MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, demonstrates significant antitumor activity[1]. MKT-077 displays low cytotoxicity, inhibiting a wide range of human cancer cell lines including colon cancer, breast cancer, and pancreatic cancer. It also impedes tumor growth in a nude mice engraftment tumor model. Its excitation/emission wavelengths are 488/543 nm[2].
体内研究
Systemic administration of MKT-077 effectively retards the growth of TT xenografts in mice throughout treatment. At the conclusion of MKT-077 treatment, tumor weights are approximately halved compared to the control group. However, MKT-077 treatment also leads to weight loss and general toxicity in animals[1].
Results reveal that the succinate-induced, ADP-stimulated respiratory rate in mitochondria isolated from the livers of rats treated with a bolus i.v. injection of 15 mg MKT-077 per kg body weight each day for 5 days is significantly lower than that of untreated controls[3].
MKT-077 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MCF-7/TAM-R
0.1–100 µM
48 h
To evaluate the cytotoxicity of MKT-077 in breast cancer cells and its synergy with tamoxifen.
Breast Cancer Res. 2024 Feb 26;26(1):33.
T47D/TAM-R
0.1–100 µM
48 h
To evaluate the cytotoxicity of MKT-077 in breast cancer cells and its synergy with tamoxifen.
Breast Cancer Res. 2024 Feb 26;26(1):33.
Huh7.5 cells
0.5, 1, and 5 µM
48 h
MKT077 significantly reduced the production of infectious ZIKV particles, with a 3-log reduction in viral titre for pre-treatment and a 4-log reduction for post-treatment samples.
Emerg Microbes Infect. 2019;8(1):8-16.
HeLa cells
0.35-1.2 μM
24 h
MKT-077 promotes the clearance of hyperphosphorylated tau in a dose-dependent manner.
J Mol Biol. 2011 Aug 19;411(3):614-32.
leukemic clam hemocytes (LCH)
1 to 7 μM
6 to 8 h
disruption of mortalin/p53 binding and translocation of some p53 to the nuclei of cells treated with MKT-077
Am J Pathol. 2006 May;168(5):1526-30.
A375 cells
10 μM
24 h
Evaluate the effect of MKT-077 on apoptosis and autophagy. Results showed that MKT-077 significantly inhibited autophagy, evidenced by SQSTM1 accumulation and increased LC3 II levels.
Cancer Biol Ther. 2014 Feb;15(2):194-9.
H1299 cells
10 μM
24 h
Evaluate the effect of MKT-077 on apoptosis and autophagy. Results showed that MKT-077 significantly inhibited autophagy, evidenced by SQSTM1 accumulation and increased LC3 II levels.
Cancer Biol Ther. 2014 Feb;15(2):194-9.
MZ-CRC-1 cells
0.1 to 10 μM
48 h
MKT-077 suppressed MZ-CRC-1 cell viability at higher doses with an IC50 of 11.4 μM, primarily inducing cell cycle arrest rather than cell death
Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603.
TT cells
0.1 to 10 μM
48 h
MKT-077 significantly reduced TT cell viability with an IC50 of 0.74 μM, inducing cell cycle arrest and cell death
Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603.
MKT-077 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
TT cell xenograft model
Intraperitoneal injection
10 mg/kg
Every 2 days, total 10 doses
MKT-077 significantly suppressed the growth of TT xenografts, reducing tumor weight by approximately two-fold
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