CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader ( IC 50 = 24 nM). CPS2 can be used for the research of acute myeloid leukemiaIn VitroCPS2 (5~333 nM; 12 hours; Ramos cells) stands out as the most potent degrader. 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. The antileukemic effects of CPS2 are mediated by CDK2 degradation. CPS2 also induces granulocytic differentiation of HSCs, as assessed by cell morphological analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Ramos cells Concentration: 5~333 nM Incubation Time: 12 hours Result: Stood out as the most potent degrader.Form:SolidIC50& Target:CDK2 24 nM (IC 50 ).
Specifications and Purity: ≥99%
Molecular Formula: C38H42N12O10S2
Molecular Weight: 890.94
- UPC:
- 42261902
- Condition:
- New
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- C646566-5mg
- CAS:
- 2756741-90-7
- Product Size:
- 5mg
akash.verma@cenmed.com
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