GSK-3 Inhibitors • Tau/Related Products
 
 
ALX-270-296 Revised 17-Jul-07
Indirubin-5-sulfonic acid . sodium salt
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SYNONYMS E226
Indirubin-5-sulphonate . Na
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-296-M001   1 mg 45.00 USD Add To Cart
ALX-270-296-M005   5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C16H9N2O5S . Na
MW: 341.3 . 23.0
PURITY: ≥98% (1H-NMR)
APPEARANCE: Black powder.
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of cyclin-dependent kinases (CDKs), with selectivity for CDK1/cyclin B (IC50=55nM), CDK2/cyclin A (IC50=35nM), CDK2/cyclin E (IC50=150nM), CDK4/cyclin D1 (IC50=300nM), CDK5/p35 (IC50=65nM) and GSK-3β (IC50=280nM).
Product Specific Literature References
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nat. Cell. Biol. 1, 60 (1999)
Inhibitor binding to active and inactive cdk2. the crystal structure of cdk2-cyclin a/indirubin-5-sulphonate: T.G. Davies, et al.; Structure (Camb) 9, 389 (2001) Abstract
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
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
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Further Categories Containing This Product:
GSK-3 Inhibitors
 
 
ALX-350-347 Revised 21-May-08 New product
Indole-3-carbinol
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SYNONYMS I3C
Indole-3-methanol
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-347-M250   250 mg 40.00 USD Add To Cart
ALX-350-347-G001   1 g 90.00 USD Add To Cart
Product Specification
FORMULA: C9H9NO
MW: 147.2
CAS NUMBER: 700-06-1
RTECS: NL9483000
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol; sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Anticancer agent. Inhibits carcinogenesis at the initiation stage but has been shown to enhance tumor incidence at a post-initiation stage. Inhibits the expression of cyclin-dependent kinase 6 (CDK6) and induces G1 cell cycle arrest independent of estrogen receptor signalling. Causes a dose-dependent increase in E-cadherin and BRCA1 expression.
Product Specific Literature References
Inhibition of polycyclic aromatic hydrocarbon-induced neoplasia by naturally occurring indoles: L.W. Wattenberg & W.D. Loub; Cancer Res. 38, 1410 (1978) Abstract
Indole-3-carbinol inhibits the expression of cyclin-dependent kinase-6 and induces a G1 cell cycle arrest of human breast cancer cells independent of estrogen receptor signaling: C.M. Cover, et al.; J. Biol. Chem. 273, 3838 (1998) Abstract; Full Text
Suppression of breast cancer invasion and migration by indole-3-carbinol: associated with up-regulation of BRCA1 and E-cadherin/catenin complexes: Q. Meng, et al.; J. Mol. Med. 78, 155 (2000) Abstract; Full Text
Therapeutic intervention of experimental breast cancer bone metastasis by indole-3-carbinol in SCID-human mouse model: K.M. Rahman, et al.; Mol. Cancer Ther. 5, 2747 (2006) Abstract; Full Text
3,3’-Diindolylmethane stimulates murine immune function in vitro and in vivo: L. Xue, et al.; J. Nutr. Biochem. 19, 336 (2008) Abstract
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Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products • Natural Products for Cell Cycle Research • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-270-424 Revised 13-Feb-07
5-Iodo-indirubin-3'-monoxime
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-424-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C16H10IN3O2
MW: 403.2
PURITY: ≥98% (1H-NMR)
APPEARANCE: Dark red solid.
SOLUBILITY: Soluble in DMSO (1M).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent inhibitor of GSK-3β (IC50=9nM). Also inhibits CDK1/cyclin B (IC50=25nM) and CDK5/p25 (IC50=20nM) by binding to the ATP-binding pocket.
Product Specific Literature References
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
Related Products
Further Categories Containing This Product:
GSK-3 Inhibitors
 
 
ALX-450-006 Revised 07-Apr-08
Ionomycin (free acid)