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NVP-DKY709 is a degrader of Ikaros family zinc finger protein 2 (IKZF2) with a half-maximal degradation concentration (DC50) value of 4 nM.1 It is selective for IKZF2 over 8,656 other proteins, including IKZF1, IKZF3, and IKZF5, at 2.5 µM, but it does degrade IKZF4, which has the same zinc finger 2 β-hairpin sequence as IKZF2, and Sal-like protein 4 (SALL4; DC50s = 13 and 2 nM, respectively). It increases IL-2 secretion induced by phytohemagglutinin in Jurkat T cells in a concentration-dependent manner. NVP-DKY709 (100 mg/kg), alone or in combination with an antibody against programmed death protein 1 (PD-1), decreases tumor volume in an MDA-MB-231 humanized mouse xenograft model.
WARNING This product is not for human or veterinary use.
1. Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy. Cell Chem. Biol. 30(3), 235-247.e212 (2023).