| Bioactivity | 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]. |
| Invitro | 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. 0 --> PAD4-IN-4 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| 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 |
| Formula | C32H31ClN6O2 |
| Molar Mass | 567.08 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhu D, et al. A β-Carboline Derivate PAD4 Inhibitor Reshapes Neutrophil Phenotype and Improves the Tumor Immune Microenvironment against Triple-Negative Breast Cancer[J]. Journal of Medicinal Chemistry, 2024. |