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ALX-350-239 Revised 22-Apr-08
Gliotoxin
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SYNONYMS [3R-(3α, 5aβ,6β,10aα)]-2,3,5a,6-Tetrahydro-6-hydroxy-3-(hydroxymethyl)-2-methyl-10H-3,10a-epi-dithiopyrazino[1,2-a]indole-1,4-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-350-239-M001   1 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C13H14N2O4S2
MW: 326.4
CAS NUMBER: 67-99-2
MERCK INDEX: 14: 4441
RTECS: KB4725000
SOURCE/HOST: Isolated from Gladiocladium fimbriatum.
PURITY: ≥98% (HPLC)
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in DMSO or methanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HAZARD: TOXIC.

Product Description
Immunomodulating mycotoxin which acts by blocking membrane thiol groups. Causes apoptotic cell death in macrophages and thymocytes. Induces Ca2+ release from intact rat liver mitochondria. Inhibits the activation of transcription factor NF-κB. Antioxidant.
Product Specific Literature References
Identification of an agent in cultures of Aspergillus fumigatus displaying anti-phagocytic and immunomodulating activity in vitro: A. Müllbacher, et al.; J. Gen. Microbiol. 131, 1251 (1985) Abstract
R.J. Jones & J.G. Hancock; J. Gen. Microbiol. 134, 2067 (1988)
Gliotoxin stimulates Ca2+ release from intact rat liver mitochondria: M. Schweizer & C. Richter; Biochemistry 33, 13401 (1994) Abstract
Extracellular calcium is not required for gliotoxin or dexamethasone- induced DNA fragmentation: a reappraisal of the use of EGTA: P. Waring & A. Sjaarda; Int. J. Immunopharmacol. 17, 403 (1995) Abstract
Gliotoxin and related epipolythiodioxopiperazines: P. Waring & J. Beaver; Gen. Pharmacol. 27, 1311 (1996), Review Abstract
The immunosuppressive fungal metabolite gliotoxin specifically inhibits transcription factor NF-kappaB: H.L. Pahl, et al.; J.Exp. Med. 183, 1829 (1996) Abstract
Aspergillus fumigatus suppresses the human cellular immune response via gliotoxin-mediated apoptosis of monocytes: M. Stanzani, et al.; Blood 105, 2258 (2005) Abstract
Discovery of gliotoxin as a new small molecule targeting thioredoxin redox system: H.S. Choi, et al.; BBRC 359, 523 (2007) Abstract
 
 
ALX-350-240 Revised 05-Dec-07
Ilimaquinone
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SYNONYMS 3-[(Decahydro-1β,2β,4αβ-trimethyl-5-methylene-1-naphthyl)methyl]-2-hydroxy-5-methoxybenzoquinone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-240-C100   100 µg 140.00 USD Add To Cart
Product Specification
FORMULA: C22H30O4
MW: 358.5
CAS NUMBER: 71678-03-0
PURITY: ≥98%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Displays antimicrobial, anti-HIV and anti-inflammatory properties. Induces reversible breakdown of Golgi membranes. Inhibits the association of β-COP and ADP-ribosylation factor to Golgi membranes. Interacts with methylation enzymes. Shows anticancer activity.
Product Specific Literature References
R.T. Luibrand, et al.; Tetrahedron 35, 609 (1979)
Complete vesiculation of Golgi membranes and inhibition of protein transport by a novel sea sponge metabolite, ilimaquinone: P.A. Takizawa, et al.; Cell 73, 1079 (1993) Abstract
Interactions of (-)-ilimaquinone with methylation enzymes: implications for vesicular-mediated secretion: H.S. Radeke, et al.; Chem. Biol. 6, 639 (1999) Abstract
Ilimaquinone inhibits gap-junctional communication prior to Golgi fragmentation and block in protein transport: V. Cruciani, et al.; Exp. Cell Res. 287, 130 (2003) Abstract
Natural products with anti-HIV activity from marine organisms: L.A. Tziveleka, et al.; Curr. Top. Med. Chem. 3, 1512 (2003), Review Abstract
Interaction of the smooth endoplasmic reticulum and mitochondria: J.G. Goetz & I.R. Nabi; Biochem. Soc. Trans. 34, 370 (2006), Review Abstract
Ilimaquinone, a marine sponge metabolite, displays anticancer activity via GADD153-mediated pathway: P.H. Lu, et al.; Eur. J. Pharmacol. 556, 45 (2007) Abstract
 
 
ALX-350-241 Revised 07-Dec-07
Manumycin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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ALX-350-241-M001   1 mg 58.00 USD Add To Cart
ALX-350-241-M005   5 mg 170.00 USD Add To Cart
ALX-350-241-M010   10 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C31H38N2O7
MW: 550.7
CAS NUMBER: 52665-74-4
SOURCE/HOST: Isolated from Streptomyces parvulus.
PURITY: ≥96% (HPLC)
APPEARANCE: Yellow to brown powder.
SOLUBILITY: Soluble in methanol or DMSO; insoluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR.

Product Description
Potent, selective and competitive inhibitor of Ras farnesyltransferase. Does not affect geranylgeranyltransferase. Inhibition is competitive with respect to farnesyl pyrophosphate and non-competitive with respect to Ras. Inhibits neutral sphingomyelinase.
Product Specific Literature References
Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review) Abstract
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic: J.B. Gibbs, et al.; Cell 77, 175 (1994) Abstract
Manumycin inhibits ras signal transduction pathway and induces apoptosis in COLO320-DM human colon tumour cells: A. Di Paolo, et al.; Br. J. Cancer 82, 905 (2000) Abstract
Manumycin A and its analogues are irreversible inhibitors of neutral sphingomyelinase: C. Arenz, et al.; ChemBioChem 2, 141 (2001) Abstract
Enhancement of manumycin A-induced apoptosis by methoxyamine in myeloid leukemia cells: M. She, et al.; Leukemia 19, 595 (2005) Abstract
Binding of manumycin A inhibits IkappaB kinase beta activity: M. Bernier, et al.; J. Biol. Chem. 281, 2551 (2006) Abstract
 
 
ALX-350-245 Revised 07-Apr-08
Lactacystin (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome/Ubiquitin Modulators
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ALX-350-245-MC01   0.1 mg 60.00 USD Add To Cart
ALX-350-245-MC05   0.5 mg 250.00 USD Add To Cart
ALX-350-245-M001   1 mg 445.00 USD Add To Cart
Product Specification
FORMULA: C15H24N2O7S
MW: 376.4
CAS NUMBER: 133343-34-7
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetonitrile (20mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or water (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING: Protect from light.

Product Description

Cell permeable and irreversible proteasome inhibitor. Specifically inhibits 26S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation by inhibiting IκB degradation. Inhibits the ubiquitin proteasome pathway in cell culture (IC50=10µM). Inhibits cathepsin A. Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.

Product Specific Literature References
Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells: S. Omura, et al.; J. Antibiot. 44, 116 (1991) Abstract
A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line: G. Fenteany, et al.; PNAS 91, 3358 (1994) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis in human monoblast U937 cells: S. Imajo-Ohmi, et al.; BBRC 217, 1070 (1995) Abstract
The neuritogenesis inducer lactacystin arrests cell cycle at both G0/G1 and G2 phases in neuro 2a cells: M. Katagiri, et al.; J. Antibiotics (Tokyo) 48, 344 (1995) Abstract
Degradation process of ligand-stimulated platelet-derived growth factor beta-receptor involves ubiquitin-proteasome proteolytic pathway: S. Mori, et al.; J. Biol. Chem. 270, 29447 (1995) Abstract; Full Text
Structure-activity relationships of lactacystin, the first non-protein neurotrophic factor: T. Nagamitsu, et al.; J. Antibiotics (Tokyo) 48, 747 (1995) Abstract
Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid: H. Tanaka, et al.; BBRC 216, 291 (1995) Abstract
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Proteasome-dependent regulation of p21WAF1/CIP1 expression: M.V. Blagosklonny, et al.; BBRC 227, 564 (1996) Abstract
Enhancement of CPP32-like activity in the TNF-treated U937 cells by the proteasome inhibitors: E. Fujita, et al.; BBRC 224, 74 (1996) Abstract
Degradation of 3-hydroxy-3-methylglutaryl-CoA reductase in endoplasmic reticulum membranes is accelerated as a result of increased susceptibility to proteolysis: T.P. McGee, et al.; J.Biol. Chem. 271, 25630 (1996) Abstract; Full Text
Lactacystin increases LDL receptor level on HepG2 cells: H. Miura, et al.; BBRC 227, 684 (1996) Abstract
Proteasome pathway operates for the degradation of ornithine decarboxylase in intact cells: Y. Murakami, et al.; Biochem. J. 317, 77 (1996) Abstract; Full Text
Lactacystin, an inhibitor of the proteasome, blocks the degradation of a mutant precursor of glycosylphosphatidylinositol-linked protein in a pre-Golgi compartment: K. Oda, et al.; BBRC 219, 800 (1996) Abstract
Degradation of a mutant secretory protein, alpha1-antitrypsin Z, in the endoplasmic reticulum requires proteasome activity: D. Qu, et al.; J. Biol. Chem. 271, 22791 (1996) Abstract; Full Text
Accelerated degradation of PML-retinoic acid receptor alpha (PML-RARA) oncoprotein by all-trans-retinoic acid in acute promyelocytic leukemia: possible role of the proteasome pathway: H. Yoshida, et al.; Cancer Res. 56, 2945 (1996) Abstract
The proteasome inhibitor lactacystin induces apoptosis and sensitizes chemo- and radioresistant human chronic lymphocytic leukaemia lymphocytes to TNF-alpha-initiated apoptosis: J. Delic, et al.; Br. J. Cancer 77, 1103 (1998) Abstract
Lactacystin, proteasome function, and cell fate: G. Fenteany & S.L. Schreiber; J. Biol. Chem. 273, 8545 (1998), (Review) Abstract; Full Text
Proteasome inhibitors prevent the degradation of familial Alzheimer's disease-linked presenilin 1 and potentiate A beta 42 recovery from human cells: P. Marambaud, et al.; Mol. Med. 4, 147 (1998) Abstract
The role of proteolysis during differentiation of Trypanosoma brucei from the bloodstream to the procyclic form: M.C. Mutomba & C.C. Wang; Mol. Biochem. Parasitol. 93, 11 (1998) Abstract
Lactacystin, a proteasome inhibitor: discovery and its application in cell biology: H. Tomoda & S. Omura; Yakugaku Zasshi 120, 935 (2000), Review Abstract
Lactacystin inhibits cathepsin A activity in melanoma cell lines: L. Kozlowski, et al.; Tumour Biol. 22, 211 (2001) Abstract
Proteasome inhibition by lactacystin in primary neuronal cells induces both potentially neuroprotective and pro-apoptotic transcriptional responses: a microarray analysis: E.H. Yew, et al.; J. Neurochem. 94, 943 (2005) Abstract
 
 
ALX-350-246 Revised 07-Mar-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 that acts as a 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
 
 
ALX-350-247 Revised 21-May-08
Genistin
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SYNONYMS Genistein-7-O-glucoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-247-M010   10 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C21H20O10
MW: 432.4
CAS NUMBER: 529-59-9
MERCK INDEX: 14: 4391
PURITY: ≥98%
APPEARANCE: Off-white to light yellow powder.
SOLUBILITY: Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Glucoside of genistein (Prod. No. ALX-350-006) found in soy beans. Useful as a negative control for genistein and other tyrosine kinase inhibitors. Selective inhibitor of terminal deoxyribonucleotidyltransferase (TdT). Displays antioxidant and anticarcinogenic properties.
Product Specific Literature References
Soybean isoflavones, genistein and genistin, inhibit rat myoblast proliferation, fusion and myotube protein synthesis: S. Ji, et al.; J. Nutr. 129, 1291 (1999) Abstract
Daidzein and genistein but not their glucosides are absorbed from the rat stomach: M.K. Piskula, et al.; FEBS Lett. 447, 287 (1999) Abstract
Inhibition of CYP1A1 enzyme activity in mouse hepatoma cell culture by soybean isoflavones: H.G. Shertzer, et al.; Chem. Biol. Interact. 123, 31 (1999) Abstract
Selective inhibitors of terminal deoxyribonucleotidyltransferase (TdT): baicalin and genistin: Y. Uchiyama, et al.; Biochim. Biophys. Acta 1725, 298 (2005) Abstract
Genistin inhibits UV light-induced plasmid DNA damage and cell growth in human melanoma cells: A. Russo, et al.; J. Nutr. Biochem. 17, 103 (2006) Abstract
Pro-apoptotic effect and cytotoxicity of genistein and genistin in human ovarian cancer SK-OV-3 cells: E.J. Choi, et al.; Life Sci. 80, 1403 (2007) Abstract
 
 
ALX-350-248 Revised 23-Jun-05
Daidzin
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SYNONYMS Daidzein-7-O-glucoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-248-M002   2 mg 75.00 USD Add To Cart
ALX-350-248-M010   10 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C21H20O9
MW: 416.4
CAS NUMBER: 552-66-9
MERCK INDEX: 14: 2801
PURITY: ≥98%
APPEARANCE: White to beige powder.
SOLUBILITY: Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Glucoside of the isoflavone daidzein (Prod. No. ALX-350-009) found in soy beans.
Product Specific Literature References
Metabolism of puerarin and daidzin by human intestinal bacteria and their relation to in vitro cytotoxicity: D.H. Kim, et al.; Biol. Pharm. Bull. 21, 628 (1998) Abstract
Daidzin and its antidipsotropic analogs inhibit serotonin and dopamine metabolism in isolated mitochondria: W.M. Keung & B.L. Vallee; PNAS 95, 2198 (1998) Abstract
Daidzein and genistein but not their glucosides are absorbed from the rat stomach: M.K. Piskula, et al.; FEBS Lett. 447, 287 (1999) Abstract
Further Categories Containing This Product:
Flavonoids/Related Products • Active Substances from Fruit and Vegetables
 
 
ALX-350-249 Revised 08-Apr-08
Puerarin
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SYNONYMS 8-(β-D-Glucopyranosyl-7-hydroxy-3- (4-hydroxyphenyl)-4H-1-benzopyran-4-one
NPI-031G
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-350-249-M005   5 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C21H20O9
MW: 416.4
CAS NUMBER: 3681-99-0
RTECS: UO5216000
SOURCE/HOST: Isolated from Kudzu root.
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Biologically active isoflavone. Affects serotonin levels and platelet aggregation in blood cells. Is a 5-HT2c antagonist. Antibacterial. Displays cardioprotective effects. Induces apoptosis.
Product Specific Literature References
Daidzin and its antidipsotropic analogs inhibit serotonin and dopamine metabolism in isolated mitochondria: W.M. Keung & B.L. Vallee; PNAS 95, 2198 (1998) Abstract
Metabolism of puerarin and daidzin by human intestinal bacteria and their relation to in vitro cytotoxicity: D.H. Kim, et al.; Biol. Pharm. Bull. 21, 628 (1998) Abstract
NPI-031G (puerarin) reduces anxiogenic effects of alcohol withdrawal or benzodiazepine inverse or 5-HT2C agonists: D.H. Overstreet, et al.; Pharmacol. Biochem. Behav. 75, 619 (2003) Abstract
Puerarin reduces increased c-fos, c-jun, and type IV collagen expression caused by high glucose in glomerular mesangial cells: C.P. Mao & Z.L. Gu; Acta Pharmacol. Sin. 26, 982 (2005) Abstract
Contrasting effects of puerarin and daidzin on glucose homeostasis in mice: E. Meezan, et al.; J. Agric. Food Chem. 53, 8760 (2005) Abstract
Induction of apoptosis by puerarin in colon cancer HT-29 cells: Z. Yu & W. L; Cancer Lett. 238, 53 (2006) Abstract
Opening the calcium-activated potassium channel participates in the cardioprotective effect of puerarin: 574, 179 (2007)
:
Q. Gao, et al.; Eur. J. Pharmacol. 574, 179 (2007) Abstract
Further Categories Containing This Product: