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。
PLK1/BRD4-IN-1
PLK1/BRD4-IN-1 (9b) 是一个具有口服活性的 PLK1 和 BRD4 双重抑制剂，对 PLK1 和 BRD4 的 IC50 值分别为 22 nM 和 109 nM。PLK1/BRD4-IN-1 诱导细胞周期阻滞 (cell cycle arrest) 和凋亡 (apoptosis)，下调几种增殖相关癌基因的转录，并表现出良好的体内抗肿瘤活性。
PLK1/BRD4-IN-1 Chemical Structure
CAS No. : 2412707-81-2
| 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 |
PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity[1].
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| IC50 & Target |
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BRD4
109 nM (IC50)
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PLK1
22 nM (IC50)
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体外研究
(In Vitro) |
PLK1/BRD4-IN-1 (9b) (72 h) shows broad-spectrum antiproliferative activities[1].
PLK1/BRD4-IN-1 (0-9 µM, 24 h) induces cell cycle arrest[1].
PLK1/BRD4-IN-1 (0-9 µM, 48 h) induces cell apoptosis[1].
PLK1/BRD4-IN-1 inhibits the proliferative of cancer cells by exerting its inhibitory activity on both PLK1 and BRD4[1].
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: |
MV4-11, LnCap, HT-29, A375, SKOV-3 |
| Concentration: |
Cells were maintained in RPMI 1640 or DMEM medium supplemented with 10% FBS (v/v) in 5% CO2, except for MV4-11 cells, which were cultured in IMDM medium. |
| Incubation Time: |
72 h |
| Result: |
Showed broad-spectrum antiproliferative activities with IC50 values of 0.13, 0.14, 1.10, 2.82 and 2.51 µM against MV4-11, LnCap, SKOV-3, A375 and HT29 cells, respectively. |
Cell Cycle Analysis[1]
| Cell Line: |
MV4-11 |
| Concentration: |
0.1, 0.3, 1, 3, 9 µM |
| Incubation Time: |
24 h |
| Result: |
Induced obvious G2/M arrest in a concentration-dependent manner |
Apoptosis Analysis[1]
| Cell Line: |
MV4-11 |
| Concentration: |
0.1, 0.3, 1, 3, 9 µM |
| Incubation Time: |
48 h |
| Result: |
Significantly increased the number of Annexin V/PI-positive MV4-11 cells in a concentration-dependent manner. |
RT-PCR[1]
| Cell Line: |
MV4-11 |
| Concentration: |
0.1, 0.3, 1, 3, 9 µM |
| Incubation Time: |
24 h |
| Result: |
Reduced the transcription of c-MYC and MYCN as well as BCL-2, in a concentration-dependent manner. |
Western Blot Analysis[1]
| Cell Line: |
MV4-11 |
| Concentration: |
0.1, 0.3, 1, 3, 9 µM |
| Incubation Time: |
48 h |
| Result: |
Decreased the expression of c-Myc and Bcl-2 in a concentration dependent-manner and upregulated cleaved caspase-3 and cleaved PARP. |
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体内研究
(In Vivo) |
PLK1/BRD4-IN-1 (9b) (60 mg/kg/d; IG; 18 days) results in a significant decrease in average tumor size, with no obvious toxicity[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Five weeks old male NOD-SCID mice[1]. |
| Dosage: |
60 mg/kg/d |
| Administration: |
Oral gavage, 18 days; tumor xenograft models were established by subcutaneously injecting 100 µL of 1×108 cell/mL MV4-11 cell suspension into NOD-SCID mice. |
| Result: |
Resulted in a significant decrease in average tumor size, with 66% tumor growth inhibition, and didn’t obviously affect the body weight of mice. |
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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]. Ning-Yu Wang, et al. Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. Eur J Med Chem. 2020 Apr 1;191:112152.
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