Powder: -20°C for 3 years | In solvent: -80°C for 1 year
UNC1215 是一种选择性 L3MBTL3甲基赖氨酸结构域的拮抗剂,IC50为40 nM,Kd 为 120 nM。它可研究恶性脑瘤。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 245 | 现货 | ||
2 mg | ¥ 356 | 现货 | ||
5 mg | ¥ 566 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
25 mg | ¥ 2,160 | 现货 | ||
50 mg | ¥ 3,790 | 现货 | ||
100 mg | ¥ 5,450 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 719 | 现货 |
产品描述 | UNC1215, an effective and specific MBT (malignant brain tumor) antagonist, binds L3MBTL3 (IC50/Kd: 40/120 nM). The selectivity of UNC1215 for L3MBTL3 is 50-fold higher versus other members of the human MBT family. |
靶点活性 | L3MBTL3:120 nM(Kd), L3MBTL3:40 nM |
体内活性 | UNC1215与L3MBTL3结合,竞争性置换含单或二甲基赖氨酸的肽段。UNC1215对L3MBTL3的选择性比L3MBTL1高约75倍。UNC1215无细胞毒性,通过MBT域的Kme结合口袋,直接结合到L3MBTL3。UNC1215使GFP-L3MBTL3融合蛋白的细胞移动性与点突变增加,干扰GFP-L3MBTL3表型模拟的Kme结合功能,影响UNC1215的定位。UNC1215(30 μM)不影响UHRF1的串联Tudor域、CBX7的染色质域及JARID1A的PHD域。 |
激酶实验 | AlphaScreen assay: Compound plates (1 μL at 10 or 30 mM highest concentration) are diluted in 1×assay buffer (20 mM Tris pH 8.0, 25 mM NaCl, 2 mM DTT and 0.05% Tween-20) over 2 steps using a Multimek robotic pipettor and 1 μL is spotted into the wells of 384-well assay Proxiplates. To these plates 9 μL of protein- peptide mix in 1× assay buffer is added by Multidrop and incubated for 30 min at room temperature. At this point 2 μL of streptavidin-conjugate donor and nickel-chelate acceptor beads (45 μg/mL in 1× assay buffer) are added, the plates are allowed to incubate for an additional 30 min in the dark at room temperature. After incubation the plates are read on EnVision mulilabel reader equipped with HTS alpha screen laser. The screens reported are performed up to 10 or 30 μM, and therefore it should be noted that those compounds referred to as inactive are indeed inactive only within the concentration range tested. PHF23 and JARID1A are GST tagged and consequently for these assays GST-acceptor beads are used. It should be noted that any positive binding curves for L3MBTL4 that are generated yielded curves with very shallow slopes, suggesting a nonspecific interaction. The data for the IC50 values is calculated from replicate runs in that the datapoints for each compound concentration are averaged and plotted using 4-parameters curve fitting. |
细胞实验 | CellTiter-Glo luminescent cell viability assay(Only for Reference) |
分子量 | 529.72 |
分子式 | C32H43N5O2 |
CAS No. | 1415800-43-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (175.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 93 mg/mL (175.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.8878 mL | 9.4389 mL | 18.8779 mL | 47.1947 mL |
5 mM | 0.3776 mL | 1.8878 mL | 3.7756 mL | 9.4389 mL | |
10 mM | 0.1888 mL | 0.9439 mL | 1.8878 mL | 4.7195 mL | |
20 mM | 0.0944 mL | 0.4719 mL | 0.9439 mL | 2.3597 mL | |
50 mM | 0.0378 mL | 0.1888 mL | 0.3776 mL | 0.9439 mL | |
100 mM | 0.0189 mL | 0.0944 mL | 0.1888 mL | 0.4719 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
UNC1215 1415800-43-9 Apoptosis Chromatin/Epigenetic Histone Methyltransferase Epigenetic Reader Domain inhibit Inhibitor Cerebrum UNC-1215 probe Malignant MBT methyllysine UNC 1215 inhibitor