1. Apoptosis Protein Tyrosine Kinase/RTK
  2. Apoptosis ROS Kinase
  3. PRDX1-IN-2

PRDX1-IN-2 (compound 15) 是抗氧化酶过氧化物还蛋白 1 (PRDX1) 的选择性抑制剂 (IC50=0.35 μM)。PRDX1-IN-2 降低 SW620 细胞线粒体膜电位,可能是由于 PRDX1 抑制引起的 ROS增加,导致细胞凋亡。PRDX1-IN-2 可用于结直肠癌研究。

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PRDX1-IN-2 Chemical Structure

PRDX1-IN-2 Chemical Structure

CAS No. : 2566976-43-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) (IC50=0.35 μM). PRDX1-IN-2 decreases the mitochondria membrane potential of SW620 cells, probably due to ROS induced by PRDX1 inhibition, leading to cell apoptosis. PRDX1-IN-2 can be used for colorectal cancer research[1].

IC50 & Target

PRDX1

0.35 μM (IC50)

体外研究
(In Vitro)

PRDX1-IN-2 (0.5-2 μM, 48 h) 使细胞中 ROS 水平呈剂量依赖性升高[1]
PRDX1-IN-2 可诱导线粒体膜去极化, 降低线粒体膜电位, 最终导致线粒体功能障碍[1]
PRDX1-IN-2 (0.5, 1, 2 μM; 48 h) 诱导结肠癌细胞凋亡和 G2/M 细胞周期阻滞, 可能与其抗增殖活性有关[1]
PRDX1-IN-2 (0.25-2 μM; 48 h)通过调节与线粒体功能障碍相关的促凋亡或抗凋亡标记蛋白诱导 SW620 凋亡,最终导致抗增殖表型[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: SW620 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Led to the accumulation of SW620 cells at the G2/M phase with percentages of 7.1−17.4%.

Western Blot Analysis[1]

Cell Line: SW620 cells
Concentration: 0.25-2 μM
Incubation Time: 48 h
Result: Increased the expression of Cyt C, down-regulated the expression of anti-apoptotic proteins Bcl-2 and Bcl-xL, and accumulated the DNA damage marker γ-h2ax in a dose-dependent manner.
体内研究
(In Vivo)

PRDX1-IN-2 (20 mg/kg,ip.;每天一次持续 14 天) 具有比天然产物雷公藤红素 (HY-13067) 更高的安全性,可能是由于在 C57BL/314 6J 小鼠中对 PRDX1 的选择抑制活性[1]
PRDX1-IN-2 (2 mg/kg,ig.;每天一次持续 16 天) 通过诱导细胞凋亡成功抑制肿瘤生长,并且耐受性良好在结直肠癌细胞异种移植模型中[1]
药代动力学分析在 C57BL/314 6J 小鼠体内[1]

Route Dose (mg/kg) AUC0_t (ng•h/mL) AUC0_INF (ng•h/mL) T1/2 (h) Cmax (ng/mL) Cl (L•h/kg) V2(mL/kg)
i.v. 2 364 403 8.46 203 4986 60699

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/314 6J mice
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Observed no death or noticeable drop in body weight and no significant pathohistological differences were observed in these key organ tissues.
Animal Model: colorectal cancer cell xenograft model in the BALB/c nude mice
Dosage: 2 mg/kg
Administration: i.g.
Result: Suppressed the tumor volume and weight with the tumor growth inhibition rate (TGI) of 45.4%, which was superior to the group treated with celastrol (TGI = 28.0%).
分子量

576.77

Formula

C35H48N2O5

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
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

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PRDX1-IN-2
目录号:
HY-158368
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