货号	规格	价格	上海	北京	珠海	重庆	武汉
S89228-5mg买3赠1	98.30%	￥400.00 S89228-5mg ￥400.00 现货（买3赠1）	5 5	-	-	-	-
S89228-10mg买3赠1	98.30%	￥600.00 S89228-10mg ￥600.00 现货（买3赠1）	5 5	-	-	-	-
S89228-25mg促销	98.30%	￥1220.00 ￥976.00 S89228-25mg ￥976.00 现货	6 6	-	-	-	-
S89228-100mg促销	≥98%	￥3670.00 ￥2930.00 S89228-100mg ￥2930.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

EN4 是靶向 MYC 的半胱氨酸171(C171)的共价配体，相对于N-MYC和L-MYC对 c-MYC 具有选择性。EN4 可抑制MYC转录活性、下调MYC靶标，并损害肿瘤发生

靶点：

MYC;c-Myc

体外研究：

EN4 directly targets MYC in cells, reduces MYC and MAX thermal stability, inhibits MYC transcriptional activity, downregulates multiple MYC transcriptional targets, and impairs tumorigenesis. EN4 treatment significantly impairs 231MFP breast cancer cell proliferation in a dose- and time-dependent manner. EN4 impairs the cell survival of MYC transformed mammary epithelial MCF10A cells, but not parental MCF10A cells that are not dependent on MYC

体内研究：

EN4 treatment initiated after establishment of a 231MFP breast tumor xenograft in immune-deficient mice also significantly attenuates tumor growth in vivo

细胞实验：

Cell lines: 231MFP, MDA-MB-231, HEK293T and MCF10A cells Concentrations: 50 μM Incubation Time: 24 h Method: 231MFP cells are seeded into 6 cm dishes and cells are treated with DMSO vehicle or EN4 (50 μM) for 24 h. Cells are harvested by scraping and RNA is isolated using Qiagen RNeasy mini kit with Qiagen DNase max kit to remove any DNA contamination. mRNA is enriched for using Oligo dT beads from the KAPA mRNA Capture Kit.

动物实验：

Animal Models: C.B17 SCID female mice (6-8 weeks old) Dosages: 50 mg/kg Administration: IP

参考文献：

1. Lydia Boike, et al. Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC. Cell Chem Biol. 2021 Jan 21;28(1):4-13.e17.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.401 ml	12.006 ml	24.011 ml
5 mM	0.48 ml	2.401 ml	4.802 ml
10 mM	0.24 ml	1.201 ml	2.401 ml
50 mM	0.048 ml	0.24 ml	0.48 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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EN4 MYC inhibitor