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CAS NO.446-72-0
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Best price 446-72-0 genistein 446-72-0 Good Supplier In China genistein powder
A cell-permeable, reversible, substrate competitive inhibitor of protein tyrosine kinases, including autophosphorylation of epidermal growth factor receptor kinase (IC50 = 2.6 µM). The inhibition is competitive with respect to ATP and non-competitive with respect to the phosphate acceptor. Has only a trivial effect on the activity of PKA and PKC (IC50 >350 µM). Inhibits tumor cell proliferation and induces tumor cell differentiation. Produces cell cycle arrest and apoptosis in Jurkat T-leukemia cells. However, it prevents anti-CD3 monoclonal antibody-induced thymic apoptosis. Also inhibits topoisomerase II activity
Genistein, an isoflavonoid found in soy products, has wide variety of pharmacological effects in animal cells, including tyrosine kinase and topoisomerase II inhibition. And then, many reports suggests that genistein may reduce the risk of tumor formation.
Genistein is an isoflavonoid phytoestrogen that has been found in soybeans (G. max/S. hispida) and has kinase inhibitory, anticancer, pro-cancer, hepatoprotective, and antiviral properties. It inhibits the tyrosine kinases EGFR, pp50v-Src, and pp110gag-fes (IC50s = 6, 7-8, and 6.5 µg/ml, respectively) and decreases EGF-induced serine, threonine, and tyrosine phosphorylation of EGFR in A431 cells when used at a concentration of 20 µg/ml. Genistein inhibits proliferation and induces apoptosis in a variety of cancer cells, including Bel 7402 hepatocellular carcinoma cells when used at a concentration of 10 µg/ml. It reduces tumor invasion and angiogenesis in a Bel 7402 mouse subrenal capsule xenograft model when administered at a dose of 50 mg/kg per day. However, when administered at the same dose on postnatal days 1-5, genistein increases the incidence of uterine adenocarcinoma in a mouse model of cancer induced by the estrogen receptor agonist diethylstilbestrol (DES; Item No. 10006876). It reduces lipid accumulation and inflammation in the liver of ovariectomized (OVX) and non-OVX female rats in a model of high-fat high-fructose diet-induced nonalcoholic hepatosteatosis (NASH) when administered at a dose of 16 mg/kg per day. Genistein (10 µM) also inhibits HIV-1 DNA synthesis in resting CD4+ T cells.
Catalogue Number | G350000 |
Chemical Name | Genistein |
Synonyms | 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one; Baichanin A; Bonistein; 4',5,7-Trihydroxyisoflavone; GeniVida; Genisteol; NSC 36586; Prunetol; Sophoricol; |
CAS Number | 446-72-0 |
Molecular Formula | C??H??O? |
Appearance | Pale Yellow to Light Beige Solid |
Melting Point | >277°C (dec.) |
Molecular Weight | 270.24 |
Storage | Amber Vial, -20°C Freezer, Under inert atmosphere |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Stability | Light Sensitive |
Category | Standards; Enzyme Activators and Inhibitors; |
Applications | Exhibits specific inhibitory activity against tyrosine kinases,including autophosphorylation of epidermal growth factor receptor kinase (IC50 - 2.6uM). Also inhibits other protein kinases through competitive inhibition of ATP. Inhibits tumor cell proliferation and induces tumor cell differentiation. Produces cell-cycle arrest and apoptosis in Jurat T-leukemia cells. However, it prevents anti-CD3 monoclonal antibody-induced thymic apoptosis. Genistein also inhibits topoisomerase II activity in vitro. Genistein has also been shown to inhibit the action of GABA on recombinant GABAA receptors 2. uv(max)ethanol: 262.5 nm (e= 138). moderately sol. in hot alcohol |