| 产品描述: | CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity. |
| 靶点: |
Myst3:>100 μM (IC50); p300-HAT:1.4 μM (IC50); CBP-HAT:2.2 μM (IC50); PCAF:>100 μM (IC50) |
| 体内研究: |
CBP/p300-IN-19 hydrochloride (compound 29) shows antiproliferative activity with EC50s of 5.3, 8.5, 6.2, 4.4, 1.2, 4.3, 3.6, 8.7, 6.4 µM for MCF-7, MDA-MB231, LNCaP, PC-3, PANC-1, MDA-PANC-28, Molm-13, MV4;11, RPMI-8226 cells, respectively. CBP/p300-IN-19 hydrochloride (0, 5, 10 µM; 12 h) dose-dependenly inhibits the acetylation of H3K18, H3K9 and K27. |
| 参考文献: |
1. Nie S, et al. Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP. Eur J Med Chem. 2022 Jul 5;237:114407. |
| 保存条件: |
2-8°C, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.945 ml |
9.727 ml |
19.455 ml |
| 5 mM |
0.389 ml |
1.945 ml |
3.891 ml |
| 10 mM |
0.195 ml |
0.973 ml |
1.945 ml |
| 50 mM |
0.039 ml |
0.195 ml |
0.389 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。 |