产品
编 号：F755434
分子式：C38H42N12O10S2
分子量：890.94
分子式：C38H42N12O10S2
分子量：890.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2756741-90-7
产品详情
生物活性：
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.
体外研究：
CPS2 (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.
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.
体外研究：
CPS2 (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.
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