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ALX-270-440 Revised 20-Nov-08 New product
AMI-1
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SYNONYMS Arginine N-Methyltransferase Inhibitor-1
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY PRMTs, Mono- & Dimethylarginine / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-440-M005   5 mg 90.00 USD Add To Cart
ALX-270-440-M025   25 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C21H12N2O9S2Na4
MW: 592.4
PURITY: ≥98% (1H-NMR and HPLC)
APPEARANCE: Brown solid.
SOLUBILITY: Soluble in water, 100% ethanol or DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light. Hygroscopic.

Product Description
Potent, cell permeable and specific inhibitor of protein arginine N-methyltransferases (PRMTs) (IC50=8.8µM for human PRMT1 and 3.0µM for yeast Hmt1p). Does not compete for the AdoMet (S-adenosyl-L-methionine; SAM) binding site. Exhibits only minimal effects on lysine N-methyltransferases. Suppresses the transcriptional coactivator activity of PRMT1 and PRMT4. Inhibitor of HIV-1 RT polymerase (IC50=5.0µM).
Product Specific Literature References
A novel mechanism for inhibition of HIV-1 reverse transcriptase: A.G. Skillman, et al.; Bioorg. Chem. 30, 443 (2002) Abstract
Small molecule regulators of protein arginine methyltransferases: D. Cheng, et al.; J. Biol. Chem. 279, 23892 (2004) Abstract; Full Text
Further Categories Containing This Product:
HIV / AIDS / Related Products
 
 
ALX-270-478 Revised 30-Jul-08
SB 225002
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SYNONYMS N-(2-Bromophenyl)-N’-(2-hydroxy-4-nitrophenyl)urea
PRODUCT LINE Chemokines & Cytokines
PRODUCT CATEGORY CXC Chemokines & Receptors / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-478-M001   1 mg 30.00 USD Add To Cart
ALX-270-478-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C13H10BrN3O4
MW: 352.1
CAS NUMBER: 182498-32-4
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (40mg/ml), 100% ethanol or methanol (15mg/ml); slightly soluble in acetonitrile (2mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by MS, 1H-NMR and 13C-NMR.

Product Description
Potent and selective antagonist of CXCR2 chemokine receptor (IC50=22nM). >150-fold more selective over CXCR1 receptor. Inhibits IL-8- (IC50=8nM) and GROα-mediated (IC50=10nM) calcium mobilisation. Prevents IL-8-induced neutrophil migration. Inhibits HIV replication in lymphocytes and macrophages.
Product Specific Literature References
Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration: J.R. White, et al.; J. Biol. Chem. 273, 10095 (1998) Abstract; Full Text
Characterization of the molecular interactions of interleukin-8 (CXCL8), growth related oncogen alpha (CXCL1) and a non-peptide antagonist (SB 225002) with the human CXCR2: J. Catusse, et al.; Biochem. Pharmacol. 65, 813 (2003) Abstract
A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer: B. Wang, et al.; Cancer Res. 66, 3071 (2006) Abstract; Full Text
Further Categories Containing This Product:
HIV / AIDS / Related Products
 
 
ALX-350-019 Revised 16-Oct-08
(+)-Brefeldin A
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SYNONYMS BFA
Ascotoxin
Decumbin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-019-M005   5 mg 80.00 USD Add To Cart
ALX-350-019-M010   10 mg 130.00 USD Add To Cart
ALX-350-019-M025   25 mg 270.00 USD Add To Cart
ALX-350-019-M050   50 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C16H24O4
MW: 280.4
CAS NUMBER: 20350-15-6
MERCK INDEX: 14: 1369
SOURCE/HOST: Isolated from Eupenicillium brefeldianum.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, methanol, acetone or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Inhibitor of intracellular protein transport and protein secretion, interfering with trafficking in the trans-Golgi network, leading to the accumulation of cycling proteins in ERGIC clusters. Blocks ADP-ribosylation factor (Arf) in an inactive GDP-bound conformation and thereby prevents binding of COPI coats to ERGIC and Golgi membranes. Upon brefeldin A treatment the Golgi rapidly tubulates and fuses with the ER by an energy-, temperature-, and microtubule-dependent process. In contrast, the drug has little effect on the ERGIC, which keeps its identity, although the ERGIC clusters become larger and more uniformly distributed in the cytoplasm of the cells. Inhibits intracellular collagen degradation. Also inhibits apical Na+ channels in epithelia. Induces apoptosis.
Product Specific Literature References
Decumbin, a new compound from a species of Penicillium: V.L. Singleton, et al.; Nature 181, 1072 (1958)
Über die Isolierung neuer Stoffwechselprodukte aus Penicillium brefeldianum Dodge.: E. Harri, et al.; Helv. Chim. Acta 46, 1235 (1963)
Novel blockade by brefeldin A of intracellular transport of secretory proteins in cultured rat hepatocytes: Y. Misumi, et al.; J. Biol. Chem. 261, 11398 (1986) Abstract; Full Text
Brefeldin A causes disassembly of the Golgi complex and accumulation of secretory proteins in the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 263, 18545 (1988) Abstract; Full Text
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Brefeldin A and the endocytic pathway. Possible implications for membrane traffic and sorting: W. Hunziker, et al.; FEBS Lett. 307, 93 (1992), (Review) Abstract
Brefeldin A inhibits degradation as well as production and secretion of collagen in human lung fibroblasts: C.R. Ripley, et al.; J. Biol. Chem. 268, 3677 (1993) Abstract
Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53: R.G. Shao, et al.; Exp. Cell Res. 227, 190 (1996) Abstract
Brefeldin A inhibition of apical Na+ channels in epithelia: R.S. Fisher, et al.; Am. J. Physiol. 270, C138 (1996) Abstract
Brefeldin A: deciphering an enigmatic inhibitor of secretion: A. Nebenfuhr, et al.; Plant Physiol. 130, 1102 (2002), Review Abstract
NKT cells provide help for dendritic cell-dependent priming of MHC class I-restricted CD8+ T cells in vivo: D. Stober, et al.; J. Immunol. 170, 2540 (2003) Abstract; Full Text
Interaction of BIG2, a brefeldin A-inhibited guanine nucleotide-exchange protein, with exocyst protein Exo70: K.F. Xu, et al.; PNAS 102, 2784 (2005) Abstract
Further Categories Containing This Product:
ADP Ribosylation Factor [ARF] / Related Products • Golgi Apparatus • Collagen / Related Products • Na+ Channels • Antitumor Antibiotics • Antibiotics - Antiviral / Anti-HIV • Antibiotics - Antifungal • Autophagy Other Products • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-027 Revised 19-Aug-08
Calphostin C
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SYNONYMS UCN-1028C
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-027-C100   100 µg 85.00 USD Add To Cart
ALX-350-027-M001   1 mg 595.00 USD Add To Cart
Product Specification
FORMULA: C44H38O14
MW: 790.8
CAS NUMBER: 121263-19-2
SOURCE/HOST: Isolated from Cladosporium cladosporioides MST-FP1798.
PURITY: ≥95% (HPLC)
APPEARANCE: Dark red solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for 3 months when stored at -20°C.
HANDLING: Protect from light.

Product Description
Potent and selective inhibitor of the protein kinase C (PKC) regulatory site of diacylglycerol and phorbol esters. At higher concentrations inhibits myosin light chain kinase, cAMP-dependent protein kinase, protein kinase G and pp60v-src protein tyrosine kinase. Induces apoptotic DNA fragmentation and cell death. Kills breast cancer cells. Has antiviral potential. Inhibits cardiac L-type Ca2+ channels.
Product Specific Literature References
Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C: E. Kobayashi, et al.; BBRC 159, 548 (1989) Abstract
Potent and specific inhibitors of protein kinase C of microbial origin: T. Tamaoki and H. Nakano; Biotechnology 8, 732 (1990) Abstract
Inhibition of protein kinase C by calphostin C is light-dependent: R.F. Bruns, et al.; BBRC 176, 288 (1991) Abstract
Irreversible oxidative inactivation of protein kinase C by photosensitive inhibitor calphostin C: R. Gopalakrishna, et al.; FEBS Lett. 314, 149 (1992) Abstract
Calphostin C, a specific protein kinase C inhibitor, activates human neutrophils: effect on phospholipase A2 and aggregation: S. Svetlov and S. Nigam; Biochim. Biophys. Acta 1177, 75 (1993) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Growth inhibition of herpes simplex virus-type 1 in calphostin C-treated astrocytes: C.G. Castagnino, et al.; Intervirology 38, 332 (1995) Abstract
Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels: H.C. Hartzell & A. Rinderknecht; Am. J. Physiol. 270, C1293 (1996) Abstract
Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity: C.L. Chen, et al.; Pharm. Res. 16, 1003 (1999) Abstract
Potent killing of paclitaxel- and doxorubicin-resistant breast cancer cells by calphostin C accompanied by cytoplasmic vacuolization: B. Guo, et al.; Breast Cancer Res. Treat. 82, 125 (2003) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • PKA Inhibitors • PKC Inhibitors • PKG Inhibitors • Myosin Light Chain Kinase Inhibitors • Ca2+ Channels (L-type) • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents
 
 
ALX-350-030 Revised 20-Oct-08
Hypericin (native)
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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-350-030-M001   1 mg 50.00 USD Add To Cart
ALX-350-030-M005   5 mg 200.00 USD Add To Cart
ALX-350-030-M010   10 mg 370.00 USD Add To Cart
Product Specification
FORMULA: C30H16O8
MW: 504.4
CAS NUMBER: 548-04-9
MERCK INDEX: 14: 4863
SOURCE/HOST: Isolated from Hypericum perforatum.
PURITY: ≥98% (HPLC)
APPEARANCE: Black to black-red powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetone, ethylmethylketone, pyridine or other organic solvents and bases.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and oxygen.
HAZARD: MAY BE TERATOGENIC. HARMFUL. MAY BE MUTAGENIC.

Product Description
Inhibitor of protein kinase C (PKC). Shows anti-viral and anti-retroviral activity. Displays antineoplastic and antitumor activities. Inhibits casein kinase II (CKII) and MAP kinase. Bright red fluorescence emission and photostability. Antidepressant.
Product Specific Literature References
Therapeutic agents with dramatic antiretroviral activity and little toxicity at effective doses: aromatic polycyclic diones hypericin and pseudohypericin: D. Meruelo, et al.; PNAS 85, 5230 (1988) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Evaluation of the antiviral activity of anthraquinones, anthrones and anthraquinone derivatives against human cytomegalovirus: D.L. Barnard, et al.; Antiviral Res. 17, 63 (1992) Abstract
Photosensitized inhibition of growth factor-regulated protein kinases by hypericin: P. Agostinis, et al.; Biochem. Pharmacol. 49, 1615 (1995) Abstract
Growth inhibition and apoptosis in human neuroblastoma SK-N-SH cells induced by hypericin, a potent inhibitor of protein kinase C: W. Zhang, et al.; Cancer Lett. 96, 31 (1995) Abstract
Hypericin-induced photosensitization of HeLa cells leads to apoptosis or necrosis. Involvement of cytochrome c and procaspase-3 activation in the mechanism of apoptosis: A. Vantieghem, et al.; FEBS Lett. 440, 19 (1998) Abstract
The activation of the c-Jun N-terminal kinase and p38 mitogen-activated protein kinase signaling pathways protects HeLa cells from apoptosis following photodynamic therapy with hypericin: Z. Assefa, et al.; J. Biol. Chem. 274, 8788 (1999) Abstract; Full Text
Over-expression of Bcl-2 does not protect cells from hypericin photo- induced mitochondrial membrane depolarization, but delays subsequent events in the apoptotic pathway: R. Chaloupka, et al.; FEBS Lett. 462, 295 (1999) Abstract
Hypericin induces both differentiation and apoptosis in human promyelocytic leukemia HL-60 cells: K.T. Lee, et al.; Biol. Pharm. Bull. 22, 1271 (1999) Abstract
Apoptotic and anti-apoptotic signaling pathways induced by photodynamic therapy with hypericin: P. Agostinis, et al.; Adv. Enzyme Regul. 40, 157 (2000) Abstract
Hypericin--a new antiviral and antitumor photosensitizer: mechanism of action and interaction with biological macromolecules: P. Miskovsky; Curr. Drug Targets 3, 55 (2002), (Review) Abstract
Hypericin--the facts about a controversial agent: A. Kubin, et al.; Curr. Pharm. Des. 11, 233 (2005), (Review) Abstract
Cellular mechanisms and prospective applications of hypericin in photodynamic therapy: T. Kiesslich, et al.; Curr. Med. Chem. 13, 2189 (2006), (Review) Abstract
Further Categories Containing This Product:
Casein Kinase Inhibitors • MAPK Pathway Inhibitors • PKC Inhibitors • Neuroactive Agents Other Products • Natural Products for Neurological Research • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Antitumor Reagents
 
 
ALX-350-113 Revised 28-May-08
Gossypol
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SYNONYMS 2,2’-bis[8-Formyl-1,6,7-trihydroxy-5-isopropyl-3-
methylnaphthalene]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
Ordering Information
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ALX-350-113-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C30H30O8
MW: 518.6
CAS NUMBER: 303-45-7
MERCK INDEX: 14: 4528
RTECS: DU3100000
SOURCE/HOST: Isolated from Gossypium genus, Malvaceae.
PURITY: ≥90%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in acetone or DMSO; sparingly soluble in 100% ethanol (2mg/ml) or methanol (2mg/ml). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Mixture of ~65% (+)- and ~35% (-)-enantiomers. Male antifertility agent. Shows antitumor, antiviral and antioxidant actions. Small molecule inhibitor of Bcl-2/Bcl-XL. Induces apoptosis. Synergizes with radiation and chemotherapy in vitro. Reversible inhibitor of protein phosphatase 2B (PP2B; calcineurin). Protein kinase C (PKC) inhibitor.
Product Specific Literature References
Binding of gossypol to purified tubulin and inhibition of its assembly into microtubules: F.J. Medrano and J.M. Andreu; Eur. J. Biochem. 158, 63 (1986) Abstract
Differential inhibition of protein kinase C subtypes: J.M. Pelosin, et al.; BBRC 169, 1040 (1990) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Gossypol arrests human benign prostatic hyperplastic cell growth at G0/G1 phase of the cell cycle: F. Shidaifat, et al.; Anticancer Res. 17, 1003 (1997) Abstract
Inhibition of huntingtin fibrillogenesis by specific antibodies and small molecules: implications for Huntington’s disease therapy: V. Heiser, et al.; PNAS 97, 6739 (2000) Abstract; Full Text
Cytotoxic effect of gossypol on colon carcinoma cells: X. Wang, et al.; Life Sci. 67, 2663 (2000) Abstract
Reversible inhibition of calcineurin by the polyphenolic aldehyde gossypol: R. Baumgrass, et al.; J. Biol. Chem. 276, 47914 (2001) Abstract; Full Text
Toxicity of (+)- and (-)-gossypol to the plant pathogen, Rhizoctonia solani: L.S. Puckhaber, et al.; J. Agric. Food Chem. 50, 7017 (2002) Abstract
Telomerase inhibitors in anticancer therapy: gossypol as a potential telomerase inhibitor: M. Mego; Bratisl. Lek. Listy 103, 378 (2002) Abstract
An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines: M. Le Blanc, et al.; Pharmacol. Res. 46, 551 (2002) Abstract
Gossypol induces chloride secretion in rat proximal colon: G. Kuhn, et al.; Eur. J. Pharmacol. 457, 187 (2002) Abstract
Determination of the absolute configuration and solution conformation of gossypol by vibrational circular dichroism: T.B. Freedman, et al.; Chirality 15, 196 (2003) Abstract
In vitro effects of the BH3 mimetic, (-)-gossypol, on head and neck squamous cell carcinoma cells: C.L. Oliver, et al.; Clin. Cancer Res. 10, 7757 (2004) Abstract; Full Text
The inhibitory effects of gossypol on human prostate cancer cells-PC3 are associated with transforming growth factor beta1 (TGFbeta1) signal transduction pathway: J. Jiang, et al.; Anticancer Res. 24, 19 (2004) Abstract
(-)-Gossypol enhances response to radiation therapy and results in tumor regression of human prostate cancer: L. Xu, et al.; Mol. Cancer Ther. 4, 197 (2005) Abstract; Full Text
Investigations on gossypol: past and present developments: K. Dodou; Expert Opin. Investig. Drugs 14, 1419 (2005) Abstract
An in vitro study of cytotoxic effects of gossypol on human epidermoid larynx carcinoma cell line (HEp-2): E. Konac, et al.; Exp. Oncol. 27, 81 (2005) Abstract; Full Text
Further Categories Containing This Product:
Bcl-2 Family Modulators • Natural Products - Protein Kinase Inhibitors • PKC Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • PP2B [Calcineurin] / Related Products • Natural Products - Antioxidants • Polyphenols Other Products • Natural Products - Antiviral / anti-HIV Agents • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-138 Revised 05-Dec-06
Hexaprenylhydroquinone
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SYNONYMS HPH
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antiviral / anti-HIV Agents
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ALX-350-138-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C36H54O2
MW: 518.8
CAS NUMBER: 119980-00-6
SOURCE/HOST: Isolated from Sarcotragus sp.
PURITY: ≥97% (HPLC)
APPEARANCE: Off-white to brown solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Identity determined by MS, 1H-NMR.

Product Description
Potent inhibitor of HIV reverse transcriptase and cellular DNA polymerase. Inhibitor of CDC25A. Similar compounds have shown inhibitory effects on phospholipase A2.
Product Specific Literature References
Three new heptaprenylhydroquinone derivatives from the sponge Ircinia fasciculata: Y. Venkateswarlu and M. Venkata Rami Reddy; J. Nat. Prod. 57, 1286 (1994)
Biological effects of prenylated hydroquinones: structure-activity relationship studies in antimicrobial, brine shrimp, and fish lethality assays: S. De Rosa, et al.; J. Nat. Prod. 57, 1711 (1994) Abstract
Mode of inhibition of HIV reverse transcriptase by 2-hexaprenylhydroquinone, a novel general inhibitor of RNA-and DNA-directed DNA polymerases: S. Loya, et al.; Biochem. J. 324, 721 (1997) Abstract; Full Text
Polyprenyl-hydroquinones and -furans from three marine sponges inhibit the cell cycle regulating phosphatase CDC25A: I. Erdogan-Orhan, et al.; Nat. Prod. Res. 18, 1 (2004) Abstract
General Literature References
Effects of marine 2-polyprenyl-1,4-hydroquinones on phospholipase A2 activity and some inflammatory responses: B. Gil, et al.; Eur. J. Pharmacol. 285, 281 (1995) Abstract
Further Categories Containing This Product:
PLA2 Inhibitors • Natural Products - DNA Replication Inhibitors • Marine Natural Products • HIV / AIDS / Related Products
 
 
ALX-350-145 Revised 28-Mar-07
Isobavachalcone
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SYNONYMS 2’,4’,4-Trihydroxy-3’-[3’’-methylbut-3’’-enyl]chalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-145-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C20H20O4
MW: 324.4
CAS NUMBER: 20784-50-3
SOURCE/HOST: Isolated from plant Psoralea corylifolia.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.