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Tyrosine kinase inhibitor
Tyrosine protein kinase inhibitor. Inhibits phosphorylation of EGFR kinase. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits topoisomerase II activity in vivo. Produces cell cycle arrest and apoptosis. Potent inhibitor of α-glucosidase, IC50 = 50nM.Direct inhibitor of insulin-induced glucose uptake in adipocytes (IC50=20µM).
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Product Details
| Alternative Name |
4′,5,7-Trihydroxyisoflavone |
|---|---|
| Appearance |
Creamy off-white solid. |
| CAS |
446-72-0 |
| Couple Target |
Glucosidase, Topoisomerase |
| Couple Type |
Inhibitor |
| Formula |
C15H10O5 |
| MI |
14: 4391 |
| MW |
270.2 |
| Purity |
≥98% (HPLC) |
| RTECS |
NR2392000 |
| Solubility |
Soluble in DMSO (30mg/ml), 100% ethanol (4mg/ml) or dilute aqueous base; insoluble in water. |
| Source |
Synthetic. |
| Technical Info / Product Notes |
Replacement for ADI-HPK-103 |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Handling |
Protect from light. |
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Genistein-mediated thermogenesis and white-to-beige adipocyte differentiation involve transcriptional activation of cAMP response elements in the Ucp1 promoter: R.F. Romero, et al.; FASEB J. 37, 23079 (2023), Abstract
- Genistein Stimulation of White Adipose Tissue Thermogenesis Is Partially Dependent on GPR30 in Mice: S. Vasquez-Reyes, et al.; Mol. Nutr. Food Res. 66, e2100838 (2022), Abstract
- GM101 in Combination with Histone Deacetylase Inhibitor Enhances Anti-Tumor Effects in Desmoplastic Microenvironment: H.G. Chang, et al.; Cells 10, 2811 (2021), Application(s): U343 cells treatment, Abstract — Full Text
- Effects of Ipriflavone-Loaded Mesoporous Nanospheres on theDifferentiation of Endothelial Progenitor Cells and TheirModulation by Macrophages: L. Casarrubios, et al.; Nanomaterials 11, 1102 (2021), Abstract
- Serine-727 phosphorylation activates hypothalamic STAT-3 independently from tyrosine-705 phosphorylation: A. Breit, et al.; Mol. Endocrinol. 29, 445 (2015), Application(s): ELISA, Abstract — Full Text
- Soy isoflavones augment the effect of TRAIL-mediated apoptotic death in prostate cancer cells: Szliszka, E., Krol, W., et al.; Oncol. Rep. 26, 533 (2011), Abstract
- The combination of TRAIL and isoflavones enhances apoptosis in cancer cells: Bronikowska, J., Szliszka, E., et al.; Molecules 15, 2000 (2010), Abstract
- Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006), Abstract
- Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review, Abstract
- The role of genistein and synthetic derivatives of isoflavone in cancer prevention and therapy: F.H. Sarkar, et al.; Mini Rev. Med. Chem. 6, 401 (2006), Review, Abstract
- Genistein directly inhibits GLUT4-mediated glucose uptake in 3T3-L1 adipocytes: M. Bazuine, et al.; BBRC 325, 511 (2005), Abstract
- Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005), Abstract
- Soy isoflavone phyto-pharmaceuticals in interleukin-6 affections. Multi-purpose nutraceuticals at the crossroad of hormone replacement, anti-cancer and anti-inflammatory therapy: N. Dijsselbloem, et al.; Biochem. Pharmacol. 68, 1171 (2004), Review, Abstract
- Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus): M. Opalka, et al.; Reprod. Biol. 4, 185 (2004), Abstract
- Mechanisms of cancer chemoprevention by soy isoflavone genistein: F.H. Sarkar & Y. Li; Cancer Metastasis Rev. 21, 265 (2002), Abstract
- Genistein, a soy isoflavone, is a potent alpha-glucosidase inhibitor: D.S. Lee & S.H. Lee; FEBS Lett. 501, 84 (2001), Abstract
- The role of tyrosine phosphorylation in signal transduction through surface Ig in human B cells. Inhibition of tyrosine phosphorylation prevents intracellular calcium release: P.J. Lane et al.; J. Immunol. 146, 715 (1991), Abstract
- Platelet-activating factor stimulation of tyrosine kinase and its relationship to phospholipase C in rabbit platelets: studies with genistein and monoclonal antibody to phosphotyrosine: A. Dhar et al.; Mol. Pharmacol. 37, 519 (1990), Abstract
- Effect of genistein, a tyrosine kinase inhibitor, on U46619-induced phosphoinositide phosphorylation in human platelets: D.C. Gaudette & J. B. Holub; Biochem. Biophys. Res. Commun. 170, 238 (1990), Abstract
- T cell antigen receptor-mediated activation of phospholipase C requires tyrosine phosphorylation: T. Mustelin et al.; Science 247, 1584 (1990), Abstract
- Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets: H. Salari, et al.; FEBS Lett. 263, 104 (1990), Abstract
- Differential inhibition of T cell receptor signal transduction and early activation events by a selective inhibitor of protein-tyrosine kinase: J.M. Trevillyan et al.; J. Immunol. 145, 3223 (1990), Abstract
- Mechanisms of action in NIH-3T3 cells of genistein, an inhibitor of EGF receptor tyrosine kinase activity: C. Linassier et al.; Biochem. Pharmacol. 39, 187 (1990), Abstract
- Inhibitory effects of the tyrosine kinase inhibitor genistein on mammalian DNA topoisomerase II: J. Markovits et al.; Cancer Res. 49, 5111 (1989), Abstract — Full Text
- Effects of the tyrosine-kinase inhibitor genistein on DNA synthesis and phospholipid-derived second messenger generation in mouse 10T1/2 fibroblasts and rat liver T51B cells: N.M. Dean et al.; Biochem. Biophys. Res. Commun. 165, 795 (1989), Abstract
- Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987), Abstract — Full Text
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