1. Epigenetics
  2. Protein Arginine Deiminase
  3. PADI4-IN-1

PADI4-IN-1 是一种强效的肽基精氨酸脱亚胺酶 4 (PADI4) 抑制剂,其 IC50 值为 1.5 μM,选择性指数 (SI) (PADI1/PADI4) 为 52.1。PADI4-IN-1 能够抑制细胞瓜氨酸化事件。PADI4-IN-1 可用于炎症相关研究,如类风湿性关节炎。

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PADI4-IN-1

PADI4-IN-1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PADI4-IN-1 is a potent peptidylarginine deiminase isoform 4 (PADI4) inhibitor with an IC50 of 1.5 μM and SI (PADI1/PADI4) of 52.1. PADI4-IN-1 can inhibit cellular citrullination events. PADI4-IN-1 can be used for the research of inflammation, such as rheumatoid arthritis[1].

IC50 & Target[1]

PADI4

1.5 μM (IC50)

体外研究
(In Vitro)

PADI4-IN-1 (Compound 7) (10-100 μM, 50 mins) 会减少 HL-60 细胞裂解物中由 PADI4 介导的总细胞瓜氨酸化事件以及组蛋白 H3 的瓜氨酸化[1]

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

Western Blot Analysis[1]

Cell Line: HL-60 cells
Concentration: 10 and 100 μM
Incubation Time: 50 mins
Result: Decreased total HL-60 cellular citrullination events and histone H3 citrullination mediated by PADI4.
体内研究
(In Vivo)

PADI4-IN-1 (Compound 7) (20 mg/kg,腹腔注射,在第 3、4、5、6 和 7 天给药) 可减轻 II 型胶原蛋白抗体/LPS (HY-D1056) 诱导的类风湿性关节炎小鼠模型的病情严重程度和病理进展[1]

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

Animal Model: Collagen type II antibody/LPS (HY-D1056) induced rheumatoid arthritis mice models[1]
Dosage: 20 mg/kg
Administration: Intraperitoneally injection
Result: Decreased the arthritis score of the mice by 66 % treated at days 4, 5, 6, and 7.
Decreased the arthritis score of the mice by 100 % treated at days 3 and 4.
Reduced the expression of IL-6, IL-1β, IFN-γ, RANKL, IL-17A, CXCL15, ANXA2, HIF-1α, iNOS, and TNF-αtreated at days 3 and 4.
Reduced inflammatory cell influx, pannus formation, cartilage destruction, cartilage remnant, edema, and accumulation of inflammatory cells (mononuclear cells and neutrophil).
Reduced the erosion of cartilage and bone.
Reduced the levels of citrullinated antigens.
分子量

337.41

Formula

C21H23NO3

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

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
PADI4-IN-1
目录号:
HY-175518
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