DB1976 hydrochloride is a selenium selenium analogue of DB270, a potent and permeable cell transcription factor PU.1 inhibitor. In vitro, DB1976 hydrochloride effectively inhibited PU.1 binding (IC50 of 10 nM) and strongly inhibited PU.1 / DNA complex (with high DB1976-λB affinity, KD of 12 nM). DB1976 hydrochloride has the effect of inducing apoptosis.

DB1976 is a classic heterocyclic compound (single heteroatom), which has a strong affinity and selectivity for the AT-rich sequences common to the homologous DNA binding site of PU.1. DB1976 inhibited the PU.1-dependent transactivation of the reporter gene in PU.1-negative HEK293 cells in a dose-dependent manner, with an IC50 value of 2.4 μM. DB1976 treatment resulted in a significant reduction in the growth of PU.1 URE – / – AML cells (IC50 of 105 μM), but at a similar concentration (IC50 of 334 μM) there was little effect on normal hematopoietic cells [3]. DB1976 treatment resulted in a 1.6-fold increase in murine PU.1 URE – / – AML apoptotic cells, and a similar effect was observed in human MOLM13 cells [3]. Compared with vehicle-treated cells, DB1976 treatment resulted in a significant reduction in the number of viable cells (primary human AML cells) (average reduction of 81%) and clonal formation capacity (average reduction of 36%). Using DB1976 can increase the average number of apoptotic cells by 1.5 times.

2369663-93-2

C20H18Cl2N8Se

520.28

DB1976 hydrochloride;DB1976 dihydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years