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DNPH1 inhibitor 38

Chemical Structure : DNPH1 inhibitor 38

CAS No.:

DNPH1 inhibitor 38

货号: PC-25695Not For Human Use, Lab Use Only.

DNPH1 inhibitor 38 is a potent, non-nucleoside inhibitor of 2′-Deoxynucleoside 5′-monophosphate glycosidase (DNPH1, RCL) with binding pIC50 of 9.3, inhibits the hydrolysis of hmdUMP catalyzed by DNPH1 with pIC50 of 9.3.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DNPH1 inhibitor 38 is a potent, non-nucleoside inhibitor of 2′-Deoxynucleoside 5′-monophosphate glycosidase (DNPH1, RCL) with binding pIC50 of 9.3, inhibits the hydrolysis of hmdUMP catalyzed by DNPH1 with pIC50 of 9.3.
DNPH1 inhibitor 38 shows DNPH1 target engagement in the sub 100 nM range (pIC50=7.2).
DNPH1 inhibitor 38 (1 uM) increased DNA-bound hmdU in SUM149PT cells, selectively increases hmdU sensitivity in BRCA1m SUM149PT cells by 5-fold (IC50=0.6 uM), versus wild-type SUM149PT cell lines (IC50=2.7 uM).

物理化学性质&存储条件

分子量 603.58
分子式 C31H25F4N7O2
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

(S)-2'-Fluoro-6-((6-methyl-4-((1-(pyrimidin-5-yl)pyrrolidin-3-yl)amino)quinazolin-2-yl)amino)-3'-(trifluoromethyl)-[1,1'-biphenyl]-3-carboxylic Acid

参考文献

1. Barlaam B, et al. J Med Chem. 2025 Nov 5. doi: 10.1021/acs.jmedchem.5c02356.

2. Rzechorzek NJ, et al. Nat Commun. 2023 Oct 26;14(1):6809.

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