Prexasertib dihydrochloride 产品活性：Prexasertib dihydrochloride (LY2606368 dihydrochloride) 是一种选择性的，ATP 竞争性的第二代细胞周期检测点激酶 1 (CHK1) 抑制剂，Ki 为 0.9 nM，IC50 为 50=8 nM) 和 RSK1 (IC50=9 nM)。Prexasertib dihydrochloride 引起双链 DNA 断裂和复制突变，导致细胞凋亡 (apoptosis)。Prexasertib dihydrochloride 显示有效的抗肿瘤活性。 产品来源： https://www.medchemexpress.cn/LY2606368-dihydrochloride.html 研究领域：Cell Cycle/DNA Damage | Apoptosis 作用靶点：Checkpoint Kinase (Chk) | Apoptosis In Vitro: Prexasertib dihydrochloride (LY2606368 dihydrochloride) inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). LY2606368 requires CDC25A and CDK2 to cause DNA damage. ? Prexasertib dihydrochloride (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells. ? Prexasertib dihydrochloride (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells. ? Prexasertib dihydrochloride (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells. ? ? Prexasertib dihydrochloride (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA. In Vivo: Prexasertib dihydrochloride (LY2606368 dihydrochloride; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts. ? Prexasertib dihydrochloride (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8). 相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | Cell Death Library | Serine/Threonine Kinase Inhibitor Library | Multi-Target Compound Library | Bioactive Compound Library Max | MG-132 | 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 | DAPT 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。