APTO-253 (LOR-253) hydrochloride is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels.
APTO-253 is converted intracellularly from a monomer to a ferrous complex [Fe(253)3].
APTO-253 selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells without producing myelosuppression in various animal species and humans, induces DNA Damage in AML cells.
