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Natural Products - Protein Kinase Inhibitors
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ALX-350-292 Revised 26-Mar-05
Kahalalide F - Discontinued Due to Patent Restrictions
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-292-C500   500 µg Inquire
Product Specification
FORMULA: C75H124N14O16
MW: 1477.9
CAS NUMBER: 149204-42-2
SOURCE/HOST: Isolated from marine mollusc Elysia rufescens.
PURITY: ≥95%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Highly selective activity against prostate tumors in vitro. Disrupts lysosomal membranes. Inhibitor of c-erbB-2 (ErbB2).
Product Specific Literature References
The antitumoral compound Kahalalide F acts on cell lysosomes: M. Garcia-Rocha, et al.; Cancer Lett. 99, 43 (1996) Abstract
Synthesis and structure determination of kahalalide F (1,2): Synthesis and structure determination of kahalalide F (1,2); J. Am. Chem. Soc. 123, 11398 (2001) Abstract
Chemical and enzymatic stability of a cyclic depsipeptide, the novel, marine-derived, anti-cancer agent kahalalide F: R.W. Sparidans, et al.; Anticancer Drugs 12, 575 (2001) Abstract
Preclinical toxicity studies of kahalalide F, a new anticancer agent: single and multiple dosing regimens in the rat: A.P. Brown, et al.; Cancer Chemother. Pharmacol. 50, 333 (2002) Abstract
Quantitative analysis of the novel depsipeptide anticancer drug Kahalalide F in human plasma by high-performance liquid chromatography under basic conditions coupled to electrospray ionization tandem mass spectrometry: E. Stokvis, et al.; J. Mass. Spectrom. 37, 992 (2002) Abstract
Further Categories Containing This Product:
Natural Products - Protein Kinase Inhibitors • Tyrosine Kinase Inhibitors • erbB-2 / Related Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-350-007 Revised 07-Apr-08
Lavendustin A
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SYNONYMS 5-Amino-[(N-2,5-dihydroxybenzyl)-N'-2-hydroxybenzyl]salicylic acid
RG14355
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-007-M001   1 mg 75.00 USD Add To Cart
ALX-350-007-M005   5 mg 295.00 USD Add To Cart
Product Specification
FORMULA: C21H19NO6
MW: 381.4
CAS NUMBER: 125697-92-9
SOURCE/HOST: Synthetic.
PURITY: ≥97% (TLC)
APPEARANCE: Off-white to brown solid.
SOLUBILITY: Soluble in DMSO, methanol or dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and moisture. Hygroscopic.

Product Description
Cell permeable tyrosine kinase inhibitor with little effect on cAMP-dependent protein kinase (PKA) or protein kinase C (PKC). Inhibits autophosphorylation of EGFRs. Also inhibits NMDA-stimulated cGMP production.
Product Specific Literature References
Cellular oncogenes and retroviruses: J.M. Bishop; Annu. Rev. Biochem. 52, 301 (1983) Abstract
Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus: T. Onoda, et al.; J. Nat. Prod. 52, 1252 (1989) Abstract
Kinetic analysis of the inhibition of the epidermal growth factor receptor tyrosine kinase by Lavendustin-A and its analogue: C.-Y.J. Hsu, et al.; J. Biol. Chem. 266, 21105 (1991) Abstract
Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors: T.J. O'Dell, et al.; Nature 353, 558 (1991) Abstract
Blockade of nitric oxide synthesis by tyrosine kinase inhibitors in neurones: J. Rodriguez, et al.; Neuropharmacology 33, 1267 (1994) Abstract
Solid Phase Synthesis of Lavendustin A and Analogs: J. Green; J. Org. Chem. 60, 4287 (1995)
Suppression of VEGF-induced angiogenesis by the protein tyrosine kinase inhibitor, lavendustin A: D.E. Hu and T.-P.D. Fan; Br. J. Pharmacol. 114, 262 (1995) Abstract
Inhibition of atrial wall stretch-induced cardiac hormone secretion by lavendustin A, a potent tyrosine kinase inhibitor: P. Taskinen, et al.; Endocrinology 140, 4198 (1999) Abstract
Influence of the tyrosine kinase inhibitors STI571 (Glivec(R)), lavendustin A and genistein on human mast cell line (HMC-1(560)) activation: K. Lober, et al.; J. Cell Biochem. 103, 1076 (2007) Abstract
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Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors • Natural Products for Angiogenesis Research • Natural Products - Nitric Oxide Pathway Modulators
 
 
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-350-037 Revised 04-Feb-05
Lavendustin B
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-037-M001   1 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C21H19NO5
MW: 365.4
CAS NUMBER: 125697-91-8
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in methanol, DMSO and dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Control for lavendustin A (Prod. No. ALX-350-007); 100-fold less potent than lavendustin A.
Product Specific Literature References
Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus: T. Onoda, et al.; J. Nat. Prod. 52, 1252 (1989) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-270-066 Revised 07-Apr-08
Lavendustin C
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SYNONYMS Compound 5
5-(N-2,5-Dihydroxybenzyl)aminosalicylic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-270-066-M001   1 mg 35.00 USD Add To Cart
Product Specification
FORMULA: C14H13NO5
MW: 275.3
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Potent inhibitor of protein tyrosine kinases and Ca2+/calmodulin-dependent kinase II. Acts also as an inhibitor of EGFR tyrosine kinase and pp60c-src kinase.
Product Specific Literature References
Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus: T. Onoda, et al.; J. Nat. Prod. 52, 1252 (1989) Abstract
Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors: T.J. O'Dell, et al.; Nature 353, 558 (1991) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Inhibition of crystal-induced neutrophil activation by a protein tyrosine kinase inhibitor: H.M. Burt, et al.; J. Leukoc. Biol. 55, 112 (1994) Abstract
Endotoxin increases intercellular resistance in microvascular endothelial cells by a tyrosine kinase pathway: D. Lidington, et al.; J. Cell Physiol. 185, 117 (2000) Abstract
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Further Categories Containing This Product:
CAM Kinase Inhibitors • EGFR Kinase Inhibitors • Lipopolysaccharides [LPS] / Related Products • Tyrosine Kinase Inhibitors
 
 
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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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-162-006 Revised 07-Apr-08
Melittin (natural)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-162-006-M001   1 mg 40.00 USD Add To Cart
ALX-162-006-M005   5 mg 160.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Ile-Gly-Ala-Val-Leu-Lys-Val-Leu-Thr-Thr-Gly-Leu-Pro-Ala-Leu-Ile-Ser-Trp-Ile-Lys-Arg-Lys-Arg-Gln-Gln-NH2
FORMULA: C131H229N39O31
MW: 2846.5
CAS NUMBER: 37231-28-0
MERCK INDEX: 14: 5824
RTECS: OS3960000
SOURCE/HOST: Isolated from bee venom.
PURITY: ≥85% (HPLC)
APPEARANCE: Off-white to faint tan powder.
PURITY DETAIL: Phospholipase A2 impurity: <5 units per mg solid.
SOLUBILITY: Soluble in PBS (5mg/ml) or water (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Very hygroscopic. Protect from light.
HAZARD: HARMFUL.
Product Description
Causes disruption of normal cellular activity and cell lysis. Binds calmodulin in a calcium-dependent manner. Activates phospholipase A2 (PLA2) and inhibits protein kinase C (PKC) by binding to the catalytic domain in a Mg-ATP sensitive manner. Antirheumatic.
Product Specific Literature References
Rapid purification of calmodulin and S-100 protein by affinity chromatography with melittin immobilized to sepharose: R.L. Kincaid & C.C. Coulson; BBRC 133, 256 (1985) Abstract
Comparison of S100b protein with calmodulin: interactions with melittin and microtubule-associated tau proteins and inhibition of phosphorylation of tau proteins by protein kinase C: J. Baudier, et al.; Biochemistry 26, 2886 (1987) Abstract
Possible mechanisms of action of cobra snake venom cardiotoxins and bee venom melittin: J.E. Fletcher & M.S. Jiang; Toxicon. 31, 669 (1993) Abstract
Melittin and phospholipase A2 from bee (Apis mellifera) venom cause necrosis of murine skeletal muscle in vivo: C.L. Ownby, et al.; Toxicon. 35, 67 (1997) Abstract
Melittin binds to secretory phospholipase A2 and inhibits its enzymatic activity: S.S. Saini, et al.; BBRC 238, 436 (1997) Abstract
Phospholipase A2-independent Ca2+ entry and subsequent apoptosis induced by melittin in human MG63 osteosarcoma cells: S.T. Chu, et al.; Life Sci. 80, 364 (2007) Abstract
Further Categories Containing This Product:
Calmodulin Other Products • PKC Inhibitors • Peptides • PLA2 Activators
 
 
ALX-162-007 Revised 12-May-05
Melittin (synthetic)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-162-007-MC05   0.5 mg 70.00 USD Add To Cart
ALX-162-007-M001   1 mg 120.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Ile-Gly-Ala-Val-Leu-Lys-Val-Leu-Thr-Thr-Gly-Leu-Pro-Ala-Leu-Ile-Ser-Trp-Ile-Lys-Arg-Lys-Arg-Gln-Gln-NH2
FORMULA: C131H229N39O31
MW: 2846.5
CAS NUMBER: 37231-28-0
MERCK INDEX: 14: 5824
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.
Product Description
For technical information see melittin (natural) (Prod. No. ALX-162-006).
Further Categories Containing This Product:
PLA2 Activators • Calmodulin Other Products • PKC Inhibitors • Peptides
 
 
ALX-350-308 Revised 03-Apr-08
3-O-Acetyl-β-boswellic acid
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SYNONYMS AβBA
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-308-M001   1 mg 45.00 USD Add To Cart
ALX-350-308-M005   5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C32H50O4
MW: 498.8
CAS NUMBER: 5968-70-7
SOURCE/HOST: Isolated from Boswellia sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetone, dimethyl formamide, DMSO, dichloromethane, 100% ethanol or methanol; sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Shows antitumor and anti-inflammatory activities. Potent non-redox, non-competitive 5-lipoxygenase and topoisomerase I and IIa inhibitor leading to apoptosis. 10-100 times more potent than natural boswellic acid.
Product Specific Literature References
Effect of food intake on the bioavailability of boswellic acids from a herbal preparation in healthy volunteers: V. Sterk, et al.; Planta Med. 70, 1155 (2004) Abstract
Effects of Boswellia serrata in mouse models of chemically induced colitis: P.R. Kiela, et al.; Am. J. Physiol. Gastrointest. Liver. Physiol. 288, G798 (2005) Abstract
Inhibition of IkappaB kinase activity by acetyl-boswellic acids promotes apoptosis in androgen-independent PC-3 prostate cancer cells in vitro and in vivo: T. Syrovets, et al.; J. Biol. Chem. 280, 6170 (2005) Abstract; Full Text
Induction of central signalling pathways and select functional effects in human platelets by beta-boswellic acid: D. Poeckel, et al.; Br. J. Pharmacol. 146, 514 (2005) Abstract
Boswellic acids: biological actions and molecular targets: D. Poeckel & O. Werz; Curr. Med. Chem. 13, 3359 (2006), Review Abstract
Further Categories Containing This Product:
Natural Products - NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Protein Kinase Inhibitors • Lipoxygenases / Related Products • NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products - Topoisomerase Inhibitors • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-258 Revised 08-Apr-08
Parthenolide
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SYNONYMS (1aR-[1aR*,4E,7aS*,-10aS*,-10bR*])-2,3-6,7,7a,8,10a,10b-Octahydro-1a,5-dimethyl-8-methyleneoxireno[9,10]cyclo deca[1,2-b]furan-9(1aH)-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-258-M005   5 mg 15.00 USD