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Tyrosine Kinase Inhibitors
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ALX-380-091 Revised 03-Apr-08
17-AAG
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SYNONYMS 17-(Allylamino)-17-desmethoxygeldanamycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-091-M001   1 mg 162.00 USD Add To Cart
ALX-380-091-C100   100 µg 65.00 USD Add To Cart
Product Specification
FORMULA: C31H43N3O8
MW: 585.7
CAS NUMBER: 75747-14-7
SOURCE/HOST: Semisynthetic derivative from geldanamycin.
PURITY: ≥97%
APPEARANCE: Red to dark red powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent, less toxic derivative of geldanamycin (Prod. No. ALX-380-054). Inhibits the essential ATPase activity of HSP90. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity.
Product Specific Literature References
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: R.C. Schnur, et al.; J. Med. Chem. 38, 3806 (1995) Abstract
The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin: T.W. Schulte & L.M. Neckers; Cancer Chemother. Pharmacol. 42, 273 (1998) Abstract
Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone: P.A. Clarke, et al.; Oncogene 19, 4125 (2000) Abstract
Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts: R. Nimmanapalli, et al.; Cancer Res. 61, 1799 (2001) Abstract; Full Text
Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells: P.N. Munster, et al.; Cancer Res. 61, 2945 (2001) Abstract; Full Text
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin: J. Yang, et al.; Cancer Res. 61, 4010 (2001) Abstract; Full Text
Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis: D.M. Nguyen, et al.; Ann. Thorac. Surg. 72, 371 (2001) Abstract
ErbB2 degradation mediated by the co-chaperone protein CHIP: P. Zhou, et al.; J. Biol. Chem. 278, 13829 (2003) Abstract
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis 24, 851 (2003) Abstract
Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction: I.A. Vasilevskaya, et al.; Cancer Res. 63, 3241 (2003) Abstract
A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors: A. Kamal, et al.; Nature 425, 407 (2003) Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006) Abstract
Drugging the cancer chaperone HSP90: Combinatorial therapeutic exploitation of oncogene addiction and tumor stress: P. Workman, et al.; Ann. N.Y. Acad. Sci. 1113, 202 (2007) Abstract
Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51: Q. Yao, et al.; Clin. Cancer Res. 13, 1591 (2007) Abstract; Full Text
Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers: R.K. Ramanathan, et al.; Clin. Cancer Res. 13, 1769 (2007) Abstract
HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells: P.N. Meyer, et al.; Leuk. Res. 32, 143 (2008) Abstract
Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model: C.R. Williams, et al.; J. Urol. 178, 1528 (2007) Abstract
Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia: A.J. Johnson, et al.; Br. J. Haematol. 139, 837 (2007) Abstract
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models: U. Banerji, et al.; Cancer Chemother. Pharmacol. Epub ahead of print, (2008) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Tyrosine Kinase Inhibitors • Antibiotics - Other Signal Transduction Pathway Modulators • HSP90/HtpG/Related Products
 
 
ALX-430-096 Revised 24-Feb-05
A77 1726
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SYNONYMS N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-430-096-M005   5 mg 45.00 USD Add To Cart
ALX-430-096-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C12H9F3N2O2
MW: 270.2
CAS NUMBER: 108605-62-5
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No. ALX-430-095). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2) in vitro and in vivo.
Product Specific Literature References
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms: R.T. Elder, et al.; J. Immunol. 159, 22 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression: S.K. Manna & B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract
Further Categories Containing This Product:
Immunomodulators Other Products • COX Inhibitors • NF-kB Pathway Inhibitors
 
 
ALX-151-026 Revised 20-Jun-08
N-Acetyl-Asp-Tyr(2-malonyl)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-026-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C39H57N7O14S
MW: 880.0
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Peptide is very unstable.
Product Description
Peptide containing a phosphotyrosyl mimetic. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides: B. Ye, et al.; J. Med. Chem. 38, 4270 (1995) Abstract
Further Categories Containing This Product:
Phosphoinositide 3-kinase [PI(3)K]/Related Products • Peptides
 
 
ALX-151-027 Revised 17-Jan-05
N-Acetyl-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-027-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C36H57N7O13SP
MW: 858.9
PURITY: ≥96%
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Phosphotyrosine containing peptide. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides: B. Ye, et al.; J. Med. Chem. 38, 4270 (1995) Abstract
Further Categories Containing This Product:
Phosphoinositide 3-kinase [PI(3)K]/Related Products • Peptides
 
 
ALX-350-256 Revised 03-Apr-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
HAZARD: CYTOTOXIC.

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
 
 
ALX-350-325 Revised 25-Jun-07
Altenusin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-350-325-M001   1 mg 110.00 USD Add To Cart
ALX-350-325-M005   5 mg 380.00 USD Add To Cart
Product Specification
FORMULA: C15H14O6
MW: 290.3
CAS NUMBER: 31186-12-6
SOURCE/HOST: Isolated from Alternaria sp.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow 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 1H-NMR, 13C-NMR and MS.

Product Description
Antifungal penicillide. Non-competitive, specific neutral sphingomyelinase (N-SMase) and strong pp60c-Src inhibitor. Inhibits cFMS receptor tyrosine kinase (CSF-1/m-CSF receptor tyrosine kinase) which is implicated in cancer and bone diseases. Myosin light chain kinase inhibitor. Exhibits anti-HIV-1 integrase activity.
Product Specific Literature References
Studies in the biochemistry of micro-organisms. 103. Metabolites of Alternaria tenuis Auct.: Culture filtrate products: T. Rosett, et al.; Biochem. J. 67, 390 (1957) Full Text
Studies in the biosynthesis of fungal metabolites. 4. Alternariol monomethyl ether and its relation to other phenolic metabolites of Alternaria tenuis: R. Thomas; Biochem. J. 80, 234 (1961) Abstract; Full Text
Metabolites of some Alternaria species. The structures of altenusin and dehydroaltenusin: R. G. Coombe, et al.; Aus. J. Chem. 23, 2343 (1970)
Host-specific toxins and chemical structures from alternaria species: S. Nishimura, et al.; Ann. Rev. Phytopathol. 21, 87 (1983)
The metabolites of Talaromycesflavus: Part 1. Metabolites of the organic extracts : W. A. Ayer, et al.; Can. J. Chem. 68, 2085 (1990)
Isolation of myosin light chain kinase inhibitors from microorganisms: dehydroaltenusin, altenusin, atrovenetinone, and cyclooctasulfur: S. Nakanishi, et al.; Biosci. Biotechnol. Biochem. 59, 1333 (1995) Abstract
Alutenusin, a specific neutral sphingomyelinase inhibitor, produced by Penicillium sp. FO-7436: R. Uchida, et al.; J. Antibiot. 52, 572 (1999) Abstract
Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites: S.B. Singh, et al.; J. Ind. Microbiol. Biotechnol. 30, 721 (2003) Abstract
Fungal metabolites as potent protein kinase inhibitors: Identification of a novel metabolite and novel activities of known metabolites : M. Oyama, et al.; Lett. Drug Design Discov. 1, 24 (2004)
New penicillide derivatives isolated from Penicillium simplicissimum: S. I. Komai, et al.; J. Nat. Med. 60, 185 (2006)
HIV-1 integrase inhibitors: 2003-2004 update: R. Dayam, et al.; Med. Res. Rev. 26, 271 (2006) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • Antibiotics - Antiviral/Anti-HIV
 
 
ALX-385-021 Revised 23-Oct-07
4'-Amino-6-hydroxyflavone
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SYNONYMS Aminogenistein
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonoids/Related Products
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ALX-385-021-M001   1 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C15H11NO3
MW: 253.3
PURITY: ≥95%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of the p56lck protein-tyrosine kinase.
Product Specific Literature References
Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogues: M. Cushman, et al.; J. Med. Chem. 34, 798 (1991) Abstract
Expression of p56lck in B-cell neoplasias: A. Von Knethen, et al.; Leuk. Lymphoma 26, 551 (1997) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Src Family Kinases/Related Products • Kinases in T Cell Signal Transduction/Related Products
 
 
ALX-380-208 Revised 03-Apr-08
Asterric acid
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SYNONYMS Dimethylosoic acid
TAN 1415A
WF 12880A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
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ALX-380-208-M001   1 mg 220.00 USD Add To Cart
Product Specification
FORMULA: C17H16O8
MW: 348.3
CAS NUMBER: 577-64-0
SOURCE/HOST: Isolated from Aspergillus terreus MST-FP1370.
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Antibiotic. Inhibitor of vascular endothelial growth factor (VEGF).
Product Specific Literature References
Studies in the biochemistry of micro-organisms. 115. Metabolites of Penicillium frequentans Westling: isolation of sulochrin, asterric acid, (+)-bisdechlorogeodin and two new substituted anthraquinones, questin and questinol: A. Mahmoodian and C.E. Stickings; Biochem. J. 92, 369 (1964) Abstract; Full Text
Asterric acid, a new endothelin binding inhibitor: H. Ohashi, et al.; J. Antibiot. (Tokyo) 45, 1684 (1992) Abstract
Fungal metabolites, asterric acid derivatives inhibit vascular endothelial growth factor (VEGF)-induced tube formation of HUVECs: H.J. Lee, et al.; J. Antibiot. (Tokyo) 55, 552 (2002) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • VEGFs & VEGF-Rs Other Products
 
 
ALX-385-022 Revised 19-Nov-07
Baicalein
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SYNONYMS 5,6,7-Trihydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonoids/Related Products
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ALX-385-022-M005   5 mg 25.00 USD Add To Cart
ALX-385-022-M025   25 mg 100.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 491-67-8
MERCK INDEX: 14: 942
PURITY: ≥97%
APPEARANCE: Yellow to yellow-green crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol; almost insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Inhibitor of 12-lipoxygenase, leukotriene biosynthesis and the release of lysosomal enzymes. Inhibits cellular Ca2+ uptake and calcium mobilization. Inhibitor of protein tyrosine kinase in leukemia (CEM) cells. Induces cell cycle arrest and apoptosis. Anti-inflammatory compound. Has anti-thrombotic, anti-proliferative and anti-mitogenic effects.
Product Specific Literature References
Specific action of the lipoxygenase pathway in mediating angiotensin II- induced aldosterone synthesis in isolated adrenal glomerulosa cells: J.L. Nadler, et al.; J. Clin. Invest. 80, 1763 (1987) Abstract
Inhibition of reverse transcriptase activity by a flavonoid compound, 5,6,7-trihydroxyflavone: K. Ono, et al.; BBRC 160, 982 (1989) Abstract
Biliary excretion of metabolites of baicalin and baicalein in rats: K. Abe, et al.; Chem. Pharm. Bull. 38, 209 (1990) Abstract
Effects of baicalein and esculetin on transduction signals and growth factors expression in T-lymphoid leukemia cells: H.C. Huang, et al.; Eur. J. Pharmacol. 268, 73 (1994) Abstract
Protective effects of baicalein against cell damage by reactive oxygen species: D. Gao, et al.; Chem. Pharm. Bull. (Tokyo) 46, 1383 (1998) Abstract
Baicalein induces a dual growth arrest by modulating multiple cell cycle regulatory molecules
: S.L. Hsu, et al.; Eur. J. Pharmacol. 425, 165 (2001) Abstract
Mechanisms in mediating the anti-inflammatory effects of baicalin and baicalein in human leukocytes: Y.C. Shen, et al.; Eur. J. Pharmacol. 465, 171 (2003) Abstract
Baicalein induced cell cycle arrest and apoptosis in human lung squamous carcinoma CH27 cells: H.Z. Lee, et al.; Anticancer Res. 25, 959 (2005) Abstract
Biological properties of baicalein in cardiovascular system: Y. Huang, et al.; Curr. Drug Targets Cardiovasc. Haematol. Disord. 5, 177 (2005), (Review) Abstract
Baicalein inhibition of hydrogen peroxide-induced apoptosis via ROS-dependent heme oxygenase 1 gene expression: H.Y. Lin, et al.; Biochim. Biophys. Acta 1773, 1073 (2007) Abstract
Further Categories Containing This Product:
Natural Products for Angiogenesis Research • Tyrosine Kinase Inhibitors • Natural Products - Protein Kinase Inhibitors • Natural Products - Antiviral/anti-HIV Agents • Leukotrienes Other Products • Lipoxygenases/Related Products • Cell Cycle Blockers & Inhibitors/Related Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products - Antioxidants • Natural Products for Cell Cycle Research