| 产品描述： | kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity. |
| 靶点： |
PKD1:28.3 nM (IC50);PKD3:53.2 nM (IC50);PKD2:58.7 nM (IC50);Serine/threoninkinase |
| 体外研究： |
kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also inhibits Ser916 phosphorylation of PKD1 (IC50, 2.2 ± 0.6 μM) in LNCaP cells. Moreover, kb NB 142-70 is cytotoxic against PC3 cells with an EC50 of 8.025 μM. kb NB 142-70 (0-5 μM) concentration-dependently prevents ANG II-induced phosphorylation of HDAC4 at Ser246 and Ser632, HDAC5 at Ser259 and Ser498, and HDAC7 at Ser155 in IEC-18 cells. In addition, kb NB 142-70 (3.5 μM) also suppresses HDAC4, HDAC5, and HDAC7 phosphorylation in IEC-18 cells stimulated with ANG II for 0-240 min or with vasopressin, lysophosphatidic acid (LPA), or phorbol 12,13-dibutyrate (PDBu). |
| 参考文献： |
1. Lavalle CR, et al. Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility. BMC Chem Biol. 2010 May 5;10:5. 2. James Sinnett-Smith, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15; 306(10): C961-C971. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.979 ml |
19.895 ml |
39.789 ml |
| 5 mM |
0.796 ml |
3.979 ml |
7.958 ml |
| 10 mM |
0.398 ml |
1.989 ml |
3.979 ml |
| 50 mM |
0.08 ml |
0.398 ml |
0.796 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