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。
ZMF-10
ZMF-10 是一种高效的 PAK1 抑制剂，对 PAK1、PAK2 和 PAK3 的 IC50 分别为 174 nM、1.038 μM 和 1.372 μM。ZMF-10 可抑制 PAK1 活性，影响 MDA-MB-231 细胞中 PAK1 调控的细胞凋亡 (apoptosis)、内质网应激和迁移。ZMF-10 可用于抗癌研究。
ZMF-10 Chemical Structure
CAS No. : 2415295-37-1
| 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 |
ZMF-10 is a highly potent PAK1 inhibitor, with IC50s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer[1].
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| IC50 & Target[1] |
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PAK1
174 nM (IC50)
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PAK2
1.038 μM (IC50)
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PAK3
1.372 μM (IC50)
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体外研究
(In Vitro) |
ZMF-10 (0-10 μM; 48 hours) exhibits potent antiproliferative activity in a dose-dependent manner[1].
ZMF-10 (20 μM; 24 hours) suppresses the phosphorylation of PAK1 at Ser199 and Thr212[1].
ZMF-10 (10-40 μM; 24 hours) downregulates the expression of ERK, and suppresses the phosphorylation of c-Raf, MEK and ERK; up-regulates the expression of Bax and downregulates the expression of Bcl-2; induces apoptosis in a dose-dependent manner with the increase of early and late apoptotic cell population[1].
ZMF-10 (10-40 μM; 24 hours) inhibits the PI3K-AKT-mTOR signaling with the decreasing phosphorylation of AKT and mTOR; inhibits JNK1/2 and cells migration in MDA-MB-231 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
| Cell Line: |
MDA-MB-231[1] |
| Concentration: |
0-10 μM |
| Incubation Time: |
48 hours |
| Result: |
Exhibited potent antiproliferative activity in a dose-dependent manner with an IC50 value of 3.48 μM. |
Immunofluorescence
| Cell Line: |
MDA-MB-231[1] |
| Concentration: |
20 μM |
| Incubation Time: |
24 hours |
| Result: |
Suppressed the phosphorylation of PAK1 at Ser199 and Thr212. |
Western Blot Analysis
| Cell Line: |
MDA-MB-231[1] |
| Concentration: |
10, 20 and 40 μM |
| Incubation Time: |
24 hours |
| Result: |
Downregulated the expression of ERK, and suppressed the phosphorylation of c-Raf, MEK and ERK; up-regulated the expression of Bax and downregulated the expression of Bcl-2. |
Apoptosis Analysis
| Cell Line: |
MDA-MB-231[1] |
| Concentration: |
10, 20 and 40 μM |
| Incubation Time: |
24 hours |
| Result: |
Induced apoptosis in a dose-dependent manner with the increase of early and late apoptotic cell population. |
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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]. Zhang J, et al. Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells. Eur J Med Chem. 2020;194:112220.
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