Senexin C

• 常用名: Senexin C
• 英文名: Senexin C
• CAS号: 2375554-02-0
• 分子量: 449.558
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₈H₂₇N₅O
• 熔点: N/A
• 闪点: N/A

Senexin C用途

Senexin C是一种新型高效、选择性和口服生物利用度高的CDK8/19抑制剂,其对CDK8/CycC和CDK19/CycC的Kd分别为1.4和2.9 nM。Senexin C抑制CDK8/CycC,IC50为3.6nm,对其他HDAC亚型表现出高选择性。与原型抑制剂Senexin B相比,Senexin C代谢更稳定,对CDK8/19依赖性细胞基因表达的抑制更持久。Senexin C在系统性体内模型中抑制MV4-11白血病生长,耐受性良好。

Senexin C名称

• 英文名: Senexin C

Senexin C生物活性

• 描述: Senexin C是一种新型高效、选择性和口服生物利用度高的CDK8/19抑制剂,其对CDK8/CycC和CDK19/CycC的Kd分别为1.4和2.9 nM。Senexin C抑制CDK8/CycC,IC50为3.6nm,对其他HDAC亚型表现出高选择性。与原型抑制剂Senexin B相比,Senexin C代谢更稳定,对CDK8/19依赖性细胞基因表达的抑制更持久。Senexin C在系统性体内模型中抑制MV4-11白血病生长,耐受性良好。
• 参考文献: 1. Li Zhang, et al. J. Med. Chem. 2022

Senexin C物理化学性质

• 分子式: C₂₈H₂₇N₅O
• 分子量: 449.558
• InChIKey: AFUHWZUYZJGVKM-UHFFFAOYSA-N
• SMILES: CN1CCN(C(=O)c2ccc3cc(CCNc4ccnc5ccc(C#N)cc45)ccc3c2)CC1

Senexin C靶点实验

查看更多实验

实验名称：Inhibition of human ACVR2A assessed as percent of control at 2000 nM by KINOMEscan as... 来源：ChEMBL 靶标：Activin receptor type-2A External Id：CHEMBL4804784

实验名称：Inhibition of human ACVR2B assessed as percent of control at 2000 nM by KINOMEscan as... 来源：ChEMBL 靶标：Activin receptor type-2B External Id：CHEMBL4804785

实验名称：Inhibition of human ACVR1 assessed as percent of control at 2000 nM by KINOMEscan ass... 来源：ChEMBL 靶标：Activin receptor type-1 External Id：CHEMBL4804782

实验名称：Inhibition of human ACVR1B assessed as percent of control at 2000 nM by KINOMEscan as... 来源：ChEMBL 靶标：Activin receptor type-1B External Id：CHEMBL4804783

实验名称：Inhibition of human ADCK4 assessed as percent of control at 2000 nM by KINOMEscan ass... 来源：ChEMBL 靶标：Atypical kinase COQ8B, mitochondrial External Id：CHEMBL4804788

实验名称：Inhibition of human AKT1 assessed as percent of control at 2000 nM by KINOMEscan assa... 来源：ChEMBL 靶标：RAC-alpha serine/threonine-protein kinase External Id：CHEMBL4804789

实验名称：Inhibition of human ACVRL1 assessed as percent of control at 2000 nM by KINOMEscan as... 来源：ChEMBL 靶标：Activin receptor type-1-like External Id：CHEMBL4804786

实验名称：Inhibition of human ADCK3 assessed as percent of control at 2000 nM by KINOMEscan ass... 来源：ChEMBL 靶标：Atypical kinase COQ8A, mitochondrial External Id：CHEMBL4804787

实验名称：Inhibition of phosphorylated human ABL1 T315I mutant assessed as percent of control a... 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL4804776

实验名称：Inhibition of non-phosphorylated human ABL1 T315I mutant assessed as percent of contr... 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL4804777

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