Anticancer agent 84 是抗癌剂。Anticancer agent 84 通过稳定 G-四链体 (G4) 结构来抑制 c-MYC 的转录。Anticancer agent 84 可用于癌症研究。
| 生物活性 | Anticancer agent 84 is ananticanceragent. Anticancer agent 84 represses the transcription ofc-MYCby stabilizing theG-quadruplex(G4) structure. Anticancer agent 84 can be used for the research ofcancer[1]. |
| IC50& Target | IC50: 5.0 μM (HepG2); 3.9 μM (MDA-MB-231); ＞100 μM (HBL-100)[1] |
体外研究
(In Vitro) | Anticancer agent 84 has cytotoxicity in cancer cells (HepG2, MDA-MB-231) and normal cells (HBL-100) with IC50values of 5.0 μM, 3.9 μM and ＞100 μM, respectively[1].
Anticancer agent 84 displays good c-MYC G4 binding and stabilization abilities[1].
Anticancer agent 84 blocks c-MYC transcription by targeting the promoter G4, leading to c-MYC-dependent cancer cell death in triple-negative breast cancer cell MDA-MB-23[1].
Anticancer agent 84 (2 μM) significantly disrupts the binding of the three proteins (NM23-H2, BLM and DHX36) to c-MYC G4 with IC50values of 0.16 μM, 2.3 μM and 7.0 μM, respectively[1].
Anticancer agent 84 (0-5 μM) impacts c-MYC-related events in TNBC, including proliferation, invasion, cell cycle, and apoptosis[1].
Western Blot Analysis[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 1.25, 2.5, 5 μM | | Incubation Time: | 48 h | | Result: | Decreased the mRNA levels of c-MYC. |
Cell Cycle Analysis[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 1.25, 2.5, 5 μM | | Incubation Time: | 24 h | | Result: | Could arrest MDA-MB-231 cells at the Sub G0 phase. |
Apoptosis Analysis[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 1.25, 2.5, 5 μM | | Incubation Time: | 24 h | | Result: | Induced early apoptosis and necrosis in MDA-MB-231 cells. |
RT-PCR[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 1.25, 2.5 μM | | Incubation Time: | 24 h | | Result: | Exhibited relatively weak effects on other genes and suppressed c-MYC transcription by targeting c-MYC G4. |
Cell Cytotoxicity Assay[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | | | Incubation Time: | 48 h | | Result: | Displayed good cytotoxicity against various cancer cells, including MDA-MB-231, MCF-7, HepG2, and SiHa and displayed less cytotoxicity against normal HBL-100 and NCM460 cells. |
Cell Proliferation Assay[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 1.25, 2.5, 5 μM | | Incubation Time: | 10 days | | Result: | Exhibits good antiproliferative activity. |
Cell Invasion Assay[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 1.25, 2.5, 5 μM | | Incubation Time: | 24 h | | Result: | Obviously decreased the invasion with an IC50value of 1.7 μM. |
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体内研究
(In Vivo) | Anticancer agent 84 (i.p.; 2.5 mg/kg; daily; for 24 days) significantly inhibits tumor growth in the MDAMB-231 mouse xenograft model accompanied by c-MYC downregulation[1].
| Animal Model: | BALB/C-nu/nu mice(female, five-week-aged, 10–12 g)[1]
| | Dosage: | 2.5 mg/kg | | Administration: | intraperitoneally, daily, for 24 days | | Result: | Exhibited potent antitumor activity and could act as a c-MYC repressor in vivo. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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