DB1976 |
| カタログ番号GC39627 |
DB1976 は、DB270 のセレノフェン類似体であり、強力で細胞透過性の完全に有効な転写因子 PU.1 阻害剤です。 DB1976 は、PU.1 結合を強力に阻害し (IC50 10 nM)、PU.1/DNA 複合体を強力に阻害します (高い DB1976-ΛB 親和性、KD 12 nM)。 DB1976 にはアポトーシス誘導効果があります。
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Cas No.: 1557397-51-9
Sample solution is provided at 25 µL, 10mM.
DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-ΛB affinity, KD of 12 nM) in vitro. DB1976 has apoptosis-inducing effect[1][2][3].
[1]. Munde M, et al. Structure-dependent inhibition of the ETS-family transcription factor PU.1 by novel heterocyclic diamidines. Nucleic Acids Res. 2014 Jan;42(2):1379-90. [2]. Stephens DC, et al. Pharmacologic efficacy of PU.1 inhibition by heterocyclic dications: a mechanistic analysis. Nucleic Acids Res. 2016 May 19;44(9):4005-13. [3]. Antony-DebrÉ I, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017 Dec 1;127(12):4297-4313.
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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