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。

CRT0044876

CAS No. : 6960-45-8

MCE 站：CRT0044876

产品活性：CRT0044876 是一种高效、选择性的嘌呤/嘧啶核苷核酸内切酶 1 (APE1) 抑制剂，IC₅₀ 约为 3 μM。CRT0044876 可抑制 APE1 的 AP 内切酶、3′-磷酸二酯酶和 3′-磷酸酶活性，也是 APE1 所属的核酸外切酶 III 家族的特异性抑制剂。CRT0044876 增强了几种 DNA 碱基靶向化合物的细胞毒性。

研究领域：Cell Cycle/DNA Damage

作用靶点：DNA/RNA Synthesis

In Vitro: A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate by an AP endonuclease. CRT0044876 has an IC₅₀ for inhibition of APE1 of ?3 μM and not only inhibits AP site cleavage catalyzed by purified APE1, but also cleavage directed by APE1 in a HeLa whole cell extract. CRT0044876 inhibits the 3′-phosphoglycolate diesterase activity of APE1 with an IC₅₀ of ?5 μM.
CRT0044876 inhibits both the exonuclease and AP endonuclease activities of exonuclease III, but shows no inhibitory activity towards endonuclease IV. CRT0044876 has minimal effects on BamHI restriction endonuclease or topoisomerase I even at CRT0044876 concentrations of 100 μM.
At non-toxic concentrations, CRT0044876 potentiates the cytotoxicity of several DNA damaging agents, which generate damage that is repaired in the BER pathway, including some currently-used anticancer drugs. The combination of MMS and CRT0044876 leads to a synergistic increase in the level of AP sites. Consistent with CRT0044876 being a specific BER inhibitor, a strong potentiation of hmdUrd cytotoxicity is seen in CRT0044876-treated cells (HT1080 cells).

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Cycloheximide  |  Oxaliplatin  |  Gemcitabine  |  Actinomycin D  |  Mitomycin C  |  Bleomycin sulfate  |  Carboplatin  |  Cytarabine  |  Favipiravir  |  Methotrexate  |  Streptozocin  |  Anisomycin  |  Fludarabine  |  Thymidine  |  Epirubicin hydrochloride  |  Daunorubicin hydrochloride  |  Capecitabine  |  Hydroxyurea  |  Plicamycin  |  Urolithin A  |  Brequinar  |  Folic acid  |  ML216  |  Halofugi  |  Floxuridine  |  Triciribine  |  Galidesivir hydrochloride  |  Adenine

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。