C527
产品说明书
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同义名 : | - |
| CAS号 : | 192718-06-2 | |
| 货号 : | A280375 | |
| 分子式 : | C17H8FNO3 | |
| 纯度 : | 95% | |
| 分子量 : | 293.25 | |
| MDL号 : | MFCD01033540 | |
| 存储条件： |
Pure form Sealed in dry, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Inhibitor of DNA-binding-1 (ID1) is a transcription factor that belongs to the helix-loop-helix family. High ID1 expression is associated with poor prognosis and high chemoresistance in cancer patients. USP1 is a deubiquitinating (DUB) enzyme that rescues ID1 from proteasome degradation. C527 is a small molecule inhibitor of USP1 with an IC50 value of 0.88 ± 0.03μM. It also inhibited the DUB activity of USP5, UCH-L3, and the USP12/USP46 complex with IC50 values of 1.65±0.42μM, 2.18±0.69μM, and 5.97±0.37μM, respectively. C527 promoted the degradation of ID1 in human U20S osteosarcoma cells in a dose-dependent manner. In Hela cells, treatment with C527 (10–50μM) for 8hr increased the levels of Ub-FANCD2 and Ub-FANCI. Pretreatment of Hela cells with 1μM C527 for 24hr enhanced the cytotoxicity of Mitomycin C and Camptothecin. C527 at 0.5–5μM dose-dependently inhibited DRGFP reporter for homologous recombination repair activity. Pre-incubation of Hela cell with 5μM C527 for 1hr inhibited Camptothecin-induced RAD51 foci formation in Hela cells.[1] | ||
| 作用机制 | C527 is a pan-deubiquitinating enzyme inhibitor that inhibits the catalytic activity of USP1 and other DUB enzymes.[1] | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.41mL 0.68mL 0.34mL |
17.05mL 3.41mL 1.71mL |
34.10mL 6.82mL 3.41mL |
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