2. NF-κB Metabolic Enzyme/Protease
  3. Keap1-Nrf2 Endogenous Metabolite
  4. PRL-295

PRL-295 是一种针对 Keap1-Nrf2 相互作用的口服活性抑制剂。PRL-295 提高 Keap1 的热稳定性并破坏其与 Nrf2 的相互作用，从而激活 Nrf2 依赖的转录靶标 NAD(P)H：醌氧化还原酶 1 (NQO1)。PRL-295 保护 Acetaminophen (HY-66005) 诱发的小鼠肝损伤。

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PRL-295 Chemical Structure

PRL-295 Chemical Structure

CAS No. : 2377770-85-7

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PRL-295 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

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.

PRL-295 相关抗体:
体内研究
(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: 8-week-old male C57/BL6 mice were intraperitoneally Acetaminophen (HY-66005) (300 mg/kg)[1]
Dosage: 25 mg/kg
Administration: Oral gavage (p.o.); once a day, over a period of 3 days
Result: Reduced plasma levels of alanine aminotransferase and glutamine aminotransferase.
Animal Model: Male C57BL/6 wild-type mice[1]
Dosage: 10, 25, 50 mg/kg
Administration: Oral gavage (p.o.); 4 times, 24 h apart
Result: Increased hepatic NQO1 mRNA 2.2-fold or 2.8-fold in a dose-dependent manner at 10 mg/kg or 25 mg/kg, respectively.
Increased NQO1 mRNA moderately (1.5-fold) in kidneys at a dose of 25 mg/kg.
Did not significantly increase mRNA levels of NQO1 in the brain, colon, or lung.
分子量

639.62

Formula

C27H24F3N3O8S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PRL-295 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PRL-2952377770-85-7PRL295PRL 295Keap1-Nrf2Endogenous MetaboliteThermostabilityU2OSHeLaHL-60HepatotoxicityC57BL/6JInhibitorinhibitorinhibit

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