CPS2 

CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC₅₀= 24 nM). CPS2 can be used for the research of acute myeloid leukemia^[1].

CPS2 (5~333 nM; 12?hours; Ramos cells) stands out as the most potent degrader^[1].
CPS2 (0.5~2 μM; HSCs) inhibits the proliferation of HSCs without inducing cytotoxicity. CPS2 (1~10000 nM; 48?hours; NB4 cells) induces potent CDK2 degradation. CPS2 (250 nM; 0~6 hours; Ramos and NB4 cells) rapidly induces the degradation of CDK2. CPS2 (10~500 nM; 6 hours; Ramos cells) induces only CDK2 degradation and does not directly perturb the other CDK proteins under subnanomolar concentration conditions. CPS2 (250 nM; 6 hours; NB4 cells) stands out as the most downregulated protein in cells treated for 6 hours with CPS2, confirming the selectivity of CPS2 for CDK2. CPS2 (0~250 nM; NB4 cells) makes the levels of CDK2 obviously decreased. CPS2 (2 μM; 3?days; HL60 cells) obviously promotes ATRA-induced CD11b upregulation^[1].
The antileukemic effects of CPS2 are mediated by CDK2 degradation. CPS2 also induces granulocytic differentiation of HSCs, as assessed by cell morphological analysis^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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• [1]. Wang L, et al. Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy. Nat Chem Biol. 2021;17(5):567-575  [Content Brief]