TC-E 5003

产品说明书

Print
Chemical Structure| 17328-16-4 同义名 : NSC 30176
CAS号 : 17328-16-4
货号 : A169549
分子式 : C16H14Cl2N2O4S
纯度 : 98%+
分子量 : 401.26
MDL号 : MFCD00028183
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(299.05 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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] TC-E 5003 at concentrations of 0.125 – 1µM dose-dependently suppressed lipopolysaccharide-induced nitric oxide (NO) production in RAW264.7 cells. Treatment with TC-E 5003 also markedly reduced the expressions of inducible NO synthase, cyclooxygenase-2, tumor necrosis factor-α, interleukin (IL)-1β, and IL-6, and downregulated the nuclear translocation of nuclear factor kappa B subunits.[2] TC-E-5003 at a dose of 0.5mg exerted an anti-tumor effect (31.76%) in A549 tumor-bearing mice.[3]
作用机制 TC-E 5003 is a selective inhibitor of PRMT1.[1]
实验方案
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
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