| In Vitro |
Anticancer agent 84 has cytotoxicity in cancer cells (HepG2, MDA-MB-231) and normal cells (HBL-100) with IC50 values 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 IC50 values 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 IC50 value of 1.7 μM.
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