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MS049 {[allProObj[0].p_purity_real_show]}

货号:A567534 Ambeed 开学季,买赠积分,赢豪礼

MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM respectively.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
MS049 化学结构 CAS号:1502816-23-0
MS049 化学结构
CAS号:1502816-23-0
MS049 3D分子结构
CAS号:1502816-23-0
MS049 化学结构 CAS号:1502816-23-0
MS049 3D分子结构 CAS号:1502816-23-0
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MS049 纯度/质量文件 产品仅供科研

货号:A567534 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 {[allProObj[0].p_purity_real_show]}
UNC1999 +++

EZH2, IC50: 2 nM

EZH1, IC50: 45 nM

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EPZ005687 ++

EZH2, Ki: 24 nM

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EPZ015666 +++

PRMT5, Ki: 5 nM

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3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

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EPZ6438 +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

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GSK126 ++

EZH2, IC50: 9.9 nM

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MI-3 +

Menin-MLL, IC50: 648 nM

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MM-102 ++

MLL1, IC50: 0.4 μM

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EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

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SGC0946 ++++

DOT1L, IC50: 0.3 nM

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PFI-2 HCl ++++

SETD7, IC50: 2 nM

SETD7, Ki: 0.33 nM

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Pinometostat ++++

DOT1L, Ki: 80 pM

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EPZ004777 +++

DOT1L, IC50: 0.4 nM

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Entacapone ++

COMT, IC50: 151 nM

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UNC0379 +

SETD8, IC50: 7.9 μM

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Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

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GSK343 +++

EZH2, IC50: 4 nM

EZH1, IC50: 240 nM

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BIX-01294 3HCl +

G9a, IC50: 2.7 μM

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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。

MS049 生物活性

描述 Histone arginine methylation is a key post-translational modification that mediates epigenetic events that activate or repress gene transcription. Protein arginine methyltransferases (PRMTs) are the driving force for the process of arginine methylation, and the core histone proteins have been shown to be substrates for most PRMT family members[2].MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells. MS049 (0.1-10 μM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM).MS049 (0.1-100 μM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50=1.4±0.1 μM) in HEK293 cells.MS049 is selective for PRMT4 and PRMT6 over a broad range of epigenetic modifiers, including other PRMTs, PKMTs, DNMTs, KDMs, and methyllysine/methylarginine reader proteins, and non-epigenetic targets[3].

MS049 参考文献

[1]Shen Y, Szewczyk MM, et al. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J Med Chem. 2016 Oct 13;59(19):9124-9139.

[2] Melody D Fulton, Mengtong Cao,et al. The macromolecular complexes of histones affect protein arginine methyltransferase activities. J Biol Chem. 2021 Oct;297(4):101123.

[3] Shen Y et al. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J Med Chem. 2016 Sep 15.

MS049 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.03mL

0.81mL

0.40mL

20.13mL

4.03mL

2.01mL

40.26mL

8.05mL

4.03mL

MS049 技术信息

CAS号1502816-23-0
分子式C15H24N2O
分子量 248.364
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 30 mg/mL(120.79 mM),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

H2O: 100 mg/mL(402.64 mM)

动物实验配方
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