UNC0642

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Chemical Structure| 1481677-78-4 同义名 : -
CAS号 : 1481677-78-4
货号 : A464128
分子式 : C29H44F2N6O2
纯度 : 99%+
分子量 : 546.696
MDL号 : MFCD28044322
存储条件：

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

In solvent -20°C:1个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(91.46 mM)，配合低频超声助溶，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
描述 UNC0642 is the first G9a and GLP in vivo chemical probe with Ki value of 3.7nM, and displayed high in vitro potency for GLP with IC50<2.5nM. UNC0642 potently inhibited cellular inhibition of H3K9me2 with IC50 values of 110, 130, 130 and 40nM in MDA-MB-231, U2OS, PC3 and PANC-1 cell lines. UNC0642 reduced clonogenicity in PANC-1 cells in a concentration-dependent manner, at concentration of 0.5μM and 1μM, post 2 weeks, while it had no effect on clonogenicity in MDA-MB-231 cells[4]. UNC0642 caused a selective reduction of the dimethylation of histone H3 lysine 9 (H3K9me2) at PWS-IC (Prader–Willi syndrome), without changing DNA methylation, and activated candidate PWS-associated genes. UNC0642 improved survival and growth in a mouse model with a paternal deletion from Snrpn to Ube3a (m+/p∆S−U)[5].
作用机制 UNC0642 is competitive with the substrate and non-competitive with the cofactor SAM.[4]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.15mL

1.83mL

0.91mL

18.29mL

3.66mL

1.83mL
参考文献

[1]Liu F, Barsyte-Lovejoy D, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42.

[2]Kim Y, Lee HM, et al. Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. Nat Med. 2017 Feb;23(2):213-222.

[3]Wang DY, Kosowan J, et al. Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice. Acta Pharmacol Sin. 2018 May;39(5):866-874.

[4]Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31. PMID: 24102134; PMCID: PMC3880643.

[5]Kim Y, Lee HM, Xiong Y, Sciaky N, Hulbert SW, Cao X, Everitt JI, Jin J, Roth BL, Jiang YH. Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. Nat Med. 2017 Feb;23(2):213-222. doi: 10.1038/nm.4257. Epub 2016 Dec 26. PMID: 28024084; PMCID: PMC5589073.