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PK11007 促销  ≥98%

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO（250 mg/mL 超声）
产品描述：基本信息 产品编号：P10857 产品名称：PK11007 CAS: 874146-69-7   储存条件 粉末 -20℃ 四年     分子式： C15H11ClFN5O3S2 溶于液体 -80℃ 六个月 分子量 427.86 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 32mg/mL (67.51mM) Ethanol Insoluble Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3372mL 11.6861mL 23.3721mL 5mM 0.4674mL 2.3372mL 4.6744mL 10mM 0.2337mL 1.1686mL 2.3372mL   生物活性 产品描述 是具有抗癌活性的温和硫醇烷基化剂。PK11007 通过两个表面暴露的半胱氨酸的选择性烷基化来稳定 p53，而不影响其 DNA 结合活性。 靶点/IC50 MDM-2/p53; Reactive Oxygen Species 体外研究 PK11007 (0-120µM; 24 hours; four p53 wild-type cell lines and fours p53 mutant cell lines) treatment results in a large viability reduction in mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S) at concentrations ranging from 15 to 30 µM. PK11007 induces mainly caspase-independent cell death.PK11007 (0-60µM; 3 hours or 6 hours;NUGC-4,NUGC-3,MKN1,HUH-6, and HUH-7 cancer cells) treatment up-regulates protein levels of the p53 target genes p21, MDM2, and PUMA in a mostly concentration-dependent manner in NUGC-3 (p53-Y220C),HUH-7 (p53-Y220C) and MKN1 (p53-V143A) cells, suggesting partial restoration of transcriptional activity to destabilized p53 mutants. PK11007 also increases p53 activity in HUH-6 and NUGC-4 cells, as indicated by the increase of MDM2, PUMA, and p21 protein levels.PK11007 (15-20µM; 4.5 hours or 6 hours; MKN1, HUH-7,NUGC-3, HUH-6 cells) treatment increases transcription of p53 target genes in three mutant p53 cell lines after 6-h treatment. PUMA and p21 mRNA levels are up-regulated by a factor of 2 upon treatment of NUGC-3, MKN, and HUH-7 cells, as well as NOXA for the latter two.MDM2 levels are halved in MKN1 and NUGC-3 cells.PK11007 viability reduction is potentiated by glutathione depletion. To test whether PK11007 also increases ROS levels,NUGC-3,NUGC-4,HUH-6,HUH-7, and MKN1 cells with PK11007 are incubated for 2h. There are elevated ROS levels in all cell lines after 2h. In the mutant p53 cells MKN1, HUH-7, and NUGC-3, however, the ROS increase is higher at 60µM PK11007 than in NUGC-4 and HUH-6 cells, suggesting that the higher PK11007 sensitivity of the mutant p53 cell lines is mediated by a stronger ROS induction. Basal and PK11007-induced ROS levels in MKN1 cells are at least twofold higher than in other cell lines.PK11007 inhibits cell proliferation, induces apoptosis and alters genes involved in cell death are all consistent with the ability of PK11007 to reactivate mutant p53.Cell Viability Assay Cell Line: p53 wild-type cell lines (WI-38, HUH-6, NUGC-4, SJSA-1) and p53 mutant cell lines (HUH-7,NUGC-3,SW480,MKN1) Concentration: 0μM, 20μM, 40μM, 60µM, 80µM, 100µM and 120µM Incubation Time: 24 hours Result: There was a large viability reduction in mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S) and in p53 WT cell line SJSA-1 at concentrations ranging from 15 to 30µM. The p53 WT cancer cell lines HUH-6, NUGC-4 and WI-38 were less sensitive with reduced cell viability only at high concentrations of compound (60 and 120µM). Western Blot Analysis Cell Line: NUGC-4, NUGC-3, MKN1, HUH-6, and HUH-7 cancer cells Concentration: 0μM,15μM,30μM,60µM Incubation Time: 3 hours or 6 hours Result: Up-regulated protein levels of the p53 target genes p21, MDM2, and PUMA in a mostly concentration-dependent manner in NUGC-3 (p53-Y220C), HUH-7 (p53-Y220C) and MKN1 Up-regulated protein levels of the p53 target genes p21, MDM2, and PUMA in a mostly concentration-dependent manner in NUGC-3 (p53-Y220C), HUH-7 (p53-Y220C) and MKN1 RT-PCR Cell Line: MKN1, HUH-7, NUGC-3, HUH-6 cells Concentration: 15μM, 20μM Incubation Time: 4.5 hours or 6 hours Result: Increased transcription of p53 target genes in three mutant p53 cell lines after 6-h treatment. PUMA and p21 mRNA levels were up-regulated by a factor of 2 upon treatment of NUGC-3, MKN, and HUH-7 cells, as well as NOXA for the latter two. MDM2 levels were halved in MKN1 and NUGC-3 cells.
保存条件：-20℃

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