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。

Eprenetapopt

CAS No. : 5291-32⁻⁷

MCE 国际站：Eprenetapopt

产品活性：Eprenetapopt (APR-246) 是首创的在 TP53 突变细胞中恢复野生型p53功能的小分子。Eprenetapopt 引发肿瘤细胞凋亡。Eprenetapopt 还抑制硒蛋白硫氧还蛋白还原酶 1 (TrxR1)。

研究领域：Apoptosis | Autophagy

作用靶点：MDM-2/p53 | Autophagy | Apoptosis | Ferroptosis

In Vitro: Eprenetapopt inhibits both recombinant TrxR1 in vitro and TrxR1 in cells. Cellular TrxR1 activity is inhibited by Eprenetapopt irrespective of p53 status. Eprenetapopt can directly affect cellular redox status via targeting of TrxR1. Several small molecules have been shown to restore wild-type activity to mutant p53, including CP-31398, PRIMA-1 and Eprenetapopt, MIRA, STIMA, PhiKan-083 and NSC319726. PRIMA-1 and its methylated analog Eprenetapopt promote correct folding of mutant p53, induce cell death by apoptosis, and inhibit tumor growth in mice. Eprenetapopt has also been shown to reactivate mutant forms of the p63 and p73 proteins that share high structural homology with p53.
Eprenetapopt is a powerful apoptosis-inducing agent. Eprenetapopt can enhance apoptosis in mutant p53 carrying cells, compared to the p53 null parental cells. Most p53 mutants are in complex with Hsp70 proteins. Eprenetapopt treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. Several lines of evidence suggest that Eprenetapopt can also act independently of the p53 status of the cell. It can radiosensitize prostate carcinoma cell lines with mutant or wild type p53 and p53^-/- cells as well. Introduction of mutant p53 (p53ser249 or p53gln248) into p53^-/- hepatocarcinoma cells increases sensitivity to Eprenetapopt without the induction of p53 target genes.Eprenetapopt regularly induces apoptosis in mutant p53 expressing cells.

相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Ferroptosis Compound Library | Pyroptosis Compound Library | Glutamine Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | MG-132 | Erastin | Ferrostatin-1 | Cisplatin | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Cycloheximide | Y-27632 dihydrochloride | RSL3 | Acetylcysteine | Angiotensin II human | Deferoxamine mesylate | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | Necrostatin-1 | Verteporfin | Decitabine | Actinomycin D | Temozolomide | BAY 11⁻⁷082 | Etoposide | Mitomycin C

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。