PFK-015 | MedChemExpress (MCE)

PFK-015 产品活性：PFK-015，3PO 的衍生物，是一种特异性的 PFKFB3 抑制剂。PFK-015 可以抑制重组 PFKFB3，其 IC50 值为 110 nM，抑制癌细胞中 PFKFB3 活性，其 IC50 值为 20 nM。PFK-015 可用于肺、胃、结肠腺癌和食管鳞状细胞癌 (ESCC) 等多种癌症的研究。 产品来源： https://www.medchemexpress.cn/PFK-015.html 研究领域：Autophagy 作用靶点：Autophagy In Vitro: PFK-015 inhibits tumor growth in a dose-dependent manner in esophageal cancer cell line in vitro. PFK-015 (0-5 μM) increases HIF-1α mediated PD-L1 transcriptional activity. PFK-015 induces the expression of tumor PD-L1 via the phos-PFKFB3/HIF-1a axis. PFK-015 potently inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM. PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines and suppresses glucose uptake in cancer cells. In Vivo: PFK-015 impeds ESCC tumor growth in immunodeficient in vivo models. PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression. PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 + T cells. PFK-015 enhances the efficacy of ESCC by enhancing CD8 + T-cell activity combining PD-1 mAb in immunocompetent mouse models such as C57BL/6 and hu-PBMC-NOG. PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance. 相关产品：Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Lung Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Colorectal Cancer Compound Library | Heterocyclic Compound Library | Metabolic Enzyme Compound Library | Highly Selective Inhibitors Library | Cell Death Library | Bioactive Compound Library Max | MG-132 | Rapamycin | 3-Methyladenine | Cisplatin | Cycloheximide | Chloroquine | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Olaparib | LY294002 | Paclitaxel | Dexamethasone | Laduviglusib | Forskolin | Actinomycin D | Venetoclax | Bortezomib | Deferoxamine mesylate | Trametinib | Sorafenib | Dorsomorphin | Necrostatin-1 | Retinoic acid | Temozolomide | Gemcitabine | Mdivi-1 | Rotenone | Etoposide | Adezmapimod 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。

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途