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P005091 (P5091) 是一种选择性有效的泛素特异性蛋白酶7(USP7)抑制剂,EC50值为 4.2 μM。
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P005091 (P5091) 是一种选择性有效的泛素特异性蛋白酶7(USP7)抑制剂,EC50值为 4.2 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 247 | 现货 | |
2 mg | ¥ 359 | 现货 | |
5 mg | ¥ 622 | 现货 | |
10 mg | ¥ 898 | 现货 | |
25 mg | ¥ 1,670 | 现货 | |
50 mg | ¥ 2,890 | 现货 | |
100 mg | ¥ 4,330 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 651 | 现货 |
产品描述 | P005091 (P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM. |
靶点活性 | USP7:4.2 μM |
体外活性 | P5091与Lenalidomide,HDAC抑制剂SAHA或Dexamethasone联用显示协同的抗MM活性.在动物肿瘤模型研究中,P005091具有良好的耐受性,抑制肿瘤生长并延长生存期. |
体内活性 | P5091展现出针对USP7的强效,特异性和选择性去泛素化活性。相反,P5091不抑制测试的其他DUBs或其他家族半胱氨酸蛋白酶 (EC50>100 mM)。P5091降低HDM2和HDMX,上调p53和p21水平。总体而言,P5091-诱导的细胞毒性部分是通过HDM2-p21信号轴介导的,尽管P5091处理后p53上调,但P5091的细胞毒性不依赖于p53。P5091浓度依赖性抑制具有HA-UbVME标签的USP7。P5091剂量依赖性抑制USP7介导的超高分子量泛素链的裂解。而且,P5091抑制USP7-而非USP2-或USP8介导的-聚K48连接的泛素链的裂解。P5091抑制MM细胞中USP7去泛素化酶活性,不抑制蛋白酶活性。P5091克服骨髓间充质干细胞诱导的MM细胞生长。 |
激酶实验 | Recombinant enzymes in 20 mM Tris-HCl (pH 8.0), 2 mM CaCl2, and 2 mM β-mercaptoethanol are incubated with dose ranges of P005091 for 30 min in a 96-well plate before the addition of Ub-PLA2 and NBD C6-HPC or Ub-EKL and EKL substrate. The liberation of a fluorescent product within the linear range of the assay is monitored using a Perkin Elmer Envision fluorescence plate reader. Vehicle (2% [v/v] DMSO) and 10 mM N-ethylmaleimide (NEM) are included as controls. |
动物实验 | Animal Models: CB-17 SCID-mice are subcutaneously inoculated with MM.1S, ARP-1, or RPMI-8226 cells in 100 μL of serum free RPMI-1640 medium. Formulation: P005091 is dissolved in 4% NMP(N-methyl-2-Pyrrolidone), 4% Tween-80, and 92% Milli-Q water at a final concentration of 2 mg/mL. |
别名 | P5091 |
分子量 | 348.22 |
分子式 | C12H7Cl2NO3S2 |
CAS No. | 882257-11-6 |
Smiles | CC(=O)c1cc(c(Sc2cccc(Cl)c2Cl)s1)[N+]([O-])=O |
密度 | 1.60 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: 68 mg/mL, Sonication is recommended. |
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