2. Epigenetics Apoptosis NF-κB Immunology/Inflammation
  3. Histone Methyltransferase Apoptosis NF-κB TNF Receptor Interleukin Related
  4. MM-102

MM-102  (Synonyms: HMTase Inhibitor IX)

目录号: HY-12220 纯度: 99.17%
COA 产品使用指南 技术支持

MM-102 (HMTase Inhibitor IX) 是一种具有细胞渗透性并紧密结合的 MLL1-WDR5 相互作用抑制剂 (IC50=2.4 nM)。MM-102 能特异性抑制含有 MLL1 融合蛋白的白血病细胞的生长和诱导细胞凋亡 (apoptosis)，并减轻缺血再灌注损伤小鼠肾脏纤维化和炎症反应。此外，MM-102 也作为 H3K4 组蛋白甲基转移酶抑制剂来改善猪体细胞核移植 (SCNT) 胚胎发育。

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MM-102 Chemical Structure

MM-102 Chemical Structure

CAS No. : 1417329-24-8

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5 mg ￥1540
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10 mg ￥2520
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Other Forms of MM-102:

MM-102 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos[1][2][3][4][5].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
K562 IC50
37.8 μM
Compound: MM-102
Growth inhibition of human K562 cells after 7 days by MTS assay
Growth inhibition of human K562 cells after 7 days by MTS assay
[PMID: 27598236]
K562 IC50
37.8 μM
Compound: MM-102
Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
[PMID: 27720555]
MV4-11 IC50
20.7 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein after 72 hrs by CCK8 assay
[PMID: 27598236]
MV4-11 IC50
20.7 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
[PMID: 27720555]
MV4-11 IC50
25 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein by CellTiter-Glo assay
[PMID: 27598236]
MV4-11 IC50
25 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 after 7 days by CellTiter-Glo luminescent cell viability Assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 after 7 days by CellTiter-Glo luminescent cell viability Assay
[PMID: 27720555]
体外研究
(In Vitro)

MM-102 (40 µM; 4 d) 处理 MLL1-AF9 转化的小鼠白血病细胞可特异性地诱导具有 MLL1 易位的白血病细胞生长停滞和细胞死亡，但不会干扰正常骨髓的生长[2]。
MM-102 (2、10 和 50 µM) 以浓度依赖的方式破坏了 WDR5 和 RbBP5 与 GSTMLL1 的关联。在 2 µM 的剂量下，轻度破坏 WDR5 与 MLL1 的关联，在 10 µM 剂量下中度破坏，在 50 µM 剂量下完全破坏[2]。
MM-102特异性地抑制 MLL1 复合物的甲基转移酶活性，IC50 值为 0.32 µM[2]。
MM-102 (50 µM; 48 h) 可以显著抑制 TFK1 和 RBE 细胞的增殖、迁移和化疗耐药[3]。
MM-102 (50 µM; 1 h) 不仅显著降低 TGF-b1刺激的 NRK-49F 细胞中的 MLL1、WDR5 和 H3K4me3 的表达，还抑制 p16INK4a 的表达[4]。
MM-102 (50-100 μM; 48 h) 提高了猪 SCNT 胚胎的发育能力并改善了 SCNT 胚胎发育的关键基因表达模式[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MM-102 相关抗体:

Cell Viability Assay[3]

Cell Line: TFK1 and RBE cells
Concentration: 50 µM
Incubation Time: 48 h
Result: Inhibited the expression of ABCB1, but had no effect on the expression of MBD2 and WDR5.
体内研究
(In Vivo)

MM-102 (15 mg/kg；i.p.；每日 1 次，持续 7 天) 抑制原代 CCA 模型小鼠体内肿瘤的进展[3]。
MM-102 (15 mg/kg；i.p.；每日 1 次，持续 7 天) 抑制 p16INK4a 基因在 IRI 小鼠体内表达，并减轻 IRI 小鼠的肾纤维化和肾脏炎症[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ischemia-reperfusion injury in mice[4]
Dosage: 15 mg/kg
Administration: i.p.; Once daily for 7 days
Result: Inhibited a-SMA protein expression.
Inhibited p-NF-kB (p65), IL-1b, TNF-a, and IL-6 mRNA expression.
分子量

669.80

Formula

C35H49F2N7O4
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (186.62 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4930 mL 7.4649 mL 14.9298 mL
5 mM 0.2986 mL 1.4930 mL 2.9860 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

MM-102 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4930 mL 7.4649 mL 14.9298 mL 37.3246 mL
5 mM 0.2986 mL 1.4930 mL 2.9860 mL 7.4649 mL
10 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7325 mL
15 mM 0.0995 mL 0.4977 mL 0.9953 mL 2.4883 mL
20 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
25 mM 0.0597 mL 0.2986 mL 0.5972 mL 1.4930 mL
30 mM 0.0498 mL 0.2488 mL 0.4977 mL 1.2442 mL
40 mM 0.0373 mL 0.1866 mL 0.3732 mL 0.9331 mL
50 mM 0.0299 mL 0.1493 mL 0.2986 mL 0.7465 mL
60 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6221 mL
80 mM 0.0187 mL 0.0933 mL 0.1866 mL 0.4666 mL
100 mM 0.0149 mL 0.0746 mL 0.1493 mL 0.3732 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MM-1021417329-24-8HMTase Inhibitor IXMM102MM 102Histone MethyltransferaseApoptosisNF-κBTNF ReceptorInterleukin RelatedNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILInhibitorinhibitorinhibit

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