10058-F4
(Synonyms: 5-(4-乙基苯亚甲基)) 目录号 : GC1729510058-F4是一种c-Myc抑制剂,抑制c-Myc-Max二聚化,阻止c-Myc靶基因表达的转录激活。
Cas No.:403811-55-2
Sample solution is provided at 25 µL, 10mM.
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Cell experiment [1]: | |
Cell lines | SKOV3、Hey cells |
Preparation Method | SKOV3 and Hey cells were cultured for 24h and treated with 0-200µM 10058-F4 for 72h. Cell proliferation was assessed using the MTT assay. |
Reaction Conditions | 0-200µM; 72h |
Applications | 10058-F4 inhibited the growth of both cell lines in a concentration-dependent manner, with IC50 values of 4.4µM for SKOV3 cells and 3.2µM for Hey cells. |
Animal experiment [2]: | |
Animal models | C57BL/ 6 mice |
Preparation Method | Colitis was induced in 7-week-old male and female C57BL/ 6 mice by administering 2.5 % DSS in their drinking water for five days. Following DSS treatment, the animals were returned to normal drinking water and allowed to recover for up to four days. For lithium treatments, animals received a single 200µL intraperitoneal injection of 4mg LiCl. For experiments involving MYC inhibition, animals were given 25mg/kg 10058-F4 intraperitoneal injection daily. At each day during recovery, mice were weighed and disease activity index (DAI) scores were assessed. Colonic tissue samples were also collected during each day of the recovery period, fixed in formaldehyde and paraffin-em bedded or stored in a -80 C freezer until analysis. |
Dosage form | 25mg/kg/day; i.p. |
Applications | 10058-F4 inhibited c-MYC transcription factor (MYC) function in lithium-treated mice, reducing the beneficial effects of lithium treatment. Mice that received 10058-F4 alone had severe damage to the colonic epithelium, accompanied by widespread inflammation. |
References: [1]Wang J, Ma X, Jones H M, et al. Evaluation of the antitumor effects of c-Myc-Max heterodimerization inhibitor 100258-F4 in ovarian cancer cells[J]. Journal of translational medicine, 2014, 12: 1-11. [2]Raup-Konsavage W M, Cooper T K, Yochum G S. A role for MYC in lithium-stimulated repair of the colonic epithelium after DSS-induced damage in mice[J]. Digestive diseases and sciences, 2016, 61: 410-422. |
10058-F4 is a c-Myc inhibitor that inhibits c-Myc-Max dimerization and prevents transcriptional activation of c-Myc target gene expression[1]. 10058-F4 can promote caspase-3-dependent apoptosis and regulate autophagy[2]. 10058-F4 has anti-leukemia effects[3].
In vitro, 10058-F4 (0-200µM) treatment of ovarian cancer cell lines (SKOV3 and Hey cells) for 72h inhibited the proliferation of both cell lines in a dose-dependent manner, with IC50 values of 4.4µM and 3.2µML for SKOV3 and Hey cells, respectively, induced cell cycle arrest and apoptosis, and reduced reactive oxygen species (ROS) and ATP generation[4]. 10058-F4 (60μM) treatment of NALM6 and CEM cells for 24h significantly enhanced dexamethasone (DXM)-induced cell growth inhibition, G0/G1 phase arrest and apoptosis[5]. 10058-F4 (0-150μM) treatment of leukemia cells (HL-60, U937 and NB4 cells) for 72h inhibited the proliferation of all three cell types in a dose-dependent manner, induced cell cycle arrest and apoptosis, and myeloid differentiation[6].
In vivo, 10058-F4 (25mg/kg/day) was administered intraperitoneally to mice with acute colitis, which weakened the LiCl-induced colon regeneration effect and reduced the expression of Ccnd2 and Cad[7]. 10058-F4 (15mg/kg) was administered intraperitoneally to mice with PANC-1 cell xenografts for 30 days, 10058-F4 alone had no significant effect on tumorigenesis, but when used in combination with gemcitabine, it significantly attenuated tumorigenesis and reduced PCNA-positive cells and TUNEL-positive cells[8].
References:
[1] Lin C P, Liu J D, Chow J M, et al. Small-molecule c-Myc inhibitor, 10058-F4, inhibits proliferation, downregulates human telomerase reverse transcriptase and enhances chemosensitivity in human hepatocellular carcinoma cells[J]. Anti-cancer drugs, 2007, 18(2): 161-170.
[2] Sheikh‐Zeineddini N, Bashash D, Safaroghli‐Azar A, et al. Suppression of c‐Myc using 10058‐F4 exerts caspase‐3‐dependent apoptosis and intensifies the antileukemic effect of vincristine in pre‐B acute lymphoblastic leukemia cells[J]. Journal of cellular biochemistry, 2019, 120(8): 14004-14016.
[3] Zehtabcheh S, Sheikh‐Zeineddini N, Yousefi A M, et al. Anti-Leukemic Effects of Small Molecule Inhibitor of c-Myc (10058-F4) on Chronic Myeloid Leukemia Cells[J]. Asian Pacific Journal of Cancer Prevention, 2024, 25(6): 1959-1967.
[4] Wang J, Ma X, Jones H M, et al. Evaluation of the antitumor effects of c-Myc-Max heterodimerization inhibitor 100258-F4 in ovarian cancer cells[J]. Journal of translational medicine, 2014, 12: 1-11.
[5] Lv M, Wang Y, Wu W, et al. CMyc inhibitor 10058F4 increases the efficacy of dexamethasone on acute lymphoblastic leukaemia cells[J]. Molecular Medicine Reports, 2018, 18(1): 421-428.
[6] Huang M J, Cheng Y, Liu C R, et al. A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia[J]. Experimental hematology, 2006, 34(11): 1480-1489.
[7] Raup-Konsavage W M, Cooper T K, Yochum G S. A role for MYC in lithium-stimulated repair of the colonic epithelium after DSS-induced damage in mice[J]. Digestive diseases and sciences, 2016, 61: 410-422.
[8] Zhang M, Fan H Y, Li S C. Inhibition of c-Myc by 10058-F4 induces growth arrest and chemosensitivity in pancreatic ductal adenocarcinoma[J]. Biomedicine & pharmacotherapy, 2015, 73: 123-128.
10058-F4是一种c-Myc抑制剂,抑制c-Myc-Max二聚化,阻止c-Myc靶基因表达的转录激活[1]。10058-F4可促进caspase-3依赖的细胞凋亡并调节自噬[2]。10058-F4具有抗白血病作用[3]。
在体外,10058-F4(0-200µM)处理卵巢癌细胞系(SKOV3和Hey细胞)72h,均以剂量依赖性方式抑制了两种细胞增殖,对SKOV3和Hey细胞的IC50值分别为4.4µM和3.2µML,诱导了细胞周期停滞和凋亡,减少了活性氧(ROS)和ATP生成[4]。10058-F4(60μM)处理NALM6和CEM细胞24h,显著增强了地塞米松(DXM)诱导的细胞生长抑制、G0/G1期停滞和凋亡[5]。10058-F4(0-150μM)处理白血病细胞(HL-60、U937和NB4细胞)72h,均以剂量依赖性方式抑制了三种细胞增殖,诱导了细胞周期停滞和凋亡以及骨髓分化[6]。
在体内,10058-F4(25mg/kg/day)通过腹腔注射急性结肠炎治疗小鼠,削弱了LiCl诱导的促进结肠再生作用,降低了Ccnd2和Cad的表达[7]。10058-F4(15mg/kg)通过腹腔注射治疗PANC-1细胞异种移植小鼠30天,10058-F4单独治疗对肿瘤发生没有显著影响,与吉西他滨联合使用时显著减弱了肿瘤发生,减少了PCNA阳性细胞和TUNEL阳性细胞[8]。
Cas No. | 403811-55-2 | SDF | |
别名 | 5-(4-乙基苯亚甲基) | ||
化学名 | (5E)-5-[(4-ethylphenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | ||
Canonical SMILES | CCC1=CC=C(C=C1)C=C2C(=O)NC(=S)S2 | ||
分子式 | C12H11NOS2 | 分子量 | 249.35 |
溶解度 | ≥ 24.9mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mM | 4.0104 mL | 20.0521 mL | 40.1043 mL |
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10 mM | 0.401 mL | 2.0052 mL | 4.0104 mL |
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