PAD4-IN-4

PAD4-IN-4 产品活性：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。 产品来源： www.medchemexpress.cn/pad4-in-4.html 研究领域：Epigenetics 作用靶点：Protein Arginine Deiminase In Vitro: PAD4-IN-4 displays substantial inhibitory activity toward PAD2 and PAD4 (IC50=2.97 ± 0.29 and 0.79 ± 0.09 μM), with the best PAD4 selectivity. PAD4-IN-4 suppresses the proliferation of TNBC cells in vitro (4T1 IC50: 2.39 ± 0.54 μM; MDA-MB468 IC50: 2.34 ± 0.23 μM), with relatively low toxicity toward normal breast cells (MCF-10A IC50: 8.39 ± 0.60 μM). PAD4-IN-4 (0.5, 1, 2 μM; 48 h) has enhanced antimetastasis activity for TNBC cells. PAD4-IN-4 (0.5, 1, 2 μM; 48 h) is a potent PAD4 inhibitor for blocking histone citrullination and neutrophil extracellular trap (NET) formation. In Vivo: PAD4-IN-4 (1, 5, 10 mg/kg; i.v.; every 2 days for a total of nine times) can dosedependently suppress the lung metastasis of TNBC. PAD4-IN-4 is a promising candidate against TNBC without obvious toxicity in orthotopic 4T1-luc xenograft model in BALB/c mice. PAD4-IN-4 alters the tumor microenvironment from a suppressive condition to an antitumor milieu by modulating the proportion of immune cells and reshaping the neutrophil phenotype and function. Pharmacokinetic Analysis in Male Sprague−Dawley rats 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 相关产品：GSK484 hydrochloride | Cl-amidine hydrochloride | BB-Cl-Amidine hydrochloride | AFM-30a hydrochloride | AFM32a hydrochloride | BMS-P5 free base | GSK199 | Acefylline | PAD-IN-2 | Streptonigrin | JBI-589 | GSK121 | GSK106 | PAD4-IN-2 TFA | F-Amidine TFA | GSK199 analog hydrochloride | KP-302 | PAD4-IN-3 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种TOP期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。