MIRA-1是一种马来酰亚胺类似物,通过恢复p53依赖的转录激活功能,诱导p53突变细胞凋亡,具有显著的抗肿瘤活性,特别适用于p53突变型肿瘤的研究。


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| 产品名称 | p53 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Pifithrin-μ | ✔ | 99%+ | |||||||||||||||||
| Pifithrin-α HBr | ✔ | 98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | MIRA-1 is a maleimide analogue that induces apoptosis in mutant p53 cells by restoring p53-dependent transcriptional activation. MIRA-1 inhibits the growth of Saos-2-His273 cells expressing mutant p53, and possesses anticancer activity. At a concentration of 5 μM for 14 days, MIRA-1 significantly reduced the number of colonies formed by His273-expressing Saos-2 cells, but was much less effective in inhibiting p53-deficient Saos-2 cells. MIRA-1 induced EGFP expression, MDM2 and Bax in SKOV-His175 cells at concentrations of 5 and 10 μM for 24 hours[1]. |
| Concentration | Treated Time | Description | References | |
| Normal PBMCs | 0.2, 2, 20 μM | 72 hours | Normal PBMCs were less sensitive to NSC 19630, with an IC50 of 9.28 ± 0.23 μM. | J Hematol Oncol. 2016 Nov 9;9(1):121 |
| C91PL cells | 0.2, 2, 20 μM | 72 hours | NSC 19630 induced apoptosis in a dose-dependent manner, with an IC50 of 2.76 ± 0.29 μM. | J Hematol Oncol. 2016 Nov 9;9(1):121 |
| ATL-derived cell lines (ED) | 3 μM | 48 hours | NSC 19630 treatment showed significant accumulation of cells in the S-phase when compared with DMSO-exposed cells, suggesting that exposure to the helicase inhibitor induced accumulation of cells in the S-phase in ATL-derived cell lines. | J Hematol Oncol. 2016 Nov 9;9(1):121 |
| HTLV-1-transformed cell lines (MT-4, C8166, C91PL, 1186.94) | 3 μM | 48 hours | NSC 19630 treatment showed significant accumulation of cells in the S-phase when compared with DMSO-exposed cells, suggesting that exposure to the helicase inhibitor induced accumulation of cells in the S-phase in HTLV-1-transformed and ATL-derived cell lines. | J Hematol Oncol. 2016 Nov 9;9(1):121 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
5.46mL 1.09mL 0.55mL |
27.30mL 5.46mL 2.73mL |
54.60mL 10.92mL 5.46mL |
|
| CAS号 | 72835-26-8 |
| 分子式 | C8H9NO4 |
| 分子量 | 183.16 |
| SMILES Code | CCC(OCN1C(C=CC1=O)=O)=O |
| MDL No. | MFCD12828765 |
| 别名 | NSC 19630 |
| 运输 | 蓝冰 |
| InChI Key | YXEWPGYLMHXLPS-UHFFFAOYSA-N |
| Pubchem ID | 227681 |
| 存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 |
| 溶解方案 |
DMSO: 105 mg/mL(573.26 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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