NVS-CECR2-1 (Synonyms: NVS-1) |
| カタログ番号GC44477 |
非 BET ファミリー ブロモドメイン (BRD) 阻害剤である NVS-CECR2-1 は、強力かつ選択的なキャットアイ症候群染色体領域、候補 2 (CECR2) 阻害剤です。 NVS-CECR2-1 は高い親和性で CECR2 BRD に結合します (IC50=47 nM; KD=80 nM)。 NVS-CECR2-1 は細胞傷害活性を示し、CECR2 を標的とすることによって、および CECR2 に依存しないメカニズムによって、さまざまな癌細胞に対してアポトーシスを誘導します。
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Cas No.: 1992047-61-6
Sample solution is provided at 25 µL, 10mM.
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NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 µM by Alpha screen, Kd = 0.80 µM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has no acute toxicity. See the Structural Genomics Consortium (SGC) website for more information.
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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