DB1976

SKU: orb1709925

Description

DB1976 is a potent, cell-permeable selenophene analog that acts as a fully efficacious PU.1 transcription factor inhibitor. It demonstrates high-affinity binding (KD ~12 nM) to disrupt PU.1/DNA complexes in vitro and induces apoptosis, supporting its research use in hematological studies and cancer research.

Research Area

Cell Biology

Key Properties

• CAS Number: 1557397-51-9
• MW: 447.35
• Purity: 98.94% (May vary between batches)
• Formula: C₂₀H₁₆N₈Se
• SMILES: C(=N)(N)C=1C=C2NC(=NC2=CC1)C=3[Se]C(=CC3)C=4NC=5C(N4)=CC=C(C(=N)N)C5
• Target: Apoptosis
• Solubility: DMSO:50 mg/mL (111.77 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target 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.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DB1976, DB-1976, DB 1976

Compound Identifiers

PubChem CID

141655595