| 产品描述： | UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications |
| 靶点： |
EHMT1/GLP/KMT1D:15-23 nM (IC50);G9a:63 pM (Ki);G9a:6-9 nM (IC50);HistoneMethyltransferase |
| 体外研究： |
UNC0321 (Compound 29) 抑制 G9a ECSD、G9a CLOT、GLP ECSD 和 GLP CLOT 的活性，IC50 值分别为 9 nM、6 nM、15 nM 和 23 nM。 UNC0321 (Compound 3) 降低了 MDA-MB-231 细胞中 H3K9me2 的水平，IC50 值为 11 µM。 UNC0321 (200 pM；48 h) 显著抑制 Rab4 在 HUVEC 中的表达。 Western Blot Analysis Cell Line: HUVEC. Concentration: 50 pM, 100 pM, 200 pM. Incubation Time: 48 h. Result: Reduced glucose induced expression of Cleared Caspase3 and Bax.Relieved the inhibition of glucose on Bcl-2, Caspase3, p-AKT, p-mTOR and p70 expression.Promoted proliferation and inhibited apoptosis by inhibiting Rab4. Apoptosis Analysis Cell Line: HUVEC. Concentration: 50 pM, 100 pM, 200 pM. Incubation Time: 48 h. Result: Inhibited glucose induced apoptosis. Cell Proliferation Assay Cell Line: HUVEC. Concentration: 50 pM, 100 pM, 200 pM. Incubation Time: 48 h. Result: Relieved the inhibition of glucose on HUVEC proliferation. |
| 参考文献： |
1. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. 2. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50. 3. Nie J. UNC0321 inhibits high glucose induced apoptosis in HUVEC by targeting Rab4. Biomed Pharmacother. 2020 Nov;131:110662. |
| 溶解性： |
Soluble in DMSO |
| 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 |
1.939 ml |
9.696 ml |
19.391 ml |
| 5 mM |
0.388 ml |
1.939 ml |
3.878 ml |
| 10 mM |
0.194 ml |
0.97 ml |
1.939 ml |
| 50 mM |
0.039 ml |
0.194 ml |
0.388 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京