PIK-75 | MedChemExpress (MCE)

PIK-75 产品活性：PIK-75 是一种可逆的 DNA-PK 和 p110α-选择性的抑制剂，抑制 DNA-PK，p110α 和 p110γ，IC50 分别为 2，5.8 和 76 nM。PIK-75 抑制 p110α 效果比抑制 p110β (IC50=1.3 μM) 高 200 多倍。PIK-75 诱导凋亡 (apoptosis)。 产品来源： https://www.medchemexpress.cn/pik-75-1.html 研究领域：Cell Cycle/DNA Damage | PI3K/Akt/mTOR | Apoptosis 作用靶点：DNA-PK | PI3K | Apoptosis In Vitro: PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively. PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively. PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC50 of 78 nM. PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death. PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells. In Vivo: PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice. 相关产品：MG-132 | 3-Methyladenine | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Y-27632 | LY294002 | Paclitaxel | Z-VAD-FMK | Acetylcysteine | Angiotensin II human | 2-Deoxy-D-glucose | Staurosporine | Actinomycin D | SB-431542 | 5-Fluorouracil | Bortezomib | Deferoxamine mesylate | Oxaliplatin | Trametinib | Sorafenib | Temozolomide | Gemcitabine | Decitabine | Mdivi-1 | Rotenone | Etoposide | Elesclomol | Ruxolitinib | Monomethyl auristatin E 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