2. Epigenetics
  3. Protein Arginine Deiminase
  4. PAD4-IN-4

PAD4-IN-4 (compound 28) 是一种有效的 PAD4 抑制剂 (IC50=0.79±0.09 μM)。 PAD4-IN-4 通过重塑中性粒细胞表型，上调树突状细胞和 M1 巨噬细胞的比例，减少髓源性抑制细胞的数量，改善肿瘤免疫微环境。PAD4-IN-4 可用于三阴性乳腺癌的研究。

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PAD4-IN-4 Chemical Structure

PAD4-IN-4 Chemical Structure

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PAD4-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research[1].

IC50 & Target[1]

PAD4

0.79 μM (IC50)

PAD2

2.97 μM (IC50)

体外研究
(In Vitro)

PAD4-IN-4 对 PAD2 和 PAD4 表现出了较强的抑制活性 (IC50=2.97±0.29 μM 和 0.79±0.09 μM)，对 PAD4 的选择性最高 (3.8 μM)[1]。
PAD4-IN-4 显著抑制 TNBC 细胞体外增殖 (4T1 IC50:2.39±0.54 μM；MDA-MB468 IC50: 2.34±0.23 μM)，对正常乳腺细胞的毒性相对较低(MCF-10A IC50: 8.39±0.60 μM)[1]。
PAD4-IN-4 (0.5，1，2 μM；48 h) 具有增强的抗转移活性对于 TNBC 细胞[1]。
PAD4-IN-4 (0.5，1，2 μM；48 h) 是一种有效的 PAD4 抑制剂，可以阻断组蛋白瓜氨酸化和中性粒细胞胞外陷阱 (NET) 的形成[1]。

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

PAD4-IN-4 相关抗体:

Cell Proliferation Assay[1]

Cell Line: TNBC cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Reduced the number of metastatic cells and wound closure rate less than that of 7 at the equivalent dose, indicating that compound 28 had enhanced antimetastasis activity.

Immunofluorescence[1]

Cell Line: TNBC cells and neutrophils
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Inhibited histone citrullination and NET formation.
体内研究
(In Vivo)

PAD4-IN-4 (1，5，10 mg/kg；iv.；2 天 1 次共 9 次) 可以剂量依赖性地抑制 TNBC 肺转移，是抗 TNBC 的高活性化合物，且无明显毒性在原位 4T1-luc 异种移植模型 的 BALB/c 小鼠中[1]。
PAD4-IN-4 通过调节免疫细胞的比例和重塑中性粒细胞的表型和功能，将肿瘤微环境从抑制状态改变为抗肿瘤环境[1]。
Pharmacokinetic Analysis in Male Sprague−Dawley rats[1]

Compound Route Dose (mg/kg) AUC0_t (ng•h/mL) AUC0_INF (ng•h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) Cl (L•h/kg)
7 i.v. 3.5 14893.52 17214.17 0.13 0.08 251.2 571.87
28 i.v. 3.5 9525.86 17346.55 0.25 0.08 297.71 105.24

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

Animal Model: orthotopic 4T1-luc xenograft model in BALB/c mice[1].
Dosage: 1, 5, 10 mg/kg
Administration: Intravenous injection (i.v.)
Result: The tumor growth inhibition of the high-dose 28-treated group was 61.8%, whereas the positive control doxorubicin hydrochloride group reached 54.6%.
Had no significant differences in viscero−somatic ratio and serum biochemical indices (ALT, AST, UREA, and CREA-S) were observed in the 28-treated group.
Increased the proportion of mature TANs MHC-II+ TANs whereas it suppressed the proportion of pro-tumor phenotypes PD-L1+ /MHC-II+ TANs and MHC-II− TANs.
分子量

567.08

Formula

C32H31ClN6O2
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

PAD4-IN-4 相关分类

  • 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)

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The dilution calculator equation

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

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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.

Keywords:

PAD4-IN-4Protein Arginine DeiminasePeptidylarginine DeiminasePAD4 InhibitorTriple-negative breast cancerTNBC cellsorthotopic 4T1-luc xenograft modelInhibitorinhibitorinhibit

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