2369663-93-2
Chemical Structure
DB1976 dihydrochloride
- CAS No.: 2369663-93-2
- Formula:C20H18Cl2N8Se
- Molecular Weight:520.28
IUPAC Name: 2,2'-(selenophene-2,5-diyl)bis(1H-benzo[d]imidazole-6-carboximidamide) dihydrochloride
InChIKey: ZXDJCXGSFWTRMS-UHFFFAOYSA-N
SMILES: N=C(C1=CC=C2N=C(C3=CC=C(C4=NC5=CC=C(C(N)=N)C=C5N4)[Se]3)NC2=C1)N.[H]Cl.[H]Cl
Biological Activity: DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride 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 dihydrochloride has apoptosis-inducing effect[1][2][3].
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DB1976 dihydrochloride | 98.0% | DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride 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 dihydrochloride has apoptosis-inducing effect. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords