SML1421
EPZ015666
≥98% (HPLC)
别名:
(S)-N-（3-（3,4-二氢异喹啉-2 (1H)-基）-2-羟基丙基）-6-（氧杂坦-3-基氨基）嘧啶-4-甲酰胺, GSK3235025, YQ36286
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关于此项目
经验公式（希尔记法）:
C20H25N5O3
化学文摘社编号:
分子量:
383.44
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
EPZ015666, ≥98% (HPLC)
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
SMILES string
O[C@H](CN1CCC(C=CC=C2)=C2C1)CNC(C3=CC(NC4COC4)=NC=N3)=O
InChI key
ZKXZLIFRWWKZRY-KRWDZBQOSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
Quality Level
相关类别
Biochem/physiol Actions
EPZ015666 (GSK3235025) 是一种蛋白质精氨酸甲基转移酶 PRMT5 抑制剂。
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。
Other Notes
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 。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Organoids are in vitro three-dimensional structures that can be grown from patient tissue. Head and neck cancer (HNC) is a collective term used for multiple tumor types including squamous cell carcinomas and salivary gland adenocarcinomas. Organoids were established from HNC patient
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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
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
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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
Pan-methylarginine antibody generation using PEG linked GAR motifs as antigens.
Wang, et al.
Methods, 200, 80-86 (2023)
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