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ALX-350-095 Revised 03-Apr-08
Apicidin
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SYNONYMS cyclo-L-(2-Amino-8-oxodecanoyl)-L-(N-methoxy-tryptophan)-L-isoleucyl-D-pipecolinyl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-095-M001   1 mg 50.00 USD Add To Cart
ALX-350-095-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C34H49N5O6
MW: 623.8
CAS NUMBER: 183506-66-3
SOURCE/HOST: Isolated from Fusarium sp.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC.

Product Description
Potent inhibitor of histone deacetylase (HDAC). Inhibits proliferation. Induces cell cycle arrest. Stimulates apoptosis of cancer cells. Antiprotozoal.
Product Specific Literature References
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase: S.J. Darkin-Rattray, et al.; PNAS 93, 13143 (1996) Abstract
Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin: J.W. Han, et al.; Cancer Res. 60, 6068 (2000) Abstract
Transcriptional activation of p21(WAF1/CIP1) by apicidin, a novel histone deacetylase inhibitor: J.S. Kim, et al.; BBRC 281, 866 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 107 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 113 (2001) Abstract
Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities: S.B. Singh, et al.; J. Org. Chem. 67, 815 (2002) Abstract
Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells: J. Hong, et al.; Cancer Lett. 189, 197 (2003) Abstract
Activation of NF-kappaB by HDAC inhibitor apicidin through Sp1-dependent de novo protein synthesis: its implication for resistance to apoptosis: Y.K. Kim, et al.; Cell Death Differ. 13, 2033 (2006) Abstract
Apicidin, a novel histone deacetylase inhibitor, has profound anti-growth activity in human endometrial and ovarian cancer cells: T. Ueda, et al.; Int. J. Mol. Med. 19, 301 (2007) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products • HDAC Inhibitors • Natural Products for Cell Cycle Research • Natural Products - Other Anti-infective Agents • Parasitic Diseases Other Products • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-385-008 Revised 13-Mar-08
Apigenin
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SYNONYMS 4',5,7-Trihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-008-M010   10 mg 35.00 USD Add To Cart
ALX-385-008-M050   50 mg 105.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 520-36-5
MERCK INDEX: 14: 730
SOURCE/HOST: Synthetic.
PURITY: ≥90% (HPLC)
APPEARANCE: Light yellow to slightly brown powder.
SOLUBILITY: Soluble in diluted potassium hydroxide or DMSO; slightly soluble in 100% ethanol (hot). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: IRRITANT.

Product Description
Antioxidant flavonoid. Has chemopreventive and antitumor properties. Induces apoptosis. Inhibits the proliferation of malignant tumor cells by G2/M arrest. MAP kinase (MAPK/ERK) inhibitor. Inhibits hypoxia-inducible factor-1 (HIF-1) and vascular endothelial growth factor (VEGF) expression.
Product Specific Literature References
Apigenin and tangeretin enhance gap junctional intercellular communication in rat liver epithelial cells: C. Chaumontet, et al.; Carcinogenesis 15, 2325 (1994) Abstract
Apigenin induces morphological differentiation and G2-M arrest in rat neuronal cells: F. Sato, et al.; BBRC 204, 578 (1994) Abstract
Reversion of v-H-ras-transformed NIH 3T3 cells by apigenin through inhibiting mitogen activated protein kinase and its downstream oncogenes: M.L. Kuo and N.C. Yang; BBRC 212, 767 (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
Apigenin inhibits endothelial-cell proliferation in G(2)/M phase whereas it stimulates smooth-muscle cells by inhibiting P21 and P27 expression: V. Trochon, et al.; Int. J. Cancer 85, 691 (2000) Abstract
Induction of caspase-dependent, p53-mediated apoptosis by apigenin in human neuroblastoma: R. Torkin, et al.; Mol. Cancer Ther. 4, 1 (2005) Abstract
Apigenin and cancer chemoprevention: progress, potential and promise: D. Patel, et al.; Int. J. Oncol. 30, 233 (2007), (Review) Abstract
Apigenin inhibits tumor angiogenesis through decreasing HIF-1alpha and VEGF expression: J. Fang, et al.; Carcinogenesis 28, 858 (2007) Abstract
Apigenin-induced cell cycle arrest is mediated by modulation of MAPK, PI3K-Akt, and loss of cyclin D1 associated retinoblastoma dephosphorylation in human prostate cancer cells: S. Shukla & S. Gupta; Cell Cycle 6, 1102 (2007) Abstract
Apigenin blocks lipopolysaccharide-induced lethality in vivo and proinflammatory cytokines expression by inactivating NF-kappaB through the suppression of p65 phosphorylation: C. Nicholas, et al.; J. Immunol. 179, 7121 (2007) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Hypoxia-inducible Factor [HIF] / Related Products • Antitumor Agents (Enzyme Inhibitors) • Natural Products - Protein Kinase Inhibitors • VEGFs & VEGF-Rs Other Products • Natural Products for Angiogenesis Research • Natural Products - Chemopreventive Agents • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Antitumor Agents (Anti-proliferative) • Natural Products - Antioxidants
 
 
ALX-380-207 Revised 03-Apr-08
Apoptolidin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-207-MC01   0.1 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C58H96O21
MW: 1129.4
CAS NUMBER: 194874-06-1
SOURCE/HOST: Isolated from Amicolatopsis sp. MST-AS5912.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Originally isolated from Nocardiopsis sp. Antibiotic. Potent and highly selective apoptosis inducer in several cancer cell lines. F0F1-ATPase inhibitor.
Product Specific Literature References
Apoptolidin, a new apoptosis inducer in transformed cells from Nocardiopsis sp: J.W. Kim, et al.; J. Antibiot. (Tokyo) 50, 6628 (1997) Abstract
Understanding and exploiting the mechanistic basis for selectivity of polyketide inhibitors of F(0)F(1)-ATPase: A.R. Salomon, et al.; PNAS 97, 14766 (2000) Abstract; Full Text
Apoptolidin, a selective cytotoxic agent, is an inhibitor of F0F1-ATPase: A.R. Salomon, et al.; Chem. Biol. 8, 71 (2001) Abstract; Full Text
Apoptolidin: induction of apoptosis by a natural product: P.T. Daniel, et al.; Angew. Chem. Int. Ed. Engl. 45, 872 (2006) Abstract
Correlation of F0F1-ATPase inhibition and antiproliferative activity of apoptolidin analogues: P.A. Wender, et al.; Org. Lett. 8, 589 (2006) Abstract
Further Categories Containing This Product:
Antitumor Antibiotics • Natural Products - ATPase Inhibitors • Antitumor Agents (Apoptosis Inducers) • Respiratory Chain Other Products
 
 
ALX-350-312 Revised 28-May-08
(-)-Arctigenin
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SYNONYMS (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]dihydro-3-[(4-hydroxy-3-methoxyphenyl)methyl]-2-(3H)-furanone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-312-M025   25 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C21H24O6
MW: 372.4
CAS NUMBER: 7770-78-7
SOURCE/HOST: Isolated from Arctium lappa.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (34mg/ml, heating, sonication); sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Lignan derivative, which shows antitumor, anti-inflammatory, immunomodulatory and neuroprotective activities. Down-regulates anti-apoptotic protein Bcl-XL. Potent inhibitor of HIV type-I integrase and DNA topoisomerase II. Shows phytoestrogenic and cytotoxic properties against Hep62 cells.  Antagonist for platelet activating factor and Ca2+. Blocks the activation of Akt (protein kinase B; PKB) induced by glucose starvation.
Product Specific Literature References
Antiproliferative effect of Arctigenin and Arctiin: S.Y. Ryu, et al.; Arch. Pharm. Res. 18, 462 (1995)
(-)-Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase: E. Eich, et al.; J. Med. Chem 39, 86 (1996) Abstract
Immunomodulatory effect of arctigenin, a lignan compound, on tumour necrosis factor-alpha and nitric oxide production, and lymphocyte proliferation: J.Y. Cho, et al.; J. Pharm. Pharmacol. 51, 1267 (1999) Abstract
Arctigenin protects cultured cortical neurons from glutamate-induced neurodegeneration by binding to kainate receptor: Y.P. Jang, et al.; J. Neurosci. Res. 68, 233 (2002) 68, 233 (2002) Abstract
A phytochemical study of lignans in whole plants and cell suspension cultures of Anthriscus sylvestris: A. Koulman, et al.; Planta Med. 69, 733 (2003) Abstract
Naturally occurring lignans efficiently induce apoptosis in colorectal tumor cells: B. Hausott, et al.; J. Cancer Res. Clin. Oncol. 129, 569 (2003) Abstract
Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via potent MKK inhibition: the role in TNF-alpha inhibition: M.K. Cho, et al.; Int. Immunopharmacol. 4, 1419 (2004) Abstract
Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via potent MKK inhibition: the role in TNF-alpha inhibition: M.K. Cho, et al.; Int. Immunopharmacol. 4, 1419 (2004) Abstract
Identification of arctigenin as an antitumor agent having the ability to eliminate the tolerance of cancer cells to nutrient starvation: S. Awale, et al.; Cancer Res. 66, 1751 (2006) Abstract
The chemopreventive effects of Saussurea salicifolia through induction of apoptosis and phase II detoxification enzyme: K. Kang, et al.; Biol. Pharm. Bull. 30, 2352 (2007) Abstract
Further Categories Containing This Product:
Bcl-2 Family Modulators • Platelet Activating Factors [PAF] & Receptors / Related Products • Natural Products - Anti-inflammatory Agents • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Topoisomerase Inhibitors • Natural Products - Immunomodulators • Natural Products - Nitric Oxide Pathway Modulators • HIV / AIDS / Related Products
 
 
ALX-350-318 Revised 17-Jun-08
(-)-Arctiin
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SYNONYMS (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]-3-[[4-(β-D-glucopyranosyloxy)-3-methoxyphenyl]methyl]dihydro-2(3H)-furanone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-318-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C27H34O11
MW: 534.6
CAS NUMBER: 20362-31-6
SOURCE/HOST: Isolated from Arctium lappa.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (5mg/ml); sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Lignan derivative with antitumor activities. Down-regulates anti-apoptotic protein Bcl-XL. Potent inhibitor of HIV type-I integrase and DNA topoisomerase II. Shows phytoestrogenic activity and is an antagonist for platelet activating factor and Ca2+.
Product Specific Literature References
Platelet activating factor (PAF) antagonists contained in medicinal plants: lignans and sesquiterpenes: S. Iwakami, et al.; Chem. Pharm. Bull. (Tokyo) 40, 1196 (1992) Abstract
Antiproliferative effect of Arctigenin and Arctiin: S.Y. Ryu, et al.; Arch. Pharm. Res. 18, 462 (1995)
Cytotoxic components of bardanae fructus (goboshi): S. Moritani, et al.; Biol. Pharm. Bull. 19, 1515 (1996) Abstract
Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection: A.J. Vlietinck, et al.; Planta Med. 64, 97 (1998) Abstract
Anti-tumor-promoting activity of lignans from the aerial part of Saussurea medusa: M. Takasaki, et al.; Cancer Lett. 158, 53 (2000) Abstract
Isolation and identification of arctiin and arctigenin in leaves of burdock (Arctium lappa L.) by polyamide column chromatography in combination with HPLC-ESI/MS: S. Liu, et al.; Phytochem. Anal. 16, 86 (2005) Abstract
Application of preparative high-speed counter-current chromatography for separation and purification of arctiin from Fructus Arctii: X. Wang, et al.; J. Chromatogr. A. 1063, 247 (2005) Abstract
The chemopreventive effects of Saussurea salicifolia through induction of apoptosis and phase II detoxification enzyme: K. Kang, et al.; Biol. Pharm. Bull. 30, 2352 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Immunomodulators • Bcl-2 Family Modulators • Antitumor Agents (Anti-proliferative) • Platelet Activating Factors [PAF] & Receptors / Related Products • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Topoisomerase Inhibitors • HIV / AIDS / Related Products
 
 
ALX-350-375 Revised 22-Jul-08 New product
Arcyriaflavin A
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-375-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H11N3O2
MW: 325.3
CAS NUMBER: 118458-54-1
SOURCE/HOST: Synthetic. Originally isolated from the marine ascidian Eudistoma sp.
PURITY: ≥95% (HPLC)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in DMSO (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light. Packaged under inert gas.

Product Description
Potent inhibitor of CDK4 / cyclin D1 (IC50 = 59nM). Inhibits human cytomegalovirus (HCMV) replication in cell culture (IC50 = 200nM).
Product Specific Literature References
Staurosporine aglycone (K252-c) and arcyriaflavin A from the marine ascidian, Eudistoma sp: P.A. Horton, et al.; Experientia 50, 843 (1994) Abstract
Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication: M.J. Slater, et al.; Bioorg. Med. Chem. 7, 1067 (1999) Abstract
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors: C. Sanchez-Martinez, et al.; Bioorg. Med. Chem. Lett. 13, 3835 (2003) Abstract
Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors: G. Zhu, et al.; Bioorg. Med. Chem. Lett. 13, 1231 (2003) Abstract
Two indolocarbazole alkaloids with apoptosis activity from a marine-derived actinomycete Z(2)039-2: R. Liu, et al.; Arch. Pharm. Res. 30, 270 (2007) Abstract
Further Categories Containing This Product:
Natural Products for Cell Cycle Research • Antiviral Agents Other Products • Marine Natural Products
 
 
ALX-350-129 Revised 04-Dec-07
Aristoforin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Apoptosis Inducers & Inhibitors
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ALX-350-129-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C37H54O6
MW: 594.8
CAS NUMBER: 849215-53-8
PURITY: ≥95%
APPEARANCE: White to yellow oil.
SOLUBILITY: Soluble in DMSO or 100mM sodium hydrogen carbonate/2% DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Stable and water-soluble derivative of hyperforin (Prod. No. ALX-350-097) inducing apoptosis. Antitumor agent. Inhibits sirtuins.
Product Specific Literature References
Aristoforin, a novel stable derivative of hyperforin, is a potent anticancer agent: M. Gartner, et al.; Chembiochem. 6, 171 (2005) Abstract
Phloroglucinol Derivatives Guttiferone G, Aristoforin, and Hyperforin: Inhibitors of Human Sirtuins SIRT1 and SIRT2: C. Gey, et al.; Angew. Chem. Int. Ed. Engl. 46, 5219 (2007) Abstract
Related Products
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Sirtuins / Related Products • Natural Products - Antitumor Reagents
 
 
ALX-270-047 Revised 26-Sep-07
Aristolochic acid
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SYNONYMS 8-Methoxy-6-nitrophenanthrol(3,4-d)-1,3-dioxide-5-carboxylic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-270-047-M025   25 mg 25.00 USD Add To Cart
ALX-270-047-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C17H11NO7
MW: 341.3
CAS NUMBER: 313-67-7
MERCK INDEX: 14: 786
RTECS: CF3325000
SOURCE/HOST: Isolated from Aristolochia clematis.
PURITY: ≥97% (~1:1 mixture of aristolochic acids I (A) and II (B))
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: MAY BE CARCINOGENIC. TOXIC. MAY BE MUTAGENIC.

Product Description
Phospholipase A2 (PLA2) inhibitor active against the enzymes found in many snake venoms as well as those of human platelets and synovial fluids. Inhibits ionophore-stimulated PLA2 activity in human neutrophils. Has been shown to be nephropathic and carcinogenic.
Product Specific Literature References
Characterization of three edema-inducing phospholipase A2 enzymes from habu (Trimeresurus flavoviridis) venom and their interaction with the alkaloid aristolochic acid: B.S. Vishwanath, et al.; Toxicon 25, 501 (1987) Abstract
Interaction of aristolochic acid with Vipera russelli phospholipase A2: its effect on enzymatic and pathological activities: B.S. Vishwanath & T.V. Gowda; Toxicon 25, 929 (1987) Abstract
Interaction of phospholipase A2 from Vipera russelli venom with aristolochic acid: a circular dichroism study: B.S. Vishwanath, et al.; Toxicon 25, 939 (1987) Abstract
Edema-inducing activity of phospholipase A2 purified from human synovial fluid and inhibition by aristolochic acid: B.S. Vishwanath, et al.; Inflammation 12, 549 (1988) Abstract
Effects of aristolochic acid on phospholipase A2 activity and arachidonate metabolism of human neutrophils: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1001, 3 (1989) Abstract
Suramin alters phosphoinositide synthesis and inhibits growth factor receptor binding in HT-29 cells: R. Kopp & A. Pfeiffer; Cancer Res. 50, 6490 (1990) Abstract
The effects of the phospholipase A2 inhibitors aristolochic acid and PGBx on A23187-stimulated mobilization of arachidonate in human neutrophils are overcome by diacylglycerol or phorbol ester: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1126, 319 (1992) Abstract
Evidence for different mechanisms involved in the formation of lyso platelet-activating factor and the calcium-dependent release of arachidonic acid from human neutrophils: J.D. Winkler, et al.; Biochem. Pharmacol. 44, 2055 (1992) Abstract
Selective inhibition of group II phospholipase A2 by quercetin: M. Lindahl & C. Tagesson; Inflammation 17, 573 (1993) Abstract
Detection of DNA adducts formed by aristolochic acid in renal tissue from patients with Chinese herbs nephropathy: H.H. Schmeiser, et al.; Cancer Res. 56, 2025 (1996) Abstract
Aristolochic acid and ’Chinese herbs nephropathy’: a review of the evidence to date: J.P. Cosyns; Drug Saf. 26, 33 (2003), Review Abstract
Effect of aristolochic acid on intracellular calcium concentration and its links with apoptosis in renal tubular cells: Y.H. Hsin, et al.; Apoptosis 11, 2167 (2006) Abstract
Further Categories Containing This Product:
PLA2 Inhibitors • Carcinogens & Tumor Promoters Other Products • Natural Products - Other Tumor Promoters • Other Toxins • Alkaloids
 
 
ALX-350-219 Revised 28-May-08
Artemisinin
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SYNONYMS Qinghaosu
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antimalarial Agents
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ALX-350-219-M100   100 mg 35.00 USD