KZR-616

• 常用名: KZR-616
• 英文名: KZR-616
• CAS号: 1629677-75-3
• 分子量: 586.686
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₀H₄₂N₄O₈
• 熔点: N/A
• 闪点: N/A

KZR-616用途

KZR-616(KZR616)是一种有效的选择性双重免疫蛋白酶体亚基LMP7/LMP2抑制剂,IC50为39 nM/139 nM,弱抑制β5,MECL-1,对β1亚基无活性；10 uM时无抑制作用广泛选择性小组的20种丝氨酸,金属-,半胱氨酸和天冬氨酰蛋白酶以及11种水解酶；在抗胶原抗体诱导的关节炎(CAIA)模型。其他适应症2期临床

KZR-616名称

• 英文名: KZR-616

KZR-616生物活性

• 描述: KZR-616(KZR616)是一种有效的选择性双重免疫蛋白酶体亚基LMP7/LMP2抑制剂,IC50为39 nM/139 nM,弱抑制β5,MECL-1,对β1亚基无活性；10 uM时无抑制作用广泛选择性小组的20种丝氨酸,金属-,半胱氨酸和天冬氨酰蛋白酶以及11种水解酶；在抗胶原抗体诱导的关节炎(CAIA)模型。其他适应症2期临床
• 参考文献: References 1. Johnson HWB, et al. J Med Chem. 2018 Oct 31. doi: 10.1021/acs.jmedchem.8b01201. View Related Products by Target Proteasome Other Indication

KZR-616物理化学性质

• 分子式: C₃₀H₄₂N₄O₈
• 分子量: 586.686
• InChIKey: GHYOCDFICYLMRF-UTIIJYGPSA-N
• SMILES: COc1ccc(C(O)C(NC(=O)C(C)NC(=O)CN2CCOCC2)C(=O)NC(CC2=CCCC2)C(=O)C2(C)CO2)cc1

KZR-616靶点实验

查看更多实验

实验名称：Selectivity index, ratio of IC50 for 20S proteasome beta 1c (unknown origin) to IC50 ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4403377

实验名称：Selectivity index, ratio of IC50 for 20S proteasome beta 2c (unknown origin) to IC50 ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4403378

实验名称：Selectivity index, ratio of IC50 for 20S proteasome beta 5c (unknown origin) to IC50 ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4403379

实验名称：Antiinflammatory activity in human PBMC assessed as reduction in LPS-stimulated TNF-a... 来源：ChEMBL 靶标：PBMC External Id：CHEMBL4411766

实验名称：Antiinflammatory activity in human PBMC assessed as reduction in LPS-stimulated IL-6 ... 来源：ChEMBL 靶标：PBMC External Id：CHEMBL4411767

实验名称：Antiinflammatory activity in human PBMC assessed as reduction in LPS-stimulated p40 s... 来源：ChEMBL 靶标：PBMC External Id：CHEMBL4411768

实验名称：Antiinflammatory activity in human PBMC assessed as reduction in anti-CD3/CD28 antibo... 来源：ChEMBL 靶标：PBMC External Id：CHEMBL4411769

实验名称：Antiinflammatory activity in human PBMC assessed as reduction in anti-CD3/CD28 antibo... 来源：ChEMBL 靶标：PBMC External Id：CHEMBL4411770

实验名称：Inhibition of MECL1 in mouse A20 cells by ELISA 来源：ChEMBL 靶标：Proteasome subunit beta type-10 External Id：CHEMBL4411757

实验名称：Inhibition of 20S proteosome beta 2 in mouse A20 cells by ELISA 来源：ChEMBL 靶标：Proteasome subunit beta type-2 External Id：CHEMBL4411758

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