VAF347

VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14+CD11b+ monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects[1].

Signaling Pathways >> Immunology/Inflammation >> Aryl Hydrocarbon Receptor

Research Areas >> Inflammation/Immunology

Aryl hydrocarbon receptor[1]

VAF347 (0.01-20 μM; 48-72 hours; HL-60 cells) treatment enhances retinoic acid-induced cell cycle arrest[1]. VAF347 (20 μM; 48 hours; HL-60 cells) treatment augments retinoic acid-induced expression of AhR, Lyn, Vav1, and c-Cbl as well as p47phox. Several interactions of partners in the signalsome appear to be enhanced: Fgr interaction with c-Cbl, CD38, and with pS259c-Raf and AhR interaction with c-Cbl and Lyn[1]. Cell Cycle Analysis[1] Cell Line: HL-60 cells Concentration: 10 nM, 100 nM, 1 μM, 10 μM, 20 μM Incubation Time: 48 hours or 72 hours Result: Enhanced retinoic acid-induced cell cycle arrest in G1/0. Western Blot Analysis[1] Cell Line: HL-60 cells Concentration: 20 μM Incubation Time: 48 hours Result: Augmented retinoic acid-induced expression of AhR, Lyn, Vav1, and c-Cbl as well as p47phox.

[1]. Ibabao CN, et al. The AhR agonist VAF347 augments retinoic acid-induced differentiation in leukemia cells. FEBS Open Bio. 2015 Apr 8;5:308-18.