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UNC1215

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Chemical Structure| 1415800-43-9 同义名 : -
CAS号 : 1415800-43-9
货号 : A255611
分子式 : C32H43N5O2
纯度 : 99%+
分子量 : 529.716
MDL号 : MFCD22683289
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(471.95 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
动物实验配方：
生物活性
靶点

  • bromodomain

    L3MBTL3, IC50:120 nM

    L3MBTL3- D274A, IC50:3.5 μM
描述 UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with IC50 value of 40nM, greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. UNC1215 potently antagonized 3MBT localization in cells at 1μM, which may due to the disruption of the Kme-binding function of L3MBTL3[2].
作用机制 UNC1215 can bind to L3MBTL3 in a unique 2:2 polyvalent mode of interaction between UNC1215 and L3MBTL3 and competitively displace mono- or dimethyllysine-containing peptides.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.44mL

1.89mL

0.94mL

18.88mL

3.78mL

1.89mL
参考文献

[1]James LI, Barsyte-Lovejoy D, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91.

[2]James LI, Barsyte-Lovejoy D, Zhong N, Krichevsky L, Korboukh VK, Herold JM, MacNevin CJ, Norris JL, Sagum CA, Tempel W, Marcon E, Guo H, Gao C, Huang XP, Duan S, Emili A, Greenblatt JF, Kireev DB, Jin J, Janzen WP, Brown PJ, Bedford MT, Arrowsmith CH, Frye SV. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91. doi: 10.1038/nchembio.1157. Epub 2013 Jan 6. PMID: 23292653; PMCID: PMC3577944.