DB1976 (dihydrochloride)

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].

Product Specifications

CAS Number

[2369663-93-2]

UNSPSC

12352005

Target

Apoptosis

Type

Reference compound

Related Pathways

Apoptosis

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/db1976-hydrochloride.html

Purity

98.0

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 18.33 mg/mL (ultrasonic)

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

Molecular Formula

C20H18Cl2N8Se

Molecular Weight

520.28

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Citation 01

Cell Rep. 2024 Mar 26;43 (3) :113964.|Int J Biol Macromol. 2025 Sep;322 (Pt 1) :146515.|Nat Immunol. 2023 Nov;24 (11) :1839-1853.|Respir Res. 2023 Jan 25;24 (1) :32.|Neurochem Int. 2024 Feb:173:105674.