MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

BI 2536

CAS No. : 755038-02-9

MCE 国际站：BI 2536

产品活性：BI 2536 是 PLK1 和 BRD4 的双抑制剂，IC₅₀ 分别为 0.83 和 25 nM。BI-2536 抑制 IFNB (IFN-β，干扰素 β) 基因转录。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：Polo-like Kinase (PLK)  |  Epigenetic Reader Domain  |  Apoptosis

In Vitro: Exceeding a 100-fold concentration range starting at 10 nM, BI 2536 causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status). The half-maximal effective concentration (EC₅₀) values in this cell panel ranged 2-25 nM, whereas a concentration of 100 nM of BI 2536 is typically sufficient for inducing a complete mitotic arrest. The proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells is blocked at EC₅₀values ranging 12-31 nM, indicating a comparable sensitivity of cycling nontransformed cells to BI 2536.

In Vivo: BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment; both schedules are well-tolerated, as judged by clinical signs and absence of major body-weight changes.

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  |  Epigenetics Compound Library  |  Kinase Inhibitor Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  Anti-Prostate Cancer Compound Library  |  Heterocyclic Compound Library  |  Cell Death Library  |  Serine/Threonine Kinase Inhibitor Library  |  Anti-Hematopathy Compound Library  |  Multi-Target Compound Library  |  Bioactive Compound Library Max  |  MG-132  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Tamoxifen  |  Y-27632  |  Paclitaxel  |  Z-VAD-FMK  |  LY294002  |  2-Deoxy-D-glucose  |  Angiotensin II human  |  Acetylcysteine  |  Staurosporine  |  Actinomycin D  |  SB-431542  |  5-Fluorouracil  |  Bortezomib  |  Oxaliplatin  |  Deferoxamine mesylate  |  Sorafenib  |  Trametinib  |  Gemcitabine  |  Temozolomide  |  Etoposide  |  Rotenone  |  Mdivi-1  |  Monomethyl auristatin E  |  Decitabine  |  Ruxolitinib  |  Elesclomol  |  DAPT

热门产品线：重组蛋白  |  药物筛选  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，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；
•   50,000 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；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   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。