MDM2/4-p53-IN-2 (2q) 是一种有效的双重MDM2/ MDM4抑制剂和p53激活剂，作用于 MDM2-p53 和 MDM4-p53 复合物的IC50值分别是 70.7 nM 和 81.4 nM。MDM2/4-p53-IN-2 可以调控细胞周期，诱导细胞凋亡(apoptosis)，具有抗癌活性。
| 生物活性 | MDM2/4-p53-IN-2 (2q) is a potent dualMDM2/ MDM4inhibitor andp53activator with theIC50values of 70.7 nM for MDM2- p53 and 81.4 nM for MDM4-p53 complexes. MDM2/4-p53-IN-2 regulates the cell cycle, induces cellapoptosisand has anticancer activity[1]. |
体外研究
(In Vitro) | MDM2/4-p53-IN-2 (2q) (1-100 μM, 96 h) can inhibit the proliferation of cancer cells and induce cell apoptosis by targeting the G0/G1 cell cycle in a dose-dependent manner[1].
Cell Proliferation Assay[1] | Cell Line: | Human cancer cell lines HCT116, SJSA-1, MCF-7, LNCaP, human embryonic kidney epithelial cell line HEK 293T | | Concentration: | 1-100 μM | | Incubation Time: | 48 hours | | Result: | Showed anti-proliferative activity of HCT116 with an IC50value of 18.0 μM.
Showed well inhibition of cell viability against SJSA-1, MCF-7, LNCaP cells, all below 40%.
Reduced cell viability of HEK 293T cells by 24%. |
Apoptosis Analysis[1] | Cell Line: | SJSA-1 cell lines | | Concentration: | 15 and 22.5 μM | | Incubation Time: | 96 hours | | Result: | Increased LDH release by 1.3-fold and 1.6-fold at concentrations of 15 μM and 22.5 μM, respectively.
Caused a decrease in SJSA-1 cells, a significant decrease in cell growth and an increase in the number of early and late stage apoptotic cells at 22.5 μM.
Induced a significant accumulation of G0/G1 phase cells with a percentage of 67.5% at 15 μM and 82.2% at 22.5 μM, while reducing the percentage of S and G2/M phase cells. |
|
| 分子量 | |
| Formula | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com