上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
MA242
MA242 是特异性的 MDM2 和 NFAT1 双重抑制剂。MA242 以高亲和力直接结合 MDM2 和 NFAT1，诱导 MDM2 和 NFAT1 蛋白降解，并抑制 NFAT1 介导的 MDM2 转录。MA242 在胰腺癌细胞系中诱导凋亡。
MA242 Chemical Structure
CAS No. : 1049704-18-8
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
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IC50 & Target |
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体外研究
(In Vitro) |
MA242 (0.05-5 μM; 72 hours) significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells[1].
MA242 (0.1-0.5 μM; 24 hours) significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines[1].
MA242 decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
MA242 alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity[1].
MA242 exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 shows selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
| Cell Line: |
The human pancreatic cancer HPAC, Panc-1, AsPC-1, Mia-Paca-2 and BxPC-3 cell lines; The human pancreatic ductal epithelium (HPDE) cell line |
| Concentration: |
0.05, 0.5, and 5 μM |
| Incubation Time: |
72 hours |
| Result: |
The IC50s are 0.14, 0.14, 0.15, 0.25, 0.40, and 5.81 μM for Panc-1, Mia-Paca-2, AsPC-1, BxPC-3, HPAC, and HPDE cells, respectively. |
Western Blot Analysis[1]
| Cell Line: |
The human pancreatic cancer HPAC, Panc-1, and AsPC-1 cell lines |
| Concentration: |
0, 0.1, 0.2, and 0.5 μM |
| Incubation Time: |
24 hours |
| Result: |
Decreased the expression of MDM2 and NFAT1. |
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体内研究
(In Vivo) |
MA242 (IP; 2.5, 5, 10 mg/kg) suppresses orthotopic pancreatic tumor growth in vivo, independent of p53[1].
There were no significant differences in the average body weights between the vehicle- and MA242-treated mice in either of the models, did not have significant host toxicity at these effective doses[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Female 4-6-week-old athymic nude mice (nu/nu, 4-6 weeks) bearing AsPC-1-Luc or Panc-1-Luc tumor[1] |
| Dosage: |
2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice |
| Administration: |
IP; 2.5 or 5 mg/kg/d, 5 d/wk for five weeks for Panc-1 tumor-bearing mice;
IP; 10 mg/kg/d, 5 d/wk for three weeks for AsPC-1 tumor-bearing mice |
| Result: |
Resulted in 56.1% and 82.5% inhibition of tumor growth in nude mice bearing Panc-1 orthotopic tumors, respectively.
Significantly suppressed the growth of AsPC-1 orthotopic tumors by 89.5% (P < 0.01) compared with the tumors in control animals.
Led to almost complete tumor regression in MD242-treated mice in both models. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Wang W, et al. Discovery and Characterization of Dual Inhibitors of MDM2 and NFAT1 for Pancreatic Cancer Therapy. Cancer Res. 2018 Oct 1;78(19):5656-5667.
[2]. Wei Wang, et al. MDM2-NFAT1 dual inhibitor, MA242: Effective against hepatocellular carcinoma, independent of p53. Cancer Lett. 2019 Sep 10;459:156-167.
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