| 产品描述: | NF-κB 抑制剂;NF-κB Inhibitors;;InformationDTP3 DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.TargetsGADD45β/MKK7 ; NF-κBIn vitroDTP3 physically interacts with MKK7, both in isolation and within the complex with GADD45β, and dissociates the GADD45β/MKK7 complex via an allosteric mechanism. DTP3 selectively kills cells and induces apoptosis in MM cells with functional MKK7 and elevated GADD45β expression without toxicity to normal cells. In addition, DTP3 displays synergistic activity with bortezomib in two different MM cell lines, exhibiting a combination index of 0.21 in U266 cells and of 0.56 in KMS-12 cells.In vivoDTP3 (14.5 mg/kg/day) exhibits potent antitumor activity against MM in mouse plasmacytoma model.Cell Research(from reference)Cell lines:CD138+ cells Concentrations:~300 nM Incubation Time:8 days |
| 体内研究: |
DTP3 TFA (皮下注射;14.5 mg/kg/天;28 天) 使肿瘤显著缩小,并几乎根除小鼠皮下骨髓瘤异种移植物。 DTP3 TFA (静脉注射;10 mg/kg/天) t1/2为1.26小时,CL为27.13 ML/min/kg,Vd 为 2.80 L/kg。 |
| 保存条件: |
避光,-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.903 ml |
9.513 ml |
19.026 ml |
| 5 mM |
0.381 ml |
1.903 ml |
3.805 ml |
| 10 mM |
0.19 ml |
0.951 ml |
1.903 ml |
| 50 mM |
0.038 ml |
0.19 ml |
0.381 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。 |