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Cell Cycle Blockers & Inhibitors / Related Products
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ALX-380-026 Revised 26-Jun-08
Monensin . sodium salt
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-380-026-M100   100 mg 25.00 USD Add To Cart
ALX-380-026-G001   1 g 63.00 USD Add To Cart
Product Specification
FORMULA: C36H61O11 . Na
MW: 669.9 . 23.0
CAS NUMBER: 22373-78-0
MERCK INDEX: 14: 6246
PURITY: ≥90%
APPEARANCE: White to light yellow powder.
SOLUBILITY: Soluble in chloroform or DMSO. Clear solution (5%) in methanol with heat. Slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Antibiotic that functions as Na+ ionophore. Blocks glycoprotein secretion. Inhibits proliferation of several lymphoma cell lines through cell cycle arrest and apoptosis.
Product Specific Literature References
Monensin, a new biologically active compound. I. Discovery and isolation: M. E. Haney, Jr. & M. M. Hoehn; Antimicrobial Agents Chemother. (Bethesda) 7, 349 (1967) Abstract
Solution chemistry of monensin and its alkali metal ion complexes. Potentiometric and spectroscopic studies
:
P.G. Gertenbach & A.I. Popov; JACS 97, 4738 (1975)
Undersulfated proteoglycans are secreted by cultured chondrocytes in the presence of the ionophore monensin: K. Tajiri, et al.; J. Biol. Chem. 255, 6036 (1980) Abstract; Full Text
Expression of membrane IGM by a human B lymphoblastoid cell line in the presence of monensin: R.T. Kubo and M.L. Pigeon; Mol. Immunol. 20, 345 (1983) Abstract
Alteration of intracellular traffic by monensin; mechanism, specificity and relationship to toxicity: H. H. Mollenhauer, et al.; Biochim. Biophys. Acta 1031, 225 (1990), Review Abstract
Monensin-mediated growth inhibition in human lymphoma cells through cell cycle arrest and apoptosis: W. H. Park, et al.; Br. J. Haematol. 119, 400 (2002) Abstract
 
 
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
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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
 
 
ALX-350-013 Revised 23-Oct-07
Olomoucine (high purity)
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SYNONYMS 6-Benzylamino-2-(2-hydroxyethylamino)-9-methylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-013-M005   5 mg 65.00 USD Add To Cart
ALX-350-013-M025   25 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C15H18N6O
MW: 298.4
CAS NUMBER: 101622-51-9
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent and very selective inhibitor of cdc2, CDK and other cyclin-related kinases by competing for the ATP-binding domain of the kinase. Inhibits CDK1/cyclin B (IC50=7µM), CDK2 (IC50=7µM) and CDK5/p35 (IC50=3µM). Also inhibits DNA synthesis in interleukin-2 stimulated T lymphocytes and triggers G1 arrest similar to that observed in interleukin-2 deprived cells. Can be used to synchronize cells in G1. Triggers apoptosis in target tumor cells in vitro and in vivo and in maturing cerebellar granule neurons.
Product Specific Literature References
Inhibition of cyclin-dependent kinases by purine analogues: J. Vesely, et al.; Eur. J. Biochem. 224, 771 (1994) Abstract
Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases: R.T. Abraham, et al.; Biol. Cell 83, 105 (1995) Abstract
Mitotic disassembly of the Golgi apparatus in vivo: T. Mistelli & G. Warren; J. Cell Sci. 108, 2715 (1995) Abstract
Chemical inhibitors of cyclin-dependent kinases: L. Meijer, et al.; Meth. Enzymol. 283, 113 (1997) Abstract
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
The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res. 245, 8 (1998) Abstract
Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004) Abstract
 
 
ALX-380-210 Revised 08-Apr-08
7-Oxostaurosporine
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SYNONYMS Antibiotic BMY 41950
Antibiotic RK 1409
LCM76-L
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Protein Kinase Inhibitors
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ALX-380-210-M001   1 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C28H24N4O4
MW: 480.5
CAS NUMBER: 141196-69-2
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5345.
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, methanol or 100% ethanol; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Antibiotic. Potent inhibitor of protein kinase C (PKC). Inhibits the cell cycle at the G2 stage.

Product Specific Literature References
A new inhibitor of protein kinase C, RK-1409 (7-oxostaurosporine). I. Taxonomy and biological activity: H. Osada, et al.; J. Antibiot. 45, 189 (1992) Abstract
A new inhibitor of protein kinase C, RK-1409 (7-oxostaurosporine). II. Fermentation, isolation, physico-chemical properties and structure: H. Koshino, et al.; J. Antibiot. 45, 195 (1992) Abstract
 
 
ALX-340-047 Revised 04-Dec-08
Prostaglandin A2
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SYNONYMS Medullin
Prosta-5,10,13-trien-1-oic acid, 15-hydroxy-9-oxo-, (5Z,13E,15S)-
PRODUCT LINE Inflammation
PRODUCT CATEGORY Prostaglandins & Prostaglandin Analogs
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ALX-340-047-M001   1 mg 33.00 USD Add To Cart
ALX-340-047-M005   5 mg 147.00 USD Add To Cart
Product Specification
FORMULA: C20H30O4
MW: 334.5
CAS NUMBER: 13345-50-1
CONCENTRATION: 10mg/ml
PURITY: ≥98%
FORMULATION: Liquid. Solution in methyl acetate.
SOLUBILITY: Soluble in 100% ethanol (100mg/ml), DMSO (50mg/ml) or dimethyl formamide (75mg/ml); slightly soluble in PBS, pH 7.2 (2.4mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. PGAwill be degraded to PGB2 in basic solutions (pH > 7.4). We do not recommend storing aqueous solutions for more than one day.

Product Description
Blocks cell cycle at the G1 and G2/M phase [1] by inhibiting G1 phase cyclin dependent kinases [2] downregulating cyclin D1 [3]. Modulates all three aspects of the glutathione-mediated biotransformation system, i.e. GSH levels, glutathione S-transferase activity and transport of GSH conjugates [4].
Product Specific Literature References
[1] Prostaglandin A2 blocks the activation of G1 phase cyclin-dependent kinase without altering mitogen-activated protein kinase stimulation: M. Hitomi, et al.; J. Biol. Chem. 271, 9376 (1996) Abstract; Full Text
[2] p21Waf1 inhibits the activity of cyclin dependent kinase 2 by preventing its activating phosphorylation: M. Hitomi, et al.; Oncogene 17, 959 (1998) Abstract
[3] Down-regulation of cyclin D1 expression by prostaglandin A(2) is mediated by enhanced cyclin D1 mRNA turnover: S. Lin, et al.; Mol. Cell. Biol. 20, 7903 (2000) Abstract; Full Text
[4] Interactions of prostaglandin A2 with the glutathione-mediated biotransformation system: M.L. van Iersel, et al.; Biochem. Pharmacol. 57, 1383 (1999) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-385-001 Revised 08-Apr-08
Quercetin . dihydrate
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SYNONYMS 3,3',4',5,7-Pentahydroxyflavone . 2H2O
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonols
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ALX-385-001-G005   5 g 15.00 USD Add To Cart
ALX-385-001-G025   25 g 45.00 USD Add To Cart
Product Specification
FORMULA: C15H10O7 . 2H2O
MW: 302.2 . 36.0
CAS NUMBER: 6151-25-3
MERCK INDEX: 14: 8034
RTECS: LK8950000
SOURCE/HOST: Isolated from Sophora japonica L.
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow powder with a green or brown cast.
SOLUBILITY: Soluble in 100% ethanol or 1M sodium hydroxide; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: MAY BE MUTAGENIC. TOXIC.

Product Description
Antioxidant flavonoid. Inhibitor of mitochondrial ATPase, cAMP- and cGMP-phosphodiesterases. Inhibitor of protein tyrosine kinases and protein kinase C (PKC). Induces apoptosis. Blocks cells at the G0/G1 interface. Activator of human deacetylase SIRT1. Reversible inhibitor of fatty acid synthase (FAS). Inhibits the production of the inflammatory mediators nitric oxide (NO), TNF-α and IL-12 in activated macrophages.
Product Specific Literature References
Effects of quercetin and F1 inhibitor on mitochondrial ATPase and energy-linked reactions in submitochondrial particles: D.R. Lang & E. Racker; Biochim. Biophys. Acta 333, 180 (1974)
Flavonoid compounds are potent inhibitors of cyclic AMP phosphodiesterase: A. Beretz, et al.; Experientia 34, 1054 (1978) Abstract
Flavonoids are selective cyclic GMP phosphodiesterase inhibitors: M. Ruckstuhl, et al.; Biochem. Pharmacol. 28, 535 (1979) Abstract
The effect of quercetin on the phosphorylation activity of the Rous sarcoma virus transforming gene product in vitro and in vivo: Y. Graziani, et al.; Eur. J. Biochem. 135, 583 (1983) Abstract
Inhibition of the calcium- and phospholipid-dependent protein kinase activity from mouse brain cytosol by quercetin: M. Gschwendt, et al.; BBRC 117, 444 (1983) Abstract
Tyrosine protein kinase activity in the DMBA-induced rat mammary tumor: inhibition by quercetin: J. Levy, et al.; BBRC 123, 1227 (1984) Abstract
The phospholipid- and calcium-dependent protein kinase as a target in tumor chemotherapy: H. Grunicke, et al.; Adv. Enzyme Regul. 28, 201 (1989) Abstract
Induction of apoptosis by quercetin: involvement of heat shock protein: Y.Q. Wei, et al.; Cancer Res. 54, 4952 (1994) Abstract
Multiple effects of tyrosine kinase inhibitors on vascular smooth muscle contraction: C.M. Filipeanu, et al.; Eur. J. Pharmacol. 281, 29 (1995) Abstract
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Molecular mechanisms in the antiproliferative action of quercetin: B. Csokay, et al.; Life Sci. 60, 2157 (1997) Abstract
Modulation of the heat-induced activation of mitogen-activated protein (MAP) kinase by quercetin: Y. Nagasaka & K. Nakamura; Biochem. Pharmacol. 56, 1151 (1998) Abstract
Quercetin-induced apoptosis in colorectal tumor cells: possible role of EGF receptor signaling: M. Richter, et al.; Nutr. Cancer 34, 88 (1999) Abstract
Quercetin and anti-CD95(Fas/Apo1) enhance apoptosis in HPB-ALL cell line: M. Russo, et al.; FEBS Lett. 462, 322 (1999) Abstract
The effect of quercetin on induction of apoptosis: J. Rzymowska, et al.; Folia Histochem. Cytobiol. 37, 125 (1999) Abstract
Quercetin, coenzyme Q10, and L-canavanine as protective agents against lipid peroxidation and nitric oxide generation in endotoxin-induced shock in rat brain: H.M. Abd El-Gawad & A.E. Khalifa; Pharmacol. Res. 43, 257 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003)
Presence of fatty acid synthase inhibitors in the rhizome of Alpinia officinarum hance: B.H. Li and W.X. Tian; J. Enzyme Inhib. Med. Chem. 18, 349 (2003) Abstract
Inhibitory effects of the flavonoids isolated from Waltheria indica on the production of NO, TNF-alpha and IL-12 in activated macrophages: Y.K. Rao, et al.; Biol. Pharm. Bull. 28, 912 (2005) Abstract
Pharmacological inhibitors of Fatty Acid Synthase (FASN)--catalyzed endogenous fatty acid biogenesis: a new family of anti-cancer agents?: R. Lupu & J. A. Menendez; Curr. Pharm. Biotechnol. 7, 483 (2006), (Review) Abstract
Onions: a source of unique dietary flavonoids: R. Slimestad, et al.; J. Agric. Food Chem. 55, 10067 (2007) Abstract
 
 
ALX-380-092 Revised 03-Jul-08
Radicicol
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SYNONYMS Monorden
1aS-(1aR*,2Z,4E,14*,15aR*)]-8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-092-M001   1 mg 75.00 USD Add To Cart
ALX-380-092-M005   5 mg 295.00 USD Add To Cart
Product Specification
FORMULA: C18H17ClO6
MW: 364.8
CAS NUMBER: 12772-57-5
MERCK INDEX: 14: 6253
RTECS: RR1105000
SOURCE/HOST: Isolated from Humicola fuscoatra.
PURITY: ≥98% (HPLC)
APPEARANCE: White to light yellow powder.
SOLUBILITY: Soluble in DMSO, methanol or acetone.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Antifungal macrocyclic lactone antibiotic with antimalarial activity. Potent inhibitor of HSP90. Binds more strongly to HSP90 (nanomolar affinity) than to Grp94. Also binds to yeast HSP90, E. coli HtpG and TRAP-1. Non-competitive inhibitor of ATP citrate lyase. Anti-angiogenic. Specifically inhibits the interaction between HIF-1α/Arnt heterodimer and the hypoxia-responsive element (HRE), reducing VEGF expression. Protein tyrosine kinase inhibitor, e.g. p60v-src (IC50=0.27nM). Inhibitor of cyclooxygenase-2 (COX-2) expression (IC50=27nM) without affecting COX-1 expression in LPS-stimulated macrophages. Induces the differentiation of HL-60 cells into macrophages, blocking cell cycle at G1 and G2. Suppressor of NIH 3T3 cell transformation by diverse oncogenes such as mos, ras and src in part by blocking the key signal transduction intermediates such as MAP kinase and GAP-associated p62. Inhibitor of AP-1-, NF-κB- and serum response factor (SRF)-mediated transcription (e.g. expression of iNOS). Represses the transcriptional function of the estrogen receptor. Inhibits archeal growth and DNA topoisomerase VI (a Topo IIB family topoisomerase). Blocks replication of negative-strand RNA viruses.
Product Specific Literature References
Potent and specific inhibition of p60v-src protein kinase both in vivo and in vitro by radicicol: H.J. Kwon, et al.; Cancer Res. 52, 6926 (1992) Abstract
Radicicol, a microbial cell differentiation modulator, inhibits in vivo angiogenesis: T. Oikawa, et al.; Eur. J. Pharmacol. 241, 221 (1993) Abstract
Radicicol, a protein tyrosine kinase inhibitor, suppresses the expression of mitogen-inducible cyclooxygenase in macrophages stimulated with lipopolysaccharide and in experimental glomerulonephritis: P. Chanmugam, et al.; J. Biol. Chem. 270, 5418 (1995) Abstract; Full Text
Suppression of RAS and MOS transformation by radicicol: J.F. Zhao, et al.; Oncogene 11, 161 (1995) Abstract
Induction of differentiation of HL-60 cells by the anti-fungal antibiotic, radicicol: Y. Shimada, et al.; J. Antibiot. 48, 824 (1995) Abstract
Radicicol inhibits tyrosine phosphorylation of the mitotic Src substrate Sam68 and retards subsequent exit from mitosis of Src-transformed cells: I. Pillay, et al.; Cell Growth Differ. 7, 1487 (1996) Abstract
Radicicol leads to selective depletion of Raf kinase and disrupts K-Ras-activated aberrant signaling pathway: S. Soga, et al.; J. Biol. Chem. 273, 822 (1998) Abstract; Full Text
Antimalarial activity of radicicol, heptelidic acid and other fungal metabolites: Y. Tanaka, et al.; J. Antibiot. 51, 153 (1998) Abstract
Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol: S.V. Sharma, et al.; Oncogene 16, 2369 (1998) Abstract
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin: S.M. Roe, et al.; J. Med. Chem. 42, 260 (1999) Abstract
T.W. Schulte, et al.; Mol. Endocrinol. 13, 1435 (1999) Abstract; Full Text
Radicicol suppresses expression of inducible nitric-oxide synthase by blocking p38 kinase and nuclear factor-kappaB/Rel in lipopolysaccharide-stimulated macrophages: Y.J. Jeon, et al.; J. Pharmacol. Exp. Ther. 294, 548 (2000) Abstract; Full Text
Radicicol binds and inhibits mammalian ATP citrate lyase: S.W. Ki, et al.; J. Biol. Chem. 275, 39231 (2000) Abstract; Full Text
Radicicol suppresses transformation and restores tropomyosin-2 expression in both ras- and MEK-transformed cells without inhibiting the Raf/MEK/ERK signaling cascade: P.N. Kim, et al.; Cell Growth Differ. 12, 543 (2001) Abstract; Full Text
Radicicol-sensitive peptide binding to the N-terminal portion of GRP94: S. Vogen, et al.; J. Biol. Chem. 277, 40742 (2002) Abstract; Full Text
Reduction of hypoxia-induced transcription through the repression of hypoxia-inducible factor-1alpha/aryl hydrocarbon receptor nuclear translocator DNA binding by the 90-kDa heat-shock protein inhibitor radicicol: E. Hur, et al.; Mol. Pharmacol. 62, 975 (2002) Abstract; Full Text
Radicicol represses the transcriptional function of the estrogen receptor by suppressing the stabilization of the receptor by heat shock protein 90: M.O. Lee, et al.; Mol. Cell Endocrinol. 188, 47 (2002) Abstract
Development of radicicol analogues: S. Soga, et al.; Curr. Cancer Drug Targets 3, 359 (2003) Abstract
Heat shock protein 90 (Hsp90) chaperone complex inhibitor, radicicol, potentiated radiation-induced cell killing in a hormone-sensitive prostate cancer cell line through degradation of the androgen receptor: K. Harashima, et al.; Int. J. Radiat. Biol. 81, 63 (2005) Abstract
Inhibition of archaeal growth and DNA topoisomerase VI activities by the Hsp90 inhibitor radicicol: D. Gadelle, et al.; Nucleic Acid Res. 33, 2310 (2005) Abstract
Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site: M.K. Hadden, et al.; Curr. Top. Med. Chem. 6, 1173 (2006), Review Abstract
The topoisomerase II-Hsp90 complex: a new chemotherapeutic target?: C.R. Barker, et al.; Int. J. Cancer 118, 2685 (2006) Abstract
Structural basis for topoisomerase VI inhibition by the anti-Hsp90 drug radicicol: K.D. Corbett & J.M. Berger; Nucleic Acids Res. 34, 4269 (2006) Abstract
Chemistry and biology of resorcylic acid lactones: N. Winssinger & S. Barluenga; Chem. Commun. (Camb.) 22 (2007) Abstract
Antiviral activity and RNA polymerase degradation following Hsp90 inhibition in a range of negative strand viruses: J.H. Connor, et al.; Virology 362, 109 (2007) Abstract
 
 
ALX-270-346 Revised 28-May-08
Ratjadone A (synthetic)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-346-C002   2 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: 456.6
CAS NUMBER: 163564-92-9
SOURCE/HOST: Synthetic.
PURITY: ≥95%
FORMULATION: Liquid. Solution in methanol.