2. Epigenetics
  3. Histone Methyltransferase
  4. MS023 trihydrochloride

MS023 trihydrochloride 是一种有效选择性的，具有细胞活性的人 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂，对 PRMT1，PRMT3，PRMT4，PRMT6 和 PRMT8 的 IC50 分别为 30，119，83，4 和 5 nM。

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MS023 trihydrochloride Chemical Structure

MS023 trihydrochloride Chemical Structure

CAS No. : 2108631-19-0

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MS023 trihydrochloride 的其他形式现货产品:

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Other Forms of MS023 trihydrochloride:

MS023 trihydrochloride 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MS023 trihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively[1].

体外研究
(In Vitro)

MS023 dihydrochloride (1-1000 nM；48 小时) 抑制 MCF7 细胞中的 PRMT1 甲基转移酶活性[1]。
MS023 dihydrochloride (1-1000 nM；20 小时) 抑制 HEK293 细胞中的 PRMT6 甲基转移酶活性[1]。

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

MS023 trihydrochloride 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF7 and HEK293 cells
Concentration: 1.4, 4, 12, 37, 111, 333, and 1000 nM
Incubation Time: 48 hours for MCF7 cells; 20 hours for HEK293 cells
Result: Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC50=9 nM).Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56 nM).
体内研究
(In Vivo)

MS023 dihydrochloride (160 mg/kg，ip) 与 PKC412 (100 mg/kg，ig) 联合给药，通过抑制功能性 MLL-r ALL 起始细胞的维持来阻断 MLL-r 急性淋巴细胞白血病 (ALL) 的传播[2]。

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

Animal Model: NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells[2]
Dosage: 160 mg/kg
Administration: Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
Result: Combinatorial treatment extended survival of leukemic mice relative to single treatments.
分子量

396.78

Formula

C17H28Cl3N3O
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MS023 trihydrochloride 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

MS023 trihydrochloride2108631-19-0Histone MethyltransferaseInhibitorinhibitorinhibit

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产品名称：
MS023 trihydrochloride
目录号：
HY-19615A
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