AGN 196996是高活性RARα选择性抑制剂，Ki为2 nM，对RARβ和RARγ的亲和性极低（Ki分别为1087 nM和8523 nM）。
CAS：958295-17-5
分子式：C24H20BrNO5
分子量：482.32
纯度：98%
存储：Store at -20°C

Background:

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.