产品描述:
CPS2 is a proteolysis-targeting chimera (PROTAC) composed of the Cdk2 binder J2, a derivative of the Cdk and Aurora kinase inhibitor JNJ-7706621 (Item No. 18494), connected to the cereblon inhibitor pomalidomide (Item No. 19877) by a linker region.{51687} It selectively degrades Cdk2 (IC50 = 24 nM) over seven additional CDKs at 500 nM but also degrades Aurora A kinase and Ikaros family zinc finger protein 1 (IKZF1) at 250 nM. CPS2 reduces Cdk2 levels and increases the percentage of cells expressing CD11b, a marker of differentiation, in primary acute myeloid lymphoma (AML) cells. It also decreases proliferation without reducing the viability of, as well as induces differentiation in, primary hematopoietic stem cells (HSCs).