TC-E 5003
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货号：A169549
同义名：
NSC 30176
TC-E 5003是一种选择性 PRMT1 抑制剂，对 hPRMT1 的 IC50 为 1.5 µM，还可调节 AP-1 和 NF-κB 信号通路，并具有抗炎特性。
TC-E 5003 化学结构
TC-E 5003 3D分子结构
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TC-E 5003 纯度/质量文件 产品仅供科研
货号：A169549
标准纯度：
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产品说明书
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TC-E 5003 质控信息
TC-E 5003 生物活性
描述
Protein arginine methyltransferase 1 (PRMT1) is a major type 1 arginine methyltransferase associated with the activation of estrogen and androgen receptors; therefore, may represent a therapeutic target for hormone-dependent cancers. TC-E 5003 is an inhibitor of PRMT1 with an IC50 value of 1.5±0.2µM. The GI50 value of TC-E 5003 for the growth of MCF7a and LNCaP cell lines are 1.97 ± 0.14 and 4.49 ± 0.14µM, respectively.[1] [2] [3]
作用机制
TC-E 5003 is a selective inhibitor of PRMT1.[1]
TC-E 5003 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RAW264.7 cells
0-1 µM
15 min
TC-E inhibited c-Jun transcription in RAW264.7 cells after LPS treatment
Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells
0-1 µM
15-30 min
TC-E decreased p-c-Jun levels but did not affect phosphorylated MAPKs
Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells
0-1 µM
15-60 min
TC-E suppressed the nuclear translocation of NF-κB subunits p65 and p50 and AP-1 transcriptional factor c-Jun
Int J Mol Sci. 2020 Apr 26;21(9):3058.
HEK293T cells
0-1 µM
24 hours
TC-E did not alter Src phosphorylation in Src-overexpressing HEK293T cells
Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells
0-1 µM
24 hours
TC-E significantly reduced LPS-induced NO production without cytotoxicity
Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells
0-1 µM
2-5 min
TC-E inhibited Src phosphorylation after 2 min of LPS treatment but not Syk
Int J Mol Sci. 2020 Apr 26;21(9):3058.
MDA-MB-231
0.5965 µM (IC50)
48 hours
Evaluate the anti-tumor effect of TC-E-5003 on MDA-MB-231 cells, IC50 was 0.5965 μM.
Drug Deliv. 2020 Dec;27(1):491-501.
MCF-7
0.4128 µM (IC50)
48 hours
Evaluate the anti-tumor effect of TC-E-5003 on MCF-7 cells, IC50 was 0.4128 μM.
Drug Deliv. 2020 Dec;27(1):491-501.
NCL-H1299
0.6844 µM (IC50)
48 hours
Evaluate the anti-tumor effect of TC-E-5003 on NCL-H1299 cells, IC50 was 0.6844 μM.
Drug Deliv. 2020 Dec;27(1):491-501.
A549
0.7022 µM (IC50)
48 hours
Evaluate the anti-tumor effect of TC-E-5003 on A549 cells, IC50 was 0.7022 μM.
Drug Deliv. 2020 Dec;27(1):491-501.
RAW264.7 cells
0-1 µM
5 min
TC-E significantly downregulated IκBα phosphorylation after 5 min of LPS treatment
Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells
0-1 µM
6 hours
TC-E downregulated the expression of inflammatory genes (iNOS, COX-2, TNF-α, IL-6)
Int J Mol Sci. 2020 Apr 26;21(9):3058.
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TC-E 5003 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
ICR mice
A549 cell xenograft model
Subcutaneous injection
0.5 mg
Single dose, lasting 28 days
Evaluate the anti-tumor effect of TC-E-5003-INEI in A549 xenograft model, tumor inhibition efficiency was 68.23%.
Drug Deliv. 2020 Dec;27(1):491-501.
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TC-E 5003 参考文献
[1] Bissinger EM, Heinke R, Spannhoff A, Eberlin A, Metzger E, Cura V, Hassenboehler P, Cavarelli J, Schüle R, Bedford MT, Sippl W, Jung M. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem. 2011 Jun 15;19(12):3717-31. doi: 10.1016/j.bmc.2011.02.032
[2] Kim E, Jang J, Park JG, Kim KH, Yoon K, Yoo BC, Cho JY. Protein Arginine Methyltransferase 1 (PRMT1) Selective Inhibitor, TC-E 5003, Has Anti-Inflammatory Properties in TLR4 Signaling. Int J Mol Sci. 2020 Apr 26;21(9):3058. doi: 10.3390/ijms21093058
[3] Zhang P, Tao H, Yu L, Zhou L, Zhu C. Developing protein arginine methyltransferase 1 (PRMT1) inhibitor TC-E-5003 as an antitumor drug using INEI drug delivery systems. Drug Deliv. 2020 Dec;27(1):491-501. doi: 10.1080/10717544.2020.1745327
TC-E 5003 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.49mL
0.50mL
0.25mL
12.46mL
2.49mL
1.25mL
24.92mL
4.98mL
2.49mL
TC-E 5003 技术信息
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