Halofuginone 产品活性：Halofuginone (RU-19110)，Febrifugine 的衍生物，是一种竞争性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制剂，Ki 为 18.3 nM。Halofuginone 是 I 型胶原 (type-I collagen) 合成的特异性抑制剂，并通过抑制 TGF-β 活性可减轻骨关节炎。Halofuginone 也是一种有效的肺血管扩张剂，可激活 Kv 通道并阻断电压门控、受体操作和存储操作的 Ca2+ channels 通道。Halofuginone 具有抗疟疾、抗炎、抗癌、抗纤维化作用。 产品来源： https://www.medchemexpress.cn/Halofuginone.html 研究领域：Cell Cycle/DNA Damage | TGF-beta/Smad | Stem Cell/Wnt | Anti-infection | Membrane Transporter/Ion Channel | Neuronal Signaling 作用靶点：DNA/RNA Synthesis | TGF-beta/Smad | Parasite | Sodium Channel | Calcium Channel 来源：植物 | 虎耳草科 | 常山 结构分类：生物碱 | 哌啶类生物碱 | 结构分类 In Vitro: Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase. The IC50s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively. The IC50s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively. Halofuginone increases voltage-gated K+ (Kv) currents in pulmonary artery smooth muscle cells (PASMC) and K+ currents through KCNA5 channels in HEK cells transfected with KCNA5 gene. Halofuginone (0.03-1μM) inhibits receptor-operated Ca2+ entry (ROCE) in HEK cells transfected with calcium-sensing receptor gene and attenuates store-operated Ca2+ entry (SOCE) in PASMC. In Vivo: Halofuginone (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage. Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone. Intraperitoneal administration of Halofuginone? (0.3mg/kg, for 2 weeks) partially reverses the established pulmonary hypertension in mice. 相关产品：Natural Product Library Plus | Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Anti-Infection Compound Library | Cell Cycle/DNA Damage Compound Library | Immunology/Inflammation Compound Library | Membrane Transporter/Ion Channel Compound Library | Neuronal Signaling Compound Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Wnt/Hedgehog/Notch Compound Library | Natural Product Library | Anti-Cancer Compound Library | Clinical Compound Library | Peptidomimetic Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cardiovascular Disease Compound Library | Anti-COVID-19 Compound Library | FDA Approved & Pharmacopeial Drug Library | Neuroprotective Compound Library | Alkaloids Library | Antiparasitic Compound library | Angiogenesis-Related Compound Library | Transcription Factor-Targeted Library | Mechanoreceptors Compound Library | Rare Diseases Drug Library | Anti-Colorectal Cancer Compound Library | Anti-Cancer Natural Product Library | Plant-Sourced Natural Product Library | Calcium Channel Blocker Library | Human Metabolite Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Osteogenesis Compound Library | Cancer Stem Cells Compound Library | Coagulation and Anti-coagulation Compound Library | Heterocyclic Compound Library | Antihypertensive Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | Ion Channel Compound Library | Multi-Target Compound Library | Bioactive Compound Library Max | Anti-Fibrosis Compound Library | Cycloheximide | Chloroquine | Puromycin dihydrochloride | Actinomycin D | Oxaliplatin | Gemcitabine | Thapsigargin | Bleomycin sulfate | Carboplatin | Ionomycin | Hygromycin B | Mitomycin C | L-Ascorbic acid | Cytarabine | Doxycycline hyclate | 5-BrdU | Methotrexate | Streptozotocin | Acetaminophen | Anisomycin | Fludarabine | Pirfenidone | ART558 | Propidium Iodide | Metronidazole | Thymidine | Minocycline hydrochloride 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最新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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。