| 产品描述： | XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity |
| 靶点： |
BMK1:80 nM (Kd);BRD4:190 nM (Kd);ERK; BMI-1; EpigeneticReaderDomain |
| 体外研究： |
XMD8-92 (0-5 Μm; 48 hours) inhibits the proliferation of HMEC and cancer cells.
XMD8-92 effectively inhibits BMK1 activation as well as induces PML’s (promyelocytic leukemia protein) downstream effector, p21. XMD8-92 significantly inhibits basic fibroblast growth factor (bFGF) induced angiogenesis in Matrigel plugs. XMD8-92 significantly induces p21 expression in HeLa and A549 cells. Cell Viability Assay Cell Line: HMEC, A549 and HeLa cells Concentration: 0.16, 0.32, 0.63, 1.25, 2.5 or 5 μM Incubation Time: 48 hours Result: Inhibited the proliferation of HMEC and cancer cells. |
| 体内研究： |
XMD8-92 (i.p.; twice a day for 28 days) significantly inhibits the growth of the xenografted human tumors. Animal Model: HeLa Xenograft Model (6-week-old Nod/Scid mice)[1] Dosage: 50 mg/kg Administration: I.p.; twice a day for 28 days Result: Significantly inhibited the growth of the xenografted human tumors. |
| 参考文献： |
1. Yang Q, et al. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.Cancer Cell. 2010 Sep 14;18(3):258-67. 2. Yang Q, et al. Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin Cancer Res. 2011 Jun 1;17(11):3527-32. 3. Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016;113(42):11865-11870. 4. Umapathy G, et al. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28;7(349):ra102. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.107 ml |
10.536 ml |
21.072 ml |
| 5 mM |
0.421 ml |
2.107 ml |
4.214 ml |
| 10 mM |
0.211 ml |
1.054 ml |
2.107 ml |
| 50 mM |
0.042 ml |
0.211 ml |
0.421 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