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Chemokines & Cytokines
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ALX-350-084 Revised 07-Apr-08
Lavendustin C methyl ester
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SYNONYMS Compound 5 methyl ester
5-Amino-N-(2,5-dihydroxybenzyl)methyl salicylate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-084-M001   1 mg 50.00 USD Add To Cart
ALX-350-084-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C15H15NO5
MW: 289.3
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Inhibitor of EGFR tyrosine kinase with improved bioavailability over lavendustin C (Prod. No. ALX-270-066).
Product Specific Literature References
Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor- associated tyrosine kinase activity: H. Chen, et al.; J. Med. Chem. 36, 4094 (1993) Abstract
Structure-activity relationships in a series of 5-[(2,5- dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: importance of additional hydrophobic aromatic interactions: H. Chen, et al.; J. Med. Chem. 37, 845 (1994) Abstract
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Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors
 
 
ALX-350-091 Revised 14-Jan-08
Lavendustin A methyl ester
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-091-M001   1 mg 50.00 USD Add To Cart
ALX-350-091-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C22H21NO6
MW: 395.4
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cell permeable ester of lavendustin A (Prod. No. ALX-350-007).
Product Specific Literature References
Inhibition of tyrosine kinase and epidermal growth factor receptor internalization by lavendustin A methyl ester in cultured A431 cells: T. Onoda, et al.; Drugs Exp. Clin. Res. 16, 249 (1990) Abstract
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Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors
 
 
ALX-350-246 Revised 07-Oct-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol. Specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Glutathione S-Transferase • Chalcones • Natural Products - Chemopreventive Agents • EGFR Kinase Inhibitors • Natural Products - Antioxidants • Natural Products - Anti-inflammatory Agents • IkB Kinases [IKKs] / Related Products • Sirtuins / Related Products • Glutathione / Related Products • Phosphodiesterases / Related Products
 
 
ALX-350-256 Revised 07-Oct-08
(+)-Aeroplysinin-1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-256-M001   1 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C9H9Br2NO3
MW: 339.0
CAS NUMBER: 28656-91-9
SOURCE/HOST: Isolated from Aplysina aerophoba.
PURITY: ≥97%
APPEARANCE: Oil.
SOLUBILITY: Soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Displays cytostatic and cytotoxic activity. Inhibitor of EGFR kinase. Shows antiangiogenic activity.
Product Specific Literature References
Aeroplysinin-1, an antibacterial bromo-compound from the sponge Verongia aerophoba: E. Fattorusso, et al.; J. Chem. Soc. 1, 16 (1972) Abstract
Cytostatic activity of aeroplysinin-1 against lymphoma and epithelioma cells: M.H. Kreuter, et al.; Z. Naturforsch. [C] 44, 680 (1989) Abstract
Inhibition of intrinsic protein tyrosine kinase activity of EGF-receptor kinase complex from human breast cancer cells by the marine sponge metabolite (+)-aeroplysinin-1: M.H. Kreuter, et al.; Comp. Biochem. Physiol. B 97, 151 (1990) Abstract
Production of the cytostatic agent aeroplysinin by the sponge Verongia aerophoba in in vitro culture: M.H. Kreuter, et al.; Comp. Biochem. Physiol. 101C, 183 (1992) Abstract
Antibiotic and cytotoxic activity of brominated compounds from the marine sponge Verongia aerophoba: R. Teeyapant, et al.; Z. Naturforsch. [C] 48, 939 (1993) Abstract
Cytotoxicity and mode of action of aeroplysinin-1 and a related dienonefrom the sponge Aplysina aerophoba: A. Koulman, et al.; J. Nat. Prod. 59, 591 (1996) Abstract
Antiangiogenic activity of aeroplysinin-1, a brominated compound isolated from a marine sponge: S. Rodriguez-Nieto, et al.; FASEB J. 16, 261 (2002) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors • Natural Products with Antibiotic Activity • Natural Products for Angiogenesis Research • Natural Products - Antitumor Reagents • Marine Natural Products
 
 
ALX-380-216 Revised 20-Jun-08
Reveromycin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-216-MC01   0.1 mg 150.00 USD Add To Cart
ALX-380-216-MC25   0.25 mg 320.00 USD Add To Cart
Product Specification
SEQUENCE: 134615-37-5
FORMULA: C36H52O11
MW: 660.8
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5344.
PURITY: ≥99% (HPLC)
APPEARANCE: White to tan solid.
SOLUBILITY: Soluble in ethyl acetate, 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Unstable in acidic conditions.

Product Description
Antibiotic. Dominant analog of the reveromycin complex. Inhibitor of the mitogenic activity of epidermal growth factor (EGF). G1 phase cell cycle inhibitor, selectively inhibiting isoleucyl-tRNA synthetase. Displays antiproliferative as well as potent antifungal activity. Induces apoptosis in osteoclasts thus inhibiting bone resorption.
Product Specific Literature References
Reveromycins, new inhibitors of eukaryotic cell growth. I. Producing organism, fermentation, isolation and physico-chemical properties: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1409 (1992) Abstract
Reveromycins, new inhibitors of eukaryotic cell growth. II. Biological activities: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1414 (1992) Abstract
Chemical modification of reveromycin A and its biological activities: T. Shimizu, et al.; Bioorg. Med. Chem. Lett. 12, 3363 (2002) Abstract
Identification of Saccharomyces cerevisiae isoleucyl-tRNA synthetase as a target of the G1-specific inhibitor Reveromycin A: Y. Miyamoto, et al.; J. Biol. Chem. 277, 28810 (2002) Abstract; Full Text
Reveromycin A inhibits osteolytic bone metastasis of small-cell lung cancer cells, SBC-5, through an antiosteoclastic activity: H. Muguruma, et al.; Clin. Cancer Res. 11, 8822 (2005) Abstract; Full Text
Reveromycin A, an agent for osteoporosis, inhibits bone resorption by inducing apoptosis specifically in osteoclasts: J.T. Woo, et al.; PNAS 103, 4729 (2006) Abstract; Full Text
Molecular pathogenesis and its therapeutic modalities of lung cancer metastasis to bone: S. Sone and S. Yano; Cancer Metastasis Rev. 26, 685 (2007) Abstract
Regulation of osteoclast polarization: N. Takahashi, et al.; Odontology 95, 1 (2007), (Review) Abstract
Further Categories Containing This Product:
EGFR Kinase Inhibitors • Bone Metabolism Other Products • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-217 Revised 08-Apr-08
Reveromycin B
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-217-MC25   0.25 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C36H52O11
MW: 660.8
CAS NUMBER: 144860-68-4
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5344.
PURITY: ≥90% (HPLC)
APPEARANCE: White to tan solid.
SOLUBILITY: Soluble in ethyl acetate, 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Unstable in acidic conditions.

Product Description
Antibiotic. Much less active analog of reveromycin A (Prod. No. ALX-380-216), which is a G1 phase cell cycle inhibitor and induces apoptosis in osteoclasts. Useful negative control in resolving the mode of action of this class.
Product Specific Literature References
Reveromycins, new inhibitors of eukaryotic cell growth. I. Producing organism, fermentation, isolation and physico-chemical properties: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1409 (1992) Abstract
Reveromycins, new inhibitors of eukaryotic cell growth. II. Biological activities: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1414 (1992) Abstract
Further Categories Containing This Product:
Bone Metabolism Other Products • EGFR Kinase Inhibitors • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-218 Revised 08-Apr-08
Reveromycin C
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-218-MC25   0.25 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C37H54O11
MW: 674.8
CAS NUMBER: 144860-69-5
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5344.
PURITY: ≥95% (HPLC)
APPEARANCE: White to tan solid.
SOLUBILITY: Soluble in ethyl acetate, 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Unstable in acidic conditions.

Product Description
Antibiotic. Minor component of the reveromycin complex with similar biological profile as reveromycin A (Prod. No. ALX-380-216), which is a G1 phase cell cycle inhibitor and induces apoptosis in osteoclasts. Generally more potent than reveromycin A. Inhibitor of the mitogenic activity of epidermal growth factor (EGF).
Product Specific Literature References
Reveromycins, new inhibitors of eukaryotic cell growth. I. Producing organism, fermentation, isolation and physico-chemical properties: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1409 (1992) Abstract
Reveromycins, new inhibitors of eukaryotic cell growth. II. Biological activities: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1414 (1992) Abstract
Further Categories Containing This Product:
Bone Metabolism Other Products • EGFR Kinase Inhibitors • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-219 Revised 08-Apr-08
Reveromycin D
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-219-MC25   0.25 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C37H54O11
MW: 674.8
CAS NUMBER: 144860-70-8
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5344.
PURITY: ≥95% (HPLC)
APPEARANCE: White to tan solid.
SOLUBILITY: Soluble in ethyl acetate, 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Unstable in acidic conditions.

Product Description
Antibiotic. Minor component of the reveromycin complex. Inhibitor of the mitogenic activity of epidermal growth factor (EGF). More active than its straight chain analog reveromycin C (Prod. No. ALX-380-218).
Product Specific Literature References
Reveromycins, new inhibitors of eukaryotic cell growth. I. Producing organism, fermentation, isolation and physico-chemical properties: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1409 (1992) Abstract
Reveromycins, new inhibitors of eukaryotic cell growth. II. Biological activities: H. Takahashi, et al.; J. Antibiot. (Tokyo) 45, 1414 (1992) Abstract
Further Categories Containing This Product:
Bone Metabolism Other Products • EGFR Kinase Inhibitors • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-281 Revised 20-Jun-08
PKC412
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SYNONYMS 4’-N-Benzoyl-staurosporine
Midostaurin
CGP 41251
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-380-281-M001   1 mg 60.00 USD Add To Cart
ALX-380-281-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C35H30N4O4
MW: 570.6
CAS NUMBER: 120685-11-2
MERCK INDEX: 14: 6185
SOURCE/HOST: Semisynthetic product prepared from staurosporine (a fermentation product of Streptomyces staurosporeus) (Prod. No. ALX-380-014).
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (10mg/ml), MDC (10mg/ml) or methanol (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Inhibitor of a variety of serine/threonine and tyrosine kinases, like protein kinase C (PKC), cyclic AMP-dependent protein kinase (PKA), S6 kinase, Akt (protein kinase B; PKB) and epidermal growth factor receptor (EGFR) tyrosine kinase activity. Potently inhibits FLT-3 kinase in vitro and in vivo. Apoptosis inducer. Showed broad antiproliferative activity against various tumor cell lines. Selectively inhibits T lymphocyte production of TNF-α. Upregulates endothelial nitric oxide synthase (eNOS; NOS III).
Product Specific Literature References
Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251: E. Andrejauskas-Buchdunger & U. Regenass; Cancer Res. 52, 5353 (1992) Abstract; Full Text
Analogs of staurosporine: potential anticancer drugs?: A. Gescher; Gen. Pharmacol. 31, 721 (1998), (Review) Abstract
Differential effects of UCN-01, staurosporine and CGP 41 251 on cell cycle progression and CDC2/cyclin B1 regulation in A431 cells synchronized at M phase by nocodazole: T. Akiyama, et al.; Anticancer Drugs 10, 67 (1999) Abstract
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent: D. Fabbro, et al.; Pharmacol. Ther. 82, 293 (1999) Abstract
The phosphatidylinositide 3’-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C: A. Tenzer, et al.; Cancer Res. 61, 8203 (2001) Abstract; Full Text
Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C: D.J. Propper, et al.; J. Clin. Oncol. 19, 1485 (2001) Abstract; Full Text
A protein kinase C inhibitor induces phenotypic reversion of ras-transformed pancreatic cancer cells and cooperatively blocks tumor cell proliferation with an anti- ras peptide.: D. Way, et al.; Cancer Chemother. Pharmacol. 49, 429 (2002) Abstract
Protein kinase C inhibitors: H.C. Swannie & S.B. Kaye; Curr. Oncol. Rep. 4, 37 (2002), (Review) Abstract
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder: J. Chen, et al.; PNAS 101, 14479 (2004) Abstract; Full Text
Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3: P. George, et al.; Cancer Res. 64, 3645 (2004) Abstract; Full Text
Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activati