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

PRDX1-IN-2 Chemical Structure

CAS No. : 2566976-43-8

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规格 价格 是否有货 数量
5 mg ¥5264
4 -6 周
10 mg 询价 4 -6 周
25 mg 询价 4 -6 周
50 mg 询价 4 -6 周
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Customer Review

  • 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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
0.44 μM
Compound: 15
Inhibition of cell viability in human HCT-116 cells incubated for 72 hrs by Cell Titer Glo assay
Inhibition of cell viability in human HCT-116 cells incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38679872]
HEK-293T IC50
~ 1 μM
Compound: 15
Antiproliferative activity against HEK293T cells
Antiproliferative activity against HEK293T cells
[PMID: 38679872]
LX-2 IC50
~ 1 μM
Compound: 15
Antiproliferative activity against human LX2 cells
Antiproliferative activity against human LX2 cells
[PMID: 38679872]
SW-620 IC50
0.32 μM
Compound: 15
Inhibition of cell viability in human SW620 cells incubated for 72 hrs by Cell Titer Glo assay
Inhibition of cell viability in human SW620 cells incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38679872]
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
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  • 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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产品名称:
PRDX1-IN-2
目录号:
HY-158368
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