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.

Product information

CAS Number: 1557397-51-9

Molecular Weight: 447.35

Formula: C20H16N8Se

Chemical Name: 2-[5-(6-carbamimidoyl-1H-1,3-benzodiazol-2-yl)selenophen-2-yl]-1H-1,3-benzodiazole-6-carboximidamide

Smiles: NC(=N)C1C=C2NC(=NC2=CC=1)C1=CC=C([Se]1)C1NC2C=C(C=CC=2N=1)C(N)=N

InChiKey: NXECULIQZLOKFU-UHFFFAOYSA-N

InChi: InChI=1S/C20H16N8Se/c21-17(22)9-1-3-11-13(7-9)27-19(25-11)15-5-6-16(29-15)20-26-12-4-2-10(18(23)24)8-14(12)28-20/h1-8H,(H3,21,22)(H3,23,24)(H,25,27)(H,26,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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