In vitro activity: UM729 expands normal hematopoietic stem and progenitor cells (HSPCs) in an AhR-independent manner. UM729 prevents the AML cell differentiation. In cultured 05H163 cells, compared with AhR suppressors (flavonoid, benzothiophene, and β-carboline) alone, addition of UM729 improves the numbers of CD34+CD15- cells. UM729 has an additive effect with AhR antagonists in preventing differentiation in most AML specimens.

Cell Assay: CellTrace Violet is added at a final concentration of 3 μM to cell suspensions (107 cells/mL) containing SR1 (500 nM), UM729 (1 μM), both compounds or vehicle (0.1% DMSO). CellTrace Violet–labeled cells are stained with surface antibodies to human CD3, CD19, CD34 and CD33 on day 0, day 2 and day 4 before analysis on a flow cytometry.

Nat Methods. 2014 Apr;11(4):436-42.