Chemical Name: 1-[2-(2-Thiazolyl)diazenyl]-2-naphthalenol
Biological ActivityHigh affinity Rio Kinase 2 (RIOK2) inhibitor (Kd = 200 nM). Exhibits >6-fold selectivity for RIOK2 over a panel of 456 kinases. Inhibits ERG protein and potently inhibits growth of ERG-positive VCaP prostate cancer cells in vitro (IC50 = 169 nM) but not ERG-negative cell lines. Also inhibits growth of VCaP xenografts in mice.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth.
Mohamed et al.
Cancer Res., 2018;78:3659
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