DB1976

CAS No. 1557397-51-9

DB1976( —— )

Catalog No. M32877 CAS No. 1557397-51-9

DB1976 is a selenophene analog of DB270 and a highly potent, cell-permeable, fully efficacious transcription factor PU.1 inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 179 Get Quote
5MG 226 Get Quote
10MG 335 Get Quote
25MG 522 Get Quote
50MG 707 Get Quote
100MG 888 Get Quote
200MG 1251 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    DB1976
  • Note
    Research use only, not for human use.
  • Brief Description
    DB1976 is a selenophene analog of DB270 and a highly potent, cell-permeable, fully efficacious transcription factor PU.1 inhibitor.
  • 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.
  • In Vitro
    DB1976 is a classic heterocyclic dication (a single heteroatom) with strong affinity and selectivity for AT-rich sequences commonly found in cognate DNA binding sites for PU.1. DB1976 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.DB1976 treatment leads to a profound decrease in the growth of PU.1 URE–/– AML cells (IC50 of 105 μM), while showing little effect on normal hematopoietic cells at similar concentrations (IC50 of 334 μM). DB1976 treatment leads to a 1.6-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells, and observed similar effects in human MOLM13 cells.DB1976 treatment leads to 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 with vehicle-treated cells. The apoptotic cell fraction increased on average by 1.5-fold with DB1976.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1557397-51-9
  • Formula Weight
    447.35
  • Molecular Formula
    C20H16N8Se
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    C(=N)(N)C=1C=C2NC(=NC2=CC1)C=3[Se]C(=CC3)C=4NC=5C(N4)=CC=C(C(=N)N)C5
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.?
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