| 产品描述: | 高效,选择性和可逆的G9和GLP组蛋白甲基转移酶抑制剂;Potent, selective and reversible G9 and GLP histone methyltransferase inhibitor;;DescriptionUNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities. ApplicationIn MDA-MB-231 cells, in a concentration-dependent manner, exposure to UNC0638 for 48 h reduced H3K9me2 levels with an IC50 value of 81 ± 9 nM. Cellular levels of H3K9me2 were progressively reduced from 1 d to 4 d exposure to UNC0638 at the concentrations of 80 nM (IC50), 250 nM (IC90) and 500 nM (2 × IC90). The reductions of H3K9me2 levels with 250 nM and 500 nM treatments after 4 d were equal or very close to that of G9a and GLP knockdown cells. The effects of UNC0638 were long-lasting. In cells with 2 d exposure to UNC0638, levels of H3K9me2 remained low after washout of compound followed by 2 d incubation without the inhibitor. |
| 参考文献: |
1. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74. 2. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5. 3. Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47. 4. Nualkaew T, et al. UNC0638 induces high levels of fetal hemoglobin expression in β-thalassemia/HbE erythroid progenitor cells[J]. Annals of hematology, 2020, 99: 2027-2036. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.962 ml |
9.809 ml |
19.618 ml |
| 5 mM |
0.392 ml |
1.962 ml |
3.924 ml |
| 10 mM |
0.196 ml |
0.981 ml |
1.962 ml |
| 50 mM |
0.039 ml |
0.196 ml |
0.392 ml |
|
| 注意: |
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