10058-F4
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
10058-F4是一种新型的c-Myc小分子抑制剂。10058-F4阻止c-Myc/Max二聚体与其DNA靶标的结合,抑制白血病细胞增殖,诱导细胞通过线粒体途径的凋亡,如Bcl-2的下调、Bax的上调及胞质细胞色素C的释放[1]。
10058-F4阻止c-Myc/Max的二聚化,其是转录因子c-Myc的活性所必须的。10058-F4有效抑制HRG和IGF-1对PGC-1β mRNA和蛋白水平的诱导,表明这些生长因子对PGC-1β蛋白的诱导是一种转录事件,需要c-Myc活性的参与[2]。在淋巴瘤细胞中,10058-F4不仅通过c-Myc/Max异二聚体解离的机制阻断c-Myc的功能,还导致c-Myc mRNA水平的下降(65%,n = 3)[3]。
参考文献:
[1] Huang MJ, Cheng YC, Liu CR, Lin SF, Liu H. E. A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia. Experimental Hematology. 2006; 34: 1480–1489.
[2] Ching-yi Chang, Dmitri Kazmin, Jeff S. Jasper, Rebecca Kunder, William J. Zuercher, Donald P. McDonnell. The Metabolic Regulator ERRα, a Downstream Target of HER2/IGF-1R, as a Therapeutic Target in Breast Cancer. Cancer Cell. 18 October 2011. 20(4): 500-510.
[3] Ilsa Gomez-Curet, R. Serene Perkins, Ryan Bennett, Katherine L. Feidler, Stephen P. Dunn, Leslie J. Krueger. c-Myc inhibition negatively impacts lymphoma growth. Journal of Pediatric Surgery. January 2006. 41(1): 207-211.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 249.35 |
Cas No. | 403811-55-2 |
Formula | C12H11NOS2 |
Solubility | ≥24.9 mg/mL in DMSO; insoluble in H2O; ≥2.64 mg/mL in EtOH |
Chemical Name | (5E)-5-[(4-ethylphenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one |
SDF | Download SDF |
Canonical SMILES | CCC1=CC=C(C=C1)C=C2C(=O)NC(=S)S2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
HL-60、U937和NB-4细胞 |
制备方法 |
在DMSO中的溶解度大于12.5 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
0、30、60、100和150 μM;72小时 |
实验结果 |
10058-F4呈剂量依赖性地作用于所有AML细胞系(HL-60、U937和NB-4)。在100 μM的剂量下,经72小时处理后,10058-F4显著诱导AML细胞凋亡。此外,在所有AML细胞系中,10058-F4降低了c-Myc蛋白水平。 |
动物实验 [2]: | |
动物模型 |
携带DU145或PC-3人类前列腺癌异种移植物的SCID小鼠 |
给药剂量 |
20或30 mg/kg;静脉注射;每日1次,每周5日,持续2周 |
实验结果 |
在携带PC-3异种移植物的小鼠中,静脉注射20或30 mg/kg 10058-F4,最大平均%TC值分别为72.3%和72.9%。相似地,在携带DU145异种移植物的小鼠中,30mg/kg 10058-F4相应的最大平均%TC值为85%。在上述2个模型中,10058-F4效果微弱。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Huang MJ, Cheng YC, Liu CR, Lin SF, Liu H. E. A small-molecule c-Myc inhibitor, 10058-F4, induces cell-cycle arrest, apoptosis, and myeloid differentiation of human acute myeloid leukemia. Experimental Hematology. 2006; 34: 1480–1489. [2]. Guo J, Parise RA, Joseph E, Egorin MJ, Lazo JS, Prochownik EV, Eiseman JL. Efficacy, pharmacokinetics, tisssue distribution, and metabolism of the Myc-Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice. Cancer Chemother Pharmacol. 2009 Mar;63(4):615-25. |
描述 | 10058-F4是一种细胞通透性的c-Myc-Max二聚化小分子抑制剂。 | |||||
靶点 | c-Myc-Max dimerization | |||||
IC50 |
质量控制和MSDS
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