CPS2 is a first-in-class, highly potent, selective and irreversiblePROTACCDK2degrader (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].

890.94

C₃₈H₄₂N₁₂O₁₀S₂

2756741-90-7

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