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DB1976

Catalog No. T10964 CAS 1557397-51-9

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.

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DB1976, CAS 1557397-51-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 197.00
5 mg	In stock	$ 397.00
10 mg	In stock	$ 589.00
25 mg	In stock	$ 945.00
50 mg	In stock	$ 1,280.00
100 mg	In stock	$ 1,730.00
500 mg	In stock	$ 3,460.00

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Purity: 98.94%

Biological Description

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Description	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.
Targets&IC50	PU.1:10 nM
In vitro	DB1976 is a heterocyclic dication possessing a strong affinity and selectivity for AT-rich sequences in DNA, which are crucial for the binding of transcription factor PU.1. It effectively inhibits the activation mediated by PU.1 in a dose-dependent manner, displaying an IC50 of 2.4 μM in PU.1-negative HEK293 cells. Importantly, DB1976 significantly reduces the growth of PU.1 URE–/– AML cells, with an IC50 of 105 μM, while minimally affecting normal hematopoietic cells (IC50 of 334 μM). Treatment with DB1976 results in a notable increase in apoptosis, particularly a 1.6-fold rise in murine PU.1 URE–/– AML cells and similar outcomes in human MOLM13 cells. Furthermore, DB1976 dramatically reduces the viability (by 81%) and clonogenic capacity (by 36%) of primary human AML cells compared to those treated with a vehicle, alongside effecting a 1.5-fold increase in the apoptotic cell fraction.

Molecular Weight	447.35
Formula	C20H16N8Se
CAS No.	1557397-51-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Insoluble

References and Literature

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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Keywords

DB1976 1557397-51-9 Apoptosis Others DB-1976 DB 1976 inhibitor inhibit

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