GSK591
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货号：A112992
GSK591（EPZ015866）是一种高效、选择性的蛋白 甲基转移酶5（PRMT5）抑制剂，IC50 为4 nM。
GSK591 化学结构
GSK591 3D分子结构
规格
价格
会员价
库存
数量
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GSK591 质控信息
BRD4770
✔
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UNC1999
+++
EZH1, IC50: 45 nM
EZH2, IC50: 2 nM
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EPZ005687
++
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EPZ015666
+++
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3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
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EPZ6438
+++
EZH2, Ki: 2.5 nM
EZH2, IC50: 11 nM
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GSK126
++
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MI-3
+
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MM-102
++
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EI1
++
Ezh2 (wild-type), IC50: 15 nM
EZH2 (Y641F), IC50: 13 nM
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SGC0946
++++
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PFI-2 HCl
++++
SETD7, Ki: 0.33 nM
SETD7, IC50: 2 nM
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Pinometostat
++++
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EPZ004777
+++
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Entacapone
++
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UNC0379
+
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Menin-MLL inhibitor MI-2
+
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GSK343
+++
EZH1, IC50: 240 nM
EZH2, IC50: 4 nM
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BIX-01294 3HCl
+
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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。
GSK591 生物活性
描述
GSK591 is a potent and selective PRMT5 inhibitor with IC50 value of 22nM, an optimized inhibitor based on GSK3235025. It reduced SmD3me2s levels with IC50 value of 3nM and inhibited cell proliferation with IC50 value of 62nM in Z-138 cells[3] 50 <1μM post 6-day treatment. Inhibition of PRMT5 by GSK591 activated the p53 pathway via the induction of alternative splicing of MDM4[4]
GSK591 动物研究
Dose
Mice: 10 mg/kg - 100 mg/kg[1] [1]
Administration
p.o., i.v.
GSK591 参考文献
[1] Duncan KW, Rioux N, et al. Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6.
[2] Gerhart SV, Kellner WA, et al. Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing. Sci Rep. 2018 Jun 26;8(1):9711.
[3] Duncan KW, Rioux N, Boriack-Sjodin PA, Munchhof MJ, Reiter LA, Majer CR, Jin L, Johnston LD, Chan-Penebre E, Kuplast KG, Porter Scott M, Pollock RM, Waters NJ, Smith JJ, Moyer MP, Copeland RA, Chesworth R. Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6. doi: 10.1021/acsmedchemlett.5b00380. PMID: 26985292; PMCID: PMC4753547.
[4] Gerhart SV, Kellner WA, Thompson C, Pappalardi MB, Zhang XP, Montes de Oca R, Penebre E, Duncan K, Boriack-Sjodin A, Le B, Majer C, McCabe MT, Carpenter C, Johnson N, Kruger RG, Barbash O. Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing. Sci Rep. 2018 Jun 26;8(1):9711. doi: 10.1038/s41598-018-28002-y. PMID: 29946150; PMCID: PMC6018746.
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GSK591 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.63mL
0.53mL
0.26mL
13.14mL
2.63mL
1.31mL
26.28mL
5.26mL
2.63mL
GSK591 技术信息
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