| 产品描述: | TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation. |
| 靶点: |
IKK-2:17.9 nM (IC50);STAT3 ;Apoptosis;IκB/IKK;STAT |
| 体内研究: |
TPCA-1 (3, 10, or 20 mg/kg, i.p.) results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA). TPCA-1(10 mg/kg, i.p. daily) inhibits growth of NSCLC with EGFR mutation and potentiates antitumor effect of ZD1839 in xenograft models. |
| 参考文献: |
1. Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73. 2. Podolin PL, et al. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflamm 3. Nan J, et al. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29. |
| 溶解性: |
DMSO : ≥ 100 mg/mL (358.05 mM) |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.581 ml |
17.903 ml |
35.805 ml |
| 5 mM |
0.716 ml |
3.581 ml |
7.161 ml |
| 10 mM |
0.358 ml |
1.79 ml |
3.581 ml |
| 50 mM |
0.072 ml |
0.358 ml |
0.716 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。 |