MM-102

目录号:S7265 别名: HMTase Inhibitor IX

MM-102 Chemical Structure

Molecular Weight(MW): 669.8

MM-102是一个高亲和力的多肽模拟的MLL1抑制剂,无细胞试验中IC50为0.4 μM。

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RMB 807.01 现货
RMB 5472.63 现货
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客户使用Selleck该产品发表文献6篇:

客户使用该产品的4个实验数据:

  • Immunofluorescence staining of H3K4me2/3 (red) in the IVF, SCNT and MM-102-NT embryos. The nuclei (blue) were stained with DAPI. The merged images of H3K4me2/3 and DNA were purple. Scale bars: 50 μm.

    Cell Physiol Biochem, 2018, 45(4):1529-1540. MM-102 purchased from Selleck.

    (D) ChIP-qPCR analysis of the H3K4me3 levels in hESCs synchronized in mitosis with or without MLL1/2 inhibitors. DMSO, cells treated with DMSO only; Noc, cells blocked in mitosis with nocodazole; Noc + MLL Inh, cells blocked in mitosis with nocodazole in the presence of Mi-2 and MM-102 (20 μM each). Values for percent input are normalized to the IgG control (n = 2). One-way analysis of variance followed by Tukey's test for multiple comparisons was performed. *, P < 10−2; ****, P < 10−5; ns, not significant. (E) Reverse transcription-qPCR analysis of RNA expression levels for bivalent genes after induction of differentiation in unsynchronized H9 ES cells pretreated with MLL inhibitors. Differentiation was induced using E6 medium containing 1 μM RA per 24 h. DMSO, cells pretreated with DMSO only; MLL Inh, cells pretreated with Mi-2 and MM-102 (20 μM each) for 24 h. Unpaired parametric t test with Welch's corrections was performed. Two-tailed P values were calculated. *, P < 10−2; **, P < 10−3; ***, P < 10−4; ns, not significant. Log2 RNA levels were normalized against HPRT1 RNA levels and expressed as fold change between undifferentiated and differentiated cells.

    Mol Cell Biol, 2015, 36(4):615-27. MM-102 purchased from Selleck.

  • (d-e) The viability of cells treated with cisplatin and MM-102 for 24h in concentrations as indicated was determined CCK-8 assay.

    Int J Biol Sci, 2018, 14(9):1122-1132. MM-102 purchased from Selleck.

    NHMCs were incubated 24 h in 5.6 (white bars) or 25 mM glucose (black bars) in the presence or absence of TSA (200 nM) or MM-102 (50 μM) as indicated. mRNA was extracted from the cells after incubation and SPP1 expression was quantified by qPCR and normalized to housekeeping genes HPRT and PPIb expression. The values represent the mean ± SEM of five to eleven independent experiments. *p < 0.05, ***p < 0.001 vs. 5.6 mM glucose without inhibitors; yp < 0.05 vs. 25 mM glucose without inhibitors.

    Biochem Biophys Res Commun, 2016, 469(1):108-13. MM-102 purchased from Selleck.

产品安全说明书

Histone Methyltransferase抑制剂选择性比较

生物活性

产品描述 MM-102是一个高亲和力的多肽模拟的MLL1抑制剂,无细胞试验中IC50为0.4 μM。
靶点
MLL1 [1]
(Cell-free assay)
0.4 μM
体外研究

MM-102,作为MLL1的模拟肽,展现了与WDR5的高亲和性,相应的IC50和Ki分别为2.9nM和<1nM。在转染了MLL1-AF9的鼠源细胞中,MM-102特异性的降低了两个重要的MLL1靶基因(HoxA9andMeis-1)的表达,这两个基因是MLL1介导的白血病形成所必须的。另外,MM-102高效并且选择性的抑制了含有MLL1融合蛋白的白血病细胞的生长,并且诱导了这些细胞的凋亡。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4-11 M{e3eXBzd2yrZnXyZZRqd25iYYPzZZk> NXLSSXJVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMhcGG{Yn;ybY5oKE2OTD3BSlQh[W[2ZYKgO{Bl[Xm|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliQYPzZZktKEmFNUC9NlUh|ryP MlPtNlc4OjB3NUW=
K562 MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 M2rwU|czKGh? M{K4PWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDoZZJjd3KrbnegRmNTNUGETDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBES0t6LXLhd4VlKGOxbH;ybY1mfHKrYzDhd5NigSxiSVO1NF0{Py56IN88US=> NUjQV4xZOjd5MkC1OVU>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 23210835     


Selective inhibition of growth of leukemia cell lines with MM-102 treatment for 7 days. 

23210835

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

体外甲基化转移酶试验:

HMT试验在50mMHEPESpH7.8,100mMNaCl,1.0mMEDTA,和5%甘油组成的反应液中进行,温度为22°C.每个反应的底物包括1.5μCi辅酶,3H-S-腺苷甲硫氨酸.H3十肽,浓度为50μM.加入浓度范围在0.125到128μM的抑制剂以及浓度为0.5μM的预组装的WDR5/RbBP5/ASH2L复合物孵育2–5min。然后加入终浓度为0.5μM的MLL1蛋白开始反应,30分钟后用闪烁法测量放射性强度。将反应液滴到方形的P81滤纸上,放入到新鲜配制的浓度为50mM,pH为9.0的重碳酸钠溶液中沉淀,在经过清洗和染色后将样品放入到UltimaGold闪烁液中涡旋并计数。该试验利用0.5μMMLL1/WDR5/RbBP5/ASH2L与非反应突变WDR5D107A的复合物作为负对照。
细胞实验:

[1]

- 合并
  • Cell lines: MV4;11,KOPN8和K562细胞
  • Concentrations: ~100 μM
  • Incubation Time: 7天
  • Method:

    MV4;11,KOPN8和K562细胞培养在加入10%胎牛血清以及100 U/L青霉素和链霉素的RPMI 1640培养基中,温度37 °C5% CO2. 密度为5 × 105/每孔的1 mL细胞种在12孔板中,加入空白对照DMSO(0.2%)或者MM-102处理七天,每隔两天更换一次培养基和抑制剂。遵照生产商的说明使用发光法细胞活力检测试剂盒。首先,在每孔细胞中加入100 μL试验试剂,在回旋振荡器上混和2 min来诱导细胞分裂。室温孵育十分钟后,用酶标仪检测。


    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (149.29 mM)
Water 100 mg/mL (149.29 mM)
Ethanol 100 mg/mL (149.29 mM)

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 669.8
化学式

C35H49F2N7O4

CAS号 1417329-24-8
储存条件 粉状
溶于溶剂
别名 HMTase Inhibitor IX

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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操作手册

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID