ERB 041 |
| Catalog No.GC10389 |
ERB 041 (ERB-041) est un récepteur d'oestrogène puissant et sélectif (ER) β ; agoniste avec des IC50 de 5,4, 3,1 et 3,7 nM pour l'homme, le rat et la souris ERβ ;, respectivement. ERB 041 affiche une sélectivité >200 fois pour ERβ ; sur ERα ;. ERB 041 est un puissant agent chimiopréventif du cancer de la peau qui agit en atténuant la voie de signalisation WNT/β-caténine. ERB 041 induit l'apoptose du cancer de l'ovaire.
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Cas No.: 524684-52-4
Sample solution is provided at 25 µL, 10mM.
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Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta.IC50 value:Target: ERbeta agonistin vitro: Treatment with ERβ selective estrogen agonists liquiritigenin and ERB-041 reduced the ability to invade a reconstituted basement membrane and to migrate in response to the cellular stimulus [1]. Pretreatment the PMs with ERB-041 resulted in a significant inhibition of LPS-induced iNOS expression and NF-kappaB activation by preventing its nuclear translocation [3].in vivo: Tumor numbers and volume were reduced by 60% and 84%, respectively, in the Erb-041-treated group as compared with UVB (alone) control. This inhibition in tumorigenesis was accompanied by the decrease in proliferating cell nuclear antigen (PCNA), cyclin D1, VEGF, and CD31, and an increase in apoptosis [2].
References:
[1]. Hinsche O, et al. Estrogen receptor β selective agonists reduce invasiveness of triple-negative breast cancer cells. Int J Oncol. 2015 Feb;46(2):878-84.
[2]. Chaudhary SC, et al. Erb-041, an estrogen receptor-β agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014 Feb;7(2):186-98.
[3]. Xiu-li W, et al. ERB-041, a selective ER beta agonist, inhibits iNOS production in LPS-activated peritoneal macrophages of endometriosis via suppression of NF-kappaB activation. Mol Immunol. 2009 Jul;46(11-12):2413-8.
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