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DB1976 dihydrochloride

Catalog No. T10964L   CAS 2369663-93-2
Synonyms: DB1976 hydrochloride, DB1976 2HCl

DB1976 dihydrochloride (DB1976 2HCl) , a transcription factor PU.1 inhibitor with potential anti-inflammatory activity, slowed down inflammation and fibrosis and improved glucose homeostasis and dyslipidemia in mice in in vivo experiments.DB1976 dihydrochloride promotes apoptosis and may be used in studies of metabolic dysfunction and non-alcoholic steatohepatitis.

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DB1976 dihydrochloride Chemical Structure
DB1976 dihydrochloride, CAS 2369663-93-2
Pack Size Availability Price/USD Quantity
5 mg 6-8 weeks $ 390.00
25 mg 6-8 weeks $ 1,330.00
50 mg 6-8 weeks $ 1,740.00
100 mg 6-8 weeks $ 2,500.00
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Purity: 99.08%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description DB1976 dihydrochloride (DB1976 2HCl) , a transcription factor PU.1 inhibitor with potential anti-inflammatory activity, slowed down inflammation and fibrosis and improved glucose homeostasis and dyslipidemia in mice in in vivo experiments.DB1976 dihydrochloride promotes apoptosis and may be used in studies of metabolic dysfunction and non-alcoholic steatohepatitis.
Targets&IC50 PU.1:10 nM, PU.1 URE–/–AML cells:105 μM, PU.1-negative HEK293 cells:2.4 μM, Hematopoietic cells:334 μM
In vitro DB1976 dihydrochloride , a classic heterocyclic dication with strong affinity and selectivity for AT-rich sequences commonly found in cognate DNA binding sites for PU.1[3], inhibits PU.1-dependent transactivation of the reporter in a dose-dependent manner with an IC50 value of 2.4 μM in PU.1-negative HEK293 cells[2].
Treatment with DB1976 dihydrochloride leads to a profound decrease in the growth of PU.1 URE–/– AML cells (IC50 of 105 μM), while exhibiting little effect on normal hematopoietic cells at similar concentrations (IC50 of 334 μM)[2].Furthermore,DB1976 dihydrochloride treatment results in a 1.6-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells, with similar effects observed in human MOLM13 cells[3].In addition, DB1976 dihydrochloride treatment causes a significant decrease in the number of viable cells (primary human AML cells) (mean decrease of 81%) and clonogenic capacity (mean decrease of 36%) compared to vehicle-treated cells. The apoptotic cell fraction increases on average by 1.5-fold with DB1976 dihydrochloride[2].
Synonyms DB1976 hydrochloride, DB1976 2HCl
Molecular Weight 520.28
Formula C20H18Cl2N8Se
CAS No. 2369663-93-2

Storage

store at low temperature

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

Solubility Information

DMSO: 20 mg/mL (38.44 mM), Sonification is recommended.

H2O: 10 mg/mL (19.22 mM), Sonification is recommended.

TargetMolReferences 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. 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. 3. 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.

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Keywords

DB1976 dihydrochloride 2369663-93-2 Apoptosis NF-Κb NF-κB DB1976 hydrochloride DB1976 2HCl inhibitor inhibit

 

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