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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-IACS-17817
IACS-17817

Chemical Structure : IACS-17817

CAS No.: 3034213-62-9

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IACS-17817 (IACS17817)

货号: PC-25322Not For Human Use, Lab Use Only.

IACS-17817 is a highly potent, selective and SAM-competitive inhibitor of NSD2 (MMSET, WHSC1) with IC50 of 19.0 nM, >50-fold selective over a KMT panel including NSD1, NSD3 and SETD2.
IACS-17817 inhibits NSD2 methylation of nucleosome substrates in vitro with IC50 of 19.0 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IACS-17817 is a highly potent, selective and SAM-competitive inhibitor of NSD2 (MMSET, WHSC1) with IC50 of 19.0 nM, >50-fold selective over a KMT panel including NSD1, NSD3 and SETD2.
IACS-17817 inhibits NSD2 methylation of nucleosome substrates in vitro with IC50 of 19.0 nM.

物理化学性质&存储条件

分子量 522.56
分子式 C26H28F2N8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-3-amino-1-(4-((8-aminoimidazo[1,2-a]pyrazin-3-yl)methyl)-6-(2,5-difluoro-4-methoxyphenyl)pyridin-3-yl)-N-methylpiperidine-3-carboxamide

参考文献

1. Jeong J, et al. Nature. 2025 Aug 6. doi: 10.1038/s41586-025-09299-y.

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