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Cell Cycle
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ALX-350-236 Revised 04-Sep-08
Homoharringtonine
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Immunomodulators
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ALX-350-236-M001   1 mg 45.00 USD Add To Cart
ALX-350-236-M005   5 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C29H39NO9
MW: 545.6
CAS NUMBER: 26833-87-4
RTECS: FK0260000
SOURCE/HOST: Isolated from Cephalotaxus hainanensis.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: VERY TOXIC.

Product Description
Cephalotaxine alkaloid. Inhibits the formation of diphenylalanine and acetylphenylalanyl-puromycin in liver ribosomes. Has promising activity in hematologic malignancies. Lowers the levels of telomerase. Induces apoptosis.
Product Specific Literature References
Different effects of L-histidinol and homoharringtonine on 5- fluorouracil and bis-chloroethylnitrosourea activity in a murine model: R.C. Warrington & W.D. Fang; Anticancer Res. 11, 1879 (1991) Abstract
Selective inhibition of the polypeptide chain elongation in eukaryotic cells: R.M. Tujebajeva, et al.; Biochim. Biophys. Acta 1129, 177 (1992) Abstract
Homoharringtonine is safe and effective for patients with acute myelogenous leukemia: E. Feldman, et al.; Leukemia 6, 1185 (1992) Abstract
Homoharringtonine: history, current research, and future direction: H.M. Kantarjian, et al.; Cancer 92, 1591 (2001), Review Abstract
Homoharringtonine: a new treatment option for myeloid leukemia: C.Y. Luo, et al.; Hematology 9, 259 (2004), Review Abstract
Homoharringtonine-induced apoptosis of human leukemia HL-60 cells is associated with down-regulation of telomerase: W.Z. Xie, et al.; Am. J. Chin. Med. 34, 233 (2006) Abstract
Further Categories Containing This Product:
Natural Products - Antitumor Reagents • Telomerase / Related Products • Alkaloids • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-270-373 Revised 11-Aug-06
trans-HR22C16
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors / Related Products
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ALX-270-373-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C23H23N3O3
MW: 389.5
CAS NUMBER: 462630-41-7
PURITY: ≥95%
APPEARANCE: Yellow to ocher solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description

Cell permeable non-tubulin-interacting mitosis inhibitor. Blocks mitosis (IC50=800nM) by binding to the mitotic kinesin Eg5.
Product Specific Literature References
HR22C16: A Potent Small-Molecule Probe for the Dynamics of Cell Division: S. Hotha, et al.; Angew. Chem. Int. Ed. Engl. 42, 2379 (2003) Abstract
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins / Related 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 18-Nov-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
ALX-350-289-M001   1 mg 340.00 USD Add To Cart
Product Specification
FORMULA: C11H10BrN5O2
MW: 324.1
CAS NUMBER: 82005-12-7
SOURCE/HOST: Isolated from sponge Axinella carteri.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.
IDENTITY: Identity determined by 1H- NMR and MS.

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:
CDK & Cyclin Inhibitors • MAPK Pathway Inhibitors • Natural Products - NF-kB Pathway Inhibitors • NF-kB Pathway Inhibitors • Natural Products for Cell Cycle Research • Alkaloids • Natural Products - Nitric Oxide Pathway Modulators • DNA Damage Checkpoint Other Products • GSK-3 Inhibitors • Marine Natural Products
 
 
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 • Natural Products for Neurological Research • Alkaloids • Serotonergics & Serotonin Receptors / Related Products • Marine Natural Products
 
 
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-C250   250 µg 140.00 USD Add To Cart
ALX-380-116-M001   1 mg 420.00 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 • Antibiotics - Protein Kinase Inhibitors • Tyrosine Kinase Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Antibiotics • Antibiotics - Proteasome / Ubiquitin Modulators • Ubiquitination Other Products • CDKs & Cyclins Other Products • Ras Signalling Pathway 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: Keep cool and dry. Protect from light.
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:
Anti-inflammatory Agents Other Products • GSK-3 Inhibitors • Antitumor Reagents 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:
Tau / Related Products • Cell Cycle Blockers & Inhibitors / Related Products • GSK-3 Inhibitors
 
 
ALX-270-296 Revised 15-Aug-08
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