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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-IACS-17596
IACS-17596

Chemical Structure : IACS-17596

CAS No.: 2604513-53-1

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IACS-17596 (IACS17596)

货号: PC-25321Not For Human Use, Lab Use Only.

IACS-17596 is a highly potent, selective and SAM-competitive inhibitor of NSD2 (MMSET, WHSC1) with IC50 of 8.8 nM, >300-fold selective over a KMT panel including NSD1, NSD3 and SETD2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IACS-17596 is a highly potent, selective and SAM-competitive inhibitor of NSD2 (MMSET, WHSC1) with IC50 of 8.8 nM, >300-fold selective over a KMT panel including NSD1, NSD3 and SETD2.
IACS-17596 inhibits NSD2 methylation of nucleosome substrates in vitro with IC50 of 8.8 nM.
IACS-17596 also does not show activity against a panel of broad kinase selectivity.
IACS-17596 reduces the viability of a panel of KRAS mutant cell lines with IC50 values ranging from 20 to 300 nM, depletes H3K36me2 levels, also IACS-17596 inhibits colony formation in PDAC cells, high selective over non-cancerous human mesenchymal stem cells (MSCs).
IACS-17596 localizes in both the SAM-binding pocket and the catalytic channel of NSD2.
IACS-17596 induces epigenetic and epigenome-wide reprogramming in PDAC cells, suppresses oncogenic programming through H3K27me3 upregulation at H3K27me3 legacy loci.
IACS-17596  synergizes with Sotorasib to confer sustained survival with extensive tumour regression and elimination.

物理化学性质&存储条件

分子量 513.56
分子式 C27H25F2N9
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)-9-((5-(3-amino-3-(pyridin-2-yl)piperidin-1-yl)-2-(3,4-difluorophenyl)pyridin-4-yl)methyl)-9H-purin-6-amine

参考文献

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

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