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UNC3866  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥27mg/mL）
产品描述：基本信息 产品编号：U10078 产品名称：UNC3866 CAS: 1872382-47-2                                                   储存条件 粉末 -20℃ 四年     分子式： C43H66N6O8 溶于液体 -80℃ 六个月 分子量： 795.02 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 100mg/mL (125.78mM) Ethanol 100mg/mL (125.78mM) 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 1.2578mL 6.2891mL 12.5783mL 5mM 0.2516mL 1.2578mL 2.5157mL 10mM 0.1258mL 0.6289mL 1.2578mL 50mM 0.0252mL 0.1258mL 0.2516mL   生物活性 产品描述 一种有效的 CBX7-H3 拮抗剂，IC50 为 66±1.2nM。 靶点/IC50 PRC1 chromodomains  CBX4 chromodomains  CBX7 chromodomains    94nM(Kd) 97nM(Kd)   体外研究 UNC3866,a potent antagonist of the methyl-lysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains.UNC3866 binds the chromodomains of CBX4 and CBX7 most potently with a Kd of 100nM for each,and is 6-to 18-fold selective versus seven other CBX and CDY chromodomains while being highly selective versus >250 other protein targets.UNC3866 inhibits PC3 cell proliferation,a known CBX7 phenotype, while UNC4219,a methylated negative control compound,has negligible effects.UNC3866 is a potent and cellularly active antagonist of PRC1 chromodomains.UNC3866 is the most potent ligand reported for CBX7 with a Kd of 97±2.4nM.UNC3866 is equipotent for CBX4,which is most similar to CBX7,while it is 18-,6- and 12-fold selective for CBX4/7 over CBX2,-6 and -8,respectively.Additionally,UNC3866 is 65-fold selective for CBX4/7 over CDY1 and 9-fold selective for CBX4/7 over CDYL1b and CDYL2. 体内研究 UNC3866相对于UNC4007来说，在所检测时间点中，一直是位于血浆中的优势种类，生物利用度为25%，具有中等清除率。虽然这些数据使这个肽类化合物看起来非常有前景，但其在体内的应用受限于UNC3866的细胞透性，要在细胞内靶标发挥其作用，需要在体内具有比较高的循环浓度水平。目前，在体内实验中尝试使用较高剂量的UNC3866，以探索其潜在效用。   推荐实验方法(仅供参考) 激酶实验： The effect of UNC3866 on the methyltransferase activity of G9a,EHMT1,SUV39H1,SUV39H2,SETDB1, SETD8, SUV420H1,SUV420H2,SETD7,MLL1 trimeric complex,MLL3 tetrameric complex,EZH2 trimeric complex,PRMT1,PRMT3,PRMT5-MEP50 complex,PRMT6,PRMT7,PRMT8,PRDM9,SETD2,SMYD2,SMYD3,BCDIN3D and DNMT1 is assessed by monitoring the incorporation of tritium-labeled methyl group to lysine or arginine residues of peptide substrates using Scintillation Proximity Assay (SPA).Assays are performed in a 20μL reaction mixture containing 3H-SAM at substrate concentrations close to the Km values for each enzyme.Three concentrations (1μM,10μM,and 50μM) of UNC3866 are used in all selectivity assays. To stop the enzymatic reactions,7.5M Guanidine hydrochloride is added,followed by 180μL of buffer (20mM Tris,pH 8.0). The reactions are mixed and then transferred to a 96-well FlashPlate.The reaction mixtures in Flash plates are incubated for 1 hour and the CPM are measured using a TopCount plate reader.The CPM counts in the absence of compound for each data set are defined as 100% activity.In the absence of the enzyme, the CPM counts in each data set are defined as background (0%).   细胞实验:   PC3 cells are seeded at 200 cells/well into 24-well plates.Cells are allowed to adhere overnight.The media (DMEM supplemented with 10 % FBS) is then exchanged with fresh media containing DMSO,UNC3866 or UNC4219.On day three,the media are exchanged with fresh media containing DMSO,UNC3866 or UNC4219.For dose-response studies,the EC50 is derived from a six-point titration ranging from 100μM to 0.4μM of UNC3866 or UNC4219.At day 0,3 or 6,cells are fixed with ice-cold methanol for 30 sec.and rehydrated with PBS.Nuclei of the cells are stained with DAPI (0.05μg/mL) and numerated using High Content Microscopy.For dose-response studies,the cell count of UNC3866- or UNC4219-treated cells is normalized to the average cell count of DMSO-treated cells.The EC50 is calculated using the“log[inhibitor] vs.the normalized response-Variable slope”equation in GraphPad Prism 5.   动物实验:   动物模型 swiss albino小鼠 剂量 10mg/kg 给药处理 腹腔注射
保存条件：-20℃

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