DUN'058 (DUN058) | PIKfyve inhibitor | Probechem Biochemicals

Chemical Structure : DUN058

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DUN058 (DUN'058, DUN-058)

货号: PC-28767Not For Human Use, Lab Use Only.

DUN'058 (DUN058) is a selective CNS-penetrant covalent inhibitor of PIKfyve with IC50 of <2.5 nM and 39 nM for PIKfyve WT and PIKfyve C1970A in ADP-Glo assays respectively, specifically modifies PIKfyve C1970.

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生物&药学活性

DUN'058 (DUN058) is a selective CNS-penetrant covalent inhibitor of PIKfyve with IC50 of <2.5 nM and 39 nM for PIKfyve WT and PIKfyve C1970A in ADP-Glo assays respectively, specifically modifies PIKfyve C1970.
DUN'058 exhibits potent reversible binding with Ki of 55 nM and moderate covalent efficiency with kinact = 5.8 × 10-4 s-1.
DUN'058 engages C1970 in cells and tissue homogenates and impacts on-target downstream pathways.
DUN'058 decreases TFEB S211 phosphorylation in SU-DHL-6 cells with IC50 of 116 nM after 2 h of compound treatment.
DUN'058 treatment resulted in a dose-dependent increase in the number of both CD63- and CD81-positive exosomes in cultured iPSC-derived hMN.
DUN'058 achieves sustained target occupancy (TO) in the brains of dosed mice.

物理化学性质&存储条件

分子量	490.58
分子式	C27H31FN6O2
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	(4-((2-((3-fluoro-4-methylphenyl)amino)pyrimidin-4-yl)(2-methoxyethyl)amino)piperidin-1-yl)(2-vinylpyridin-4-yl)methanone

参考文献

1. Antony J Burton, et al. ACS Chem Biol. 2026 Nov 6. doi: 10.1021/acschembio.6c00795.

DUN058 (DUN'058, DUN-058)

生物&药学活性

物理化学性质&存储条件

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DUN058 (DUN'058, DUN-058)

生物&药学活性

物理化学性质&存储条件

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