UNC0379
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货号：A211708
UNC0379 is a selective inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3 ± 1.0 μM.
UNC0379 化学结构
UNC0379 3D分子结构
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UNC0379 纯度/质量文件 产品仅供科研
货号：A211708
标准纯度：
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产品说明书
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UNC0379 质控信息
BRD4770
✔
99%+
UNC1999
+++
EZH1, IC50: 45 nM
EZH2, IC50: 2 nM
99%+
EPZ005687
++
98+%
EPZ015666
+++
99%+
3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
99%+
Tazemetostat
+++
EZH2, IC50: 11 nM
EZH2, Ki: 2.5 nM
98%
GSK126
++
99%+
MI-3
+
98%
MM-102
++
99%
EI1
++
Ezh2 (wild-type), IC50: 15 nM
EZH2 (Y641F), IC50: 13 nM
98%
SGC0946
++++
99%+
PFI-2 HCl
++++
SETD7, Ki: 0.33 nM
SETD7, IC50: 2 nM
99%+
Pinometostat
++++
99%+
EPZ004777
+++
99%+
Entacapone
++
95%
UNC0379
+
99%+
Menin-MLL inhibitor MI-2
+
98%
GSK343
+++
EZH1, IC50: 240 nM
EZH2, IC50: 4 nM
99%+
BIX-01294 3HCl
+
99%+
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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。
UNC0379 生物活性
靶点
描述
UNC0379 is the first substrate-competitive inhibitor of SETD8 with IC50 value of 7.3μM, selective for SETD8 over 15 other methyltransferases[4]
作用机制
UNC0379 is a substrate-competitive SETD8 inhibitor. The quinazoline rings of the compound fill the space that in the SETD8-SAH complex is occupied by the amino group of the substrate lysine side chain.[3]
UNC0379 参考文献
[1] Ma A, Yu W, et al. Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.
[2] Butler KV, Ma A, et al. Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase. J Med Chem. 2016 Nov 10;59(21):9881-9889. Epub 2016 Nov 2.
[3] Butler KV, Ma A, Yu W, Li F, Tempel W, Babault N, Pittella-Silva F, Shao J, Wang J, Luo M, Vedadi M, Brown PJ, Arrowsmith CH, Jin J. Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase. J Med Chem. 2016 Nov 10;59(21):9881-9889. doi: 10.1021/acs.jmedchem.6b01244. Epub 2016 Nov 2. PMID: 27804297; PMCID: PMC5148670.
[4] Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J. Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33. doi: 10.1021/jm500871s. Epub 2014 Jul 25. PMID: 25032507; PMCID: PMC4136711.
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UNC0379 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
2.42mL
0.48mL
0.24mL
12.09mL
2.42mL
1.21mL
24.18mL
4.84mL
2.42mL
UNC0379 技术信息
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