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 :	-
	动物实验配方：

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