| 产品描述: | KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity |
| 靶点: |
MBD2 (methyl-CpG-binding domain protein 2);DNAAlkylator/Crosslinker |
| 体外研究: |
KCC-07 (10 μM; 72 hours; MB cells) treatment clearly inhibited MB cell growth in vitro, consistent with induction of anti-proliferative BAI1/p53/p21 signaling.
KCC-07 (10 μM; 48 hours; MB cells) treatment largely abrogates MBD2 binding to the ADGRB1 promoter and restores BAI1 mRNA and protein expression in BAI1-silent MB cells. |
| 体内研究: |
KCC-07 (100 mg/kg; intraperitoneal injection; 5 days/week; athymic nude mice) treatment inhibits tumor growth and significantly extends the survival of MB xenografts in vivo. Animal Model: Outbred athymic nude mice (females; 8-10 weeks old) injected with MB cells Dosage: 100 mg/kg Administration: Intraperitoneal injection; 5 days/weekResult: Significantly extended the survival of MB xenografts in vivo. |
| 参考文献: |
1. Dan Zhu, et al. BAI1 Suppresses Medulloblastoma Formation by Protecting p53 From Mdm2-Mediated Degradation. Cancer Cell. 2018 Jun 11;33(6):1004-1016.e5. |
| 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 |
3.713 ml |
18.565 ml |
37.131 ml |
| 5 mM |
0.743 ml |
3.713 ml |
7.426 ml |
| 10 mM |
0.371 ml |
1.857 ml |
3.713 ml |
| 50 mM |
0.074 ml |
0.371 ml |
0.743 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。 |