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| 品牌 | absin | CAS | 881202-45-5 |
|---|---|---|---|
| 分子式 | C21H20N4 | 纯度 | ＞98% |
| 分子量 | 328.41 | 货号 | abs810579 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | acts as a HDM2 ubiquitin ligase antagon | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
JNJ26854165 881202-45-5
| 产品描述 | |
| 描述 | JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | JNJ 26854165; JNJ26854165; JNJ-26854165 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO ：66 mg/mL (200.96 mM) Ethanol ：2 mg/mL (6.08 mM) |
| 生物活性 | |
| 靶点 | p53,HDM2,Mdm2 |
| In vitro(体外研究) | JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. |
| In vivo(体内研究) | JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks. |
| 研究领域 | |
| 研究领域 | CancerCell cycleCell cycle inhibitorsp53 pathway CancerOncoproteins/suppressorsTumor suppressorsp53 pathway ApoptosisIntracellularp53 Pathway Cell CycleCell Cycle Inhibitorsp53 EpigeneticsCell cycleCell Cycle Inhibitorsp53 EpigeneticsDNA / RNADNA Damage & RepairDNA Damage Responsep53 EpigeneticsTranscriptionCancer susceptibilityTumor Suppressors NeuroscienceDevelopment NeuroscienceProcesses Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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