PRMT5 inhibitor 16-19F

Chemical Structure : PRMT5 inhibitor 16-19F

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货号: PC-24714Not For Human Use, Lab Use Only.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

PRMT5 inhibitor 16-19F is a specific synthetic inhibitor of the PRMT5-MTA complex with SPR KD of 2.54, 0.36 and 0.15 uM against apo-PRMT5:MEP50 and SAM- and MTA-bound PRMT5:MEP50 complexes respectively, selectively inhibits MTAP-deleted cancer cell growth.
16-19F preferentially binds to and stabilizes the catalytically inactive PRMT5·MTA complex, which would inhibit PRMT5 activity in MTAP–/– cells while preserving PRMT5 activity in MTAP+ cells.
16-19F demonstrates potent selectivity to MTAP–/– cancer cell lines with IC50 values of 17.8 and 15.7 μM in MDA-MB-231 and MIA PaCa-2, compared to IC50 >100 μM in MDA-MB-435s cells, which SAM-cooperative inhibitor (GSK3326595) shows little cell viability inhibition.
16-19F strongly inhibited PRMT5 coimmunoprecipitated MCM7 sDMA compared to GSK3326595.
16-19F binds to the PRMT5•MTA, PRMT5•SAH, and PRMT5•SAM complexes and selectively inhibited MTAP-deleted cancer cell growth.

物理化学性质&存储条件

分子量	353.81
分子式	C18H16ClN5O
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	8-chloro-1-((2,4-diaminoquinazolin-7-yl)methyl)-3,4-dihydroquinolin-2(1H)-one

参考文献

1. Shen Z, et al. ACS Chem Biol. 2025 May 29. doi: 10.1021/acschembio.5c00160.