| Bioactivity | PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction。PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice[1]. |
| Invitro | PRL-295 在表达 Keap1-mCherry 的 U2OS 细胞裂解液 (15 μM, 1 h)、HL-60 细胞裂解液 (30 μM, 1 h) 和 HL-60 细胞 (10 μM, 3 h) 中增加 Keap1 的热稳定性[1]。PRL-295 (50 μM, 1 h) 可破坏共表达 sfGFP-Nrf2 和 Keap1-mCherry 的单个 HeLa 细胞中的 Keap1-Nrf2 蛋白复合物[1]。PRL-295 (大约 60 nM-10 μM, 48 h) 浓度依赖性地诱导 Hepa1c1c7 和 ARPE-19 细胞中的 Nrf2 靶标NAD(P)H:quinone oxidoreductase 1 (NQO1)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PRL-295 相关抗体: |
| In Vivo | PRL-295 (10-50 mg/kg，口服，4 次，每次间隔 24 h) 剂量依赖性地增加小鼠肝脏中 Keap1 的热稳定性并激活 Nrf2 转录靶标 NQO1[1]。PRL-295 (25 mg/kg，口服，3 天) 对 Acetaminophen (HY-66005) 诱发的 C57/BL6 小鼠肝损伤起保护作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 2377770-85-7 |
| Formula | C27H24F3N3O8S2 |
| Molar Mass | 639.62 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Dayalan Naidu S, et al. The isoquinoline PRL-295 increases the thermostability of Keap1 and disrupts its interaction with Nrf2. iScience. 2021 Dec 27, 25(1):103703. |
PRL-295
CAS: 2377770-85-7 F: C27H24F3N3O8S2 W: 639.62
PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction。PRL-295 increases the thermal stability of Keap1
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