| Bioactivity | MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription[1]. |
| Invitro | MEL23 增加 Mdm2(wt)-荧光素酶细胞的发光，EC50 值为 2.7 μg/mL[1]。MEL23（3.16-100 μM；48 小时）导致 p53 依赖性细胞死亡[1]。 MEL23（2.5-5 μg/mL；48 小时）增加了亚 G1 细胞群，并导致 HT-1080 细胞中 G2 细胞周期轻微停滞[1]。MEL23（5 μg/mL；6 小时）增加了 Mdm2、p53 和 MdmX 的水平并激活 p53[1]。MEL23（5 μg/mL；24-48 小时）增加了 p53 靶基因 Mdm2、p21、puma 和 bax 的转录[1]。 在亲本 HT-1080 细胞中，MEL23 抑制 Erastin (HY-15763) 诱导的细胞死亡，并显著降低铁死亡的程度[2]。HT-1080 cells 2.5 μg/mL (7 μM), 5 μg/mL (14 μM)48 hoursIncreased the sub-G1 population and caused a slight G2-cell cycle arrest.U2OS, RKO, and HCT116 cells (p53 wild-type) 5 μg/mL (14 μM)6 hoursIncreased the Mdm2 and p53 levels. RKO cells 5 μg/mL (14 μM)24 hours, 48 hoursIncreased the transcription of p53 target genes, Mdm2, p21, puma, and bax. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> MEL23 相关抗体: Cell Viability Assay[1] Cell Line: |
| CAS | 642072-49-9 |
| Formula | C19H22N4O3 |
| Molar Mass | 354.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Herman AG, et al. Discovery of Mdm2-MdmX E3 ligase inhibitors using a cell-based ubiquitination assay. Cancer Discov. 2011 Sep;1(4):312-25. [2]. Divya Venkatesh, et al. MDM2 and MDMX promote ferroptosis by PPARα-mediated lipid remodeling. Genes Dev. 2020 Apr 1;34(7-8):526-543. |