Deferasirox | Iron Chelator

Deferasirox (201530-41-8) is a clinically useful iron chelator used in long term care of ß-thalassemia and other heavily transfused hematological patients.^1,2 It has been shown to potent inhibitor of JumonjiC Domain-Containing Histone Demethylases (IC₅₀’s = KDM4A(JMJD2A) 4.76 µM, KDM5A(JARID1A) 5.00 µM, KDM6B(JMJD3) 3.95 µM).³  Deferasirox has also been investigated as a potential anticancer agent.^4-6

References/Citations:

1. Heinz et al. (1999), 4-[3,5-Bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl]-benzoic acid: A Novel Efficient and Selective Iron(III) Complexing Agent; Ang. Chem. Int. Ed., 38 2568
2. Palumbo et al. (2021), From Biology to Clinical Practice: Iron Chelation Therapy With Deferasirox; Front. Oncol., 11 752192
3. Roatsch et al. (2019), The Clinically Used Iron Chelator Deferasirox Is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases; ACS Chem. Biol., 14 1737
4. Lui et al. (2015), Targeting cancer by binding iron: Dissecting cellular signaling pathways; Oncotarget, 6 18748
5. Ibrahim and O’Sullivan (2020), Iron chelators in cancer therapy; Biometals, 33 201
6. Szymonik et al. (2021), The Impact of Iron Chelators on the Biology of Cancer Stem Cells; Int. J. Mol. Sci., 23 89