DB1976 hydrochloride |
| Catalog No.GC39628 |
Le chlorhydrate de DB1769 est un analogue sélénophène de DB270 et un inhibiteur puissant et perméable aux cellules du facteur de transcription PU.1. Le chlorhydrate de DB1769 inhibe puissamment la liaison de PU.1 (IC50 de 10 nM) et inhibe fortement le complexe PU.1/ADN (avec une forte affinité DB1769-ΛB, KD de 12 nM) in vitro. Le chlorhydrate de DB1769 a un effet inducteur d'apoptose.
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Cas No.: 2369663-93-2
Sample solution is provided at 25 µL, 10mM.
DB1976 hydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 hydrochloride 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 hydrochloride 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.
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