AGN 196996 |
Katalog-Nr.GC35266 |
AGN 196996 ist ein potenter und selektiver RARα-Antagonist mit einem Ki-Wert von 2 nM; geringe BindungsaffinitÄt fÜr RARβ (Ki = 1087 nM) und RARγ (Ki = 8523 nM).
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Cas No.: 958295-17-5
Sample solution is provided at 25 µL, 10mM.
AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).IC50 value: 2 nM(Ki)Target: RARα antagonistAGN 196996 shows no activity in transactivation assays, but instead block the gene transcriptional activity induced by ATRA and other RAR agonists.
[1]. Hammond LA, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62. [2]. Keedwell RG, et al. An antagonist of retinoic acid receptors more effectively inhibits growth of human prostate cancer cells than normal prostate epithelium. Br J Cancer. 2004 Aug 2;91(3):580-8.
Average Rating: 5
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