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Menin-MLL inhibitor MI-2 {[allProObj[0].p_purity_real_show]}

货号:A166598 同义名: MI-2;Menin-MLL Inhibitor

MI-2 can inhibits menin-MLL interaction with IC50 of 446 ± 28 nM.

Menin-MLL inhibitor MI-2 化学结构 CAS号:1271738-62-5
Menin-MLL inhibitor MI-2 化学结构
CAS号:1271738-62-5
Menin-MLL inhibitor MI-2 3D分子结构
CAS号:1271738-62-5
Menin-MLL inhibitor MI-2 化学结构 CAS号:1271738-62-5
Menin-MLL inhibitor MI-2 3D分子结构 CAS号:1271738-62-5
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Menin-MLL inhibitor MI-2 纯度/质量文件 产品仅供科研

货号:A166598 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Histone Methyltransferase 其他靶点 纯度
BRD4770 99%+
UNC1999 +++

EZH2, IC50: 2 nM

EZH1, IC50: 45 nM

99%+
EPZ005687 ++

EZH2, Ki: 24 nM

98+%
EPZ015666 +++

PRMT5, Ki: 5 nM

99%+
3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

99%+
Tazemetostat +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

98%
GSK126 ++

EZH2, IC50: 9.9 nM

99%+
MI-3 +

Menin-MLL, IC50: 648 nM

98%
MM-102 ++

MLL1, IC50: 0.4 μM

99%
EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

98%
SGC0946 ++++

DOT1L, IC50: 0.3 nM

99%+
PFI-2 HCl ++++

SETD7, Ki: 0.33 nM

SETD7, IC50: 2 nM

99%+
Pinometostat ++++

DOT1L, Ki: 80 pM

99%+
EPZ004777 +++

DOT1L, IC50: 0.4 nM

99%+
Entacapone ++

COMT, IC50: 151 nM

95%
UNC0379 +

SETD8, IC50: 7.9 μM

99%+
Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

98%
GSK343 +++

EZH2, IC50: 4 nM

EZH1, IC50: 240 nM

99%+
BIX-01294 3HCl +

G9a, IC50: 2.7 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Menin-MLL inhibitor MI-2 生物活性

靶点
  • Histone Methyltransferase

    Menin-MLL, IC50:446 nM

描述 MI-2 is a potent menin-MLL inhibitor with IC50 value of 446nM. Treatment with MI-2 at concentration of 12.5μM, 25μM and 50μM, efficiently disrupted the menin-MLL-AF9 complex without affecting the expression level of menin and MLL-AF9 in HEK293 cells transfected with Flag-MLL-AF9. It reduced menin-MLL-AF9 occupancy on the Hoxa9 locus and downregulated MLL fusion target genes. MI-2 blocked proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 value of about 5μM, but showed only a small effect on the cell growth of E2A-HLF transduced BMC. MI-2 substantially and specifically reduced the immortalization potential of cells transformed with MLL fusion oncoproteins. Treatment with MI-2 and MI-3 resulted in much smaller, diffuse colonies, indicative of differentiation[3]. MI-2 also works as a direct inhibitor of the lanosterol synthase. It induced prominent accumulation of 24,25 epoxycholesterol and Shunt pathway metabolites[4].
作用机制 MI-2 can disrupt the menin-MLL-AF9 complex and reduce menin-MLL-AF9 occupancy on the Hoxa9 locus, thus downregulating MLL fusion target genes.[3]

Menin-MLL inhibitor MI-2 动物研究

Dose Mice: 0.05 mg/kg - 25 mg/kg[3] (i.p.)
Administration i.p.

Menin-MLL inhibitor MI-2 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01528696 Obesity Compl... 展开 >>ications; Caesarean Section, Wound 收起 << Phase 4 Terminated(Insufficient Recrui... 展开 >>tment) 收起 << - United States, Michigan ... 展开 >> University of Michigan Von Voigtlander Womens' Hospital Ann Arbor, Michigan, United States, 48109 收起 <<
NCT01528696 - Terminated(Insufficient Recrui... 展开 >>tment) 收起 << - -
NCT03680391 - Not yet recruiting October 2019 Egypt ... 展开 >> Kasr Alainy medical school Cairo, Egypt, 12111 收起 <<

Menin-MLL inhibitor MI-2 参考文献

[1]Grembecka J, He S, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nat Chem Biol. 2012 Jan 29;8(3):277-84.

[2]Phillips RE, Yang Y, et al. Target identification reveals lanosterol synthase as a vulnerability in glioma. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7957-7962.

[3]Grembecka J, He S, Shi A, Purohit T, Muntean AG, Sorenson RJ, Showalter HD, Murai MJ, Belcher AM, Hartley T, Hess JL, Cierpicki T. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nat Chem Biol. 2012 Jan 29;8(3):277-84. doi: 10.1038/nchembio.773. PMID: 22286128; PMCID: PMC3401603.

[4]Phillips RE, Yang Y, Smith RC, Thompson BM, Yamasaki T, Soto-Feliciano YM, Funato K, Liang Y, Garcia-Bermudez J, Wang X, Garcia BA, Yamasaki K, McDonald JG, Birsoy K, Tabar V, Allis CD. Target identification reveals lanosterol synthase as a vulnerability in glioma. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7957-7962. doi: 10.1073/pnas.1820989116. Epub 2019 Mar 28. PMID: 30923116; PMCID: PMC6475387.

Menin-MLL inhibitor MI-2 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.31mL

2.66mL

1.33mL

26.63mL

5.33mL

2.66mL

Menin-MLL inhibitor MI-2 技术信息

CAS号1271738-62-5
分子式C18H25N5S2
分子量 375.555
别名 MI-2;Menin-MLL Inhibitor;MI-2 MLL inhibitor;Menin-MLL inhibitor 2
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(133.14 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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