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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
O[C@H](CN1CCC(C=CC=C2)=C2C1)CNC(C3=CC(NC4COC4)=NC=N3)=O
InChI
1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1
InChI 密鑰
ZKXZLIFRWWKZRY-KRWDZBQOSA-N
生化／生理作用
EPZ015666 (GSK3235025) 是一种蛋白质精氨酸甲基转移酶 PRMT5 抑制剂，在生物化学试验中 IC 50 值为 22 nM，在最高试验浓度 50 μM 时对20 种蛋白甲基转移酶的组合无抑制作用。相对于 SAM，抑制作用不具有竞争性。EPZ015666 在多种 体外 和 体内 套细胞淋巴瘤 (MCL) 模型中显示剂量依赖性抗肿瘤活性，处理 MCL 细胞系导致抑制 SmD3 甲基化和细胞死亡。
其他說明
化学探针门户网站已对 EPZ015666 进行了专家评审和推荐。欲了解更多信息，请访问化学探针门户网站上的 EPZ015666 探针摘要 。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Zhengxin Wang et al.
Molecular and cellular biology, 42(4), e0052321-e0052321 (2022-03-22)
Protein arginine methyltransferase (PRMT) enzymes catalyze posttranslational modifications of target proteins and are often upregulated in human cancers. In this study, we purified two chemical compounds from seeds of Foeniculum vulgare based on their ability to inhibit the enzymatic activity
David Shifteh et al.
Cancers, 12(8) (2020-08-01)
Nearly 45% of colorectal cancer (CRC) patients harbor a mutation in their KRAS gene for which, despite many years of research, there are still no targeted therapies available. Protein Arginine Methyltransferase 5 (PRMT5) is a transcription regulator for multiple cellular
Maneka Chitiprolu et al.
Nature communications, 9(1), 2794-2794 (2018-07-20)
Mutations in proteins like FUS which cause Amyotrophic Lateral Sclerosis (ALS) result in the aberrant formation of stress granules while ALS-linked mutations in other proteins impede elimination of stress granules. Repeat expansions in C9ORF72, the major cause of ALS, reduce
Kazuki Fukumoto et al.
Communications biology, 5(1), 313-313 (2022-04-07)
The global dietary supplement market is valued at over USD 100 billion. One popular dietary supplement, S-adenosylmethionine, is marketed to improve joints, liver health and emotional well-being in the US since 1999, and has been a prescription drug in Europe
Edward M Courchaine et al.
Cell, 184(14), 3612-3625 (2021-06-12)
Biomolecular condensation is a widespread mechanism of cellular compartmentalization. Because the "survival of motor neuron protein" (SMN) is implicated in the formation of three different membraneless organelles (MLOs), we hypothesized that SMN promotes condensation. Unexpectedly, we found that SMN's globular
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