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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MNK-NSP-1047
NSP-1047

Chemical Structure : NSP-1047

CAS No.: 2458263-58-4

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NSP-1047 (NSP1047)

货号: PC-26315Not For Human Use, Lab Use Only.

NSP-1047 is a potent, selective inhibitor of MAPK-interacting kinases MNK1 and MNK2 with IC50 of 0.5 nM and 0.1 nM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

NSP-1047 is a potent, selective inhibitor of MAPK-interacting kinases MNK1 and MNK2 with IC50 of 0.5 nM and 0.1 nM respectively.
NSP-1047 demonstrates remarkable in vitro inhibition of eIF4E phosphorylation with IC50 of 0.2 nM in OCI-Ly7 cells.
NSP-1047 binds to the ATP active site of MNK2.
NSP-1047 exhibits good kinase selectivity against a panel of 211 kinases at 0.5 uM.
NSP-1047 effectively inhibits the expression of various immune checkpoint proteins in vitro, including PD-1, LAG-3, TIM-3, CTLA-4 and VISITA, while also reducing the expression of pro-inflammatory cytokines such as IFN-γ, IL-8 and TNF-α.
NSP-1047 displays inhibitory effects across 14 AML tumor cell lines with IC50 values of <1 uM in MV-4-11, Molm-13, KASUMI-1, and OCI-AML-1 cell lines.
NSP-1047 exhibits significant antitumor activity in animal models, particularly in combination with low doses of Ara-C (cytarabine) or with venetoclax.

物理化学性质&存储条件

分子量 419.49
分子式 C23H25N5O3
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

N-(12'-Methyl-1',5'-dioxo-2',5',6',11'-tetrahydro-1'H-spiro[cyclohexane-1,3'-imidazo[1',5':1,6]pyrido[3,4-b][1,6]naphthyridin]-8'-yl)cyclopropanecarboxamide

参考文献

1. Bing Li, et al. J Med Chem. 2025 Aug 14;68(15):15617-15635.

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