2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. Reactive Oxygen Species (ROS) NOD-like Receptor (NLR)
  4. PRDX1-IN-4

PRDX1-IN-4 是一种 PRDX1 抑制剂，针对人源靶点的 IC50 为 122 nM，且具有高亚型选择性。PRDX1-IN-4 可与 PRDX1 共价结合以促进 ROS 积累。PRDX1-IN-4 可抑制 NLRP3 炎症小体激活、阻断肝星状细胞活化并减少胶原沉积。PRDX1-IN-4 可诱导活化肝星状细胞凋亡 (apoptosis)。PRDX1-IN-4 具有良好的安全性，在小鼠中以 20 mg/kg 给药时未出现显著体重下降或肝毒性。PRDX1-IN-4 在小鼠中以 1 mg/kg 给药时可改善 CCl4 诱导的肝损伤和肝纤维化。PRDX1-IN-4 可用于肝纤维化的研究。

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PRDX1-IN-4

PRDX1-IN-4 Chemical Structure

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PRDX1-IN-4 相关抗体

Top Publications Citing Use of Products

查看 NOD-like Receptor (NLR) 亚型特异性产品:

查看所有亚型
NLRP3 NLRP1 NOD1 NOD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRDX1-IN-4 is a PRDX1 inhibitor with an IC50 of 122 nM against human targets and high subtype selectivity. PRDX1-IN-4 covalently binds to PRDX1 to promote ROS accumulation. PRDX1-IN-4 inhibits NLRP3 inflammasome activation, blocks hepatic stellate cell activation and reduces collagen deposition. PRDX1-IN-4 induces apoptosis (apoptosis) in activated hepatic stellate cells. PRDX1-IN-4 has good safety profile, with no significant body weight loss or hepatotoxicity observed in mice at a dose of 20 mg/kg. PRDX1-IN-4 ameliorates CCl4-induced liver injury and liver fibrosis in mice at a dose of 1 mg/kg. PRDX1-IN-4 can be used for the research of liver fibrosis[1].

IC50 & Target

NLRP3

 

体外研究
(In Vitro)

PRDX1-IN-4 (derivative 5) (0.1-2 μM；处理 48 h) 剂量依赖性降低 TGF-β1 诱导的活化 LX-2 细胞中 α-SMA 和 COL1A1 的蛋白表达水平[1]。
PRDX1-IN-4 (0.1-2 μM；48 h) 剂量依赖性升高 TGF-β1 诱导的活化 LX-2 细胞内 ROS 水平，0.1、1、2 μ 浓度下 ROS 阳性率分别达 18.0%、26.4%、34.7%[1]。
PRDX1-IN-4 (0.1-1 μM；48 h) 剂量依赖性上调 TGF-β1 诱导的活化 LX-2 细胞中促凋亡蛋白 Bax、Cyt c 及活化 Caspase-3 的表达，下调抗凋亡蛋白 Bcl-2 及 pro-Caspase-3 的表达[1]。
PRDX1-IN-4 (0.5 μM；6 h) 对 THP-M 细胞活力无显著影响，其 NLRP3 抑制活性并非源于细胞毒性[1]。

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

PRDX1-IN-4 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: THP-1-derived macrophages (induced by 100 ng/mL PMA overnight)
Concentration: 0.5 μM
Incubation Time: 6 h
Result: Showed no significant effect on the viability of THP-M cells, indicating that its NLRP3 inhibitory activity was not attributed to cytotoxicity.

Western Blot Analysis[1]

Cell Line: THP-1-derived macrophages (induced by 100 ng/mL PMA overnight)
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: Pretreated for 0.5 h, then stimulated with 10 μM Nigericin for 1 h, 5 mM ATP for 1 h, or 200 μg/mL MSU for 4 h
Result: Dose-dependently reduced the levels of cleaved caspase-1 p20 and mature IL-1β in the supernatants, and inhibited ASC oligomerization in the pellets. It did not consistently affect the expression of pro-IL-1β, pro-caspase-1, total ASC, or NLRP3 in the cell lysates.
体内研究
(In Vivo)

PRDX1-IN-4 (derivative 5) (20 mg/kg；腹腔注射；单次；14 天观察期) 在野生型 C57BL/6 雄性小鼠急性毒性模型中未导致死亡事件发生，无明显体重下降及心、肝、脾、肺、肾组织病理损伤，血清 ALT、AST 及红细胞计数无异常，安全性显著优于同剂量雷公藤红素[1]。
PRDX1-IN-4 (1 mg/kg；腹腔注射；每日 1 次；连续 4 周，从造模第 3 周开始) 在 CCl4 诱导的 C57BL/6 雄性小鼠肝纤维化模型中， 显著改善 CCl4 诱导的肝损伤与纤维化，降低肝/体重比及血清 ALT、AST 水平，减少胶原纤维沉积，下调肝组织中 α-SMA、COL1A1 的表达，抑制 NLRP3 炎症小体活化，且无小鼠死亡，安全性优于同剂量雷公藤红素[1]。

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

Animal Model: Male C57BL/6 mice, housed under SPF conditions, acclimatized for 1 week; hepatic fibrosis model established by intraperitoneal injection of CCl4 (1 mL/kg, diluted 1:8 in corn oil) twice weekly for 6 consecutive weeks[1]
Dosage: 1 mg/kg
Administration: intraperitoneal injection once daily for 4 weeks
Result: Significantly normalized the liver/body weight ratio and reduced the serum levels of ALT and AST, indicating improved liver function. H&E staining showed that derivative 5 alleviated CCl4-induced hemorrhagic necrosis and inflammatory cell infiltration in the liver.
Markedly reduced collagen fiber deposition in the fibrotic liver.
Downregulated the protein expression of α-SMA and COL1A1, and decreased the levels of IL-1β and cleaved caspase-1 without altering the total expression of NLRP3.
分子量

629.62

Formula

C33H45BrN2O5
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

PRDX1-IN-4 相关分类

  • 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.

Keywords:

PRDX1-IN-4Reactive Oxygen Species (ROS)NOD-like Receptor (NLR)hepatotoxicitymiceapoptosishepatic fibrosishepatic stellate cellcollagen depositionNLRP3 inflammasomePRDX1ROSCCl4-induced hepatic damageInhibitorinhibitorinhibit

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