NUV-244 | PNPLA3 I148M degrader | Probechem Biochemicals

Chemical Structure : NUV-244

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NUV-244 (NUV244)

货号: PC-24529Not For Human Use, Lab Use Only.

NUV-244 is a potent, specific small molecule degrader of PNPLA3 I148M variant, degrades PNPLA3 I148M via the ubiquitin-proteasome system and involving the E3 ligase BFAR.

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生物&药学活性

NUV-244 is a potent, specific small molecule degrader of PNPLA3 I148M variant, degrades PNPLA3 I148M via the ubiquitin-proteasome system and involving the E3 ligase BFAR.
NUV-244 demonstrates dose-dependent reduction of PNPLA3 I148M-tagRFP on lipid droplets in Huh7 cells with an EC50 of 228 nM, with no effect on PNPLA2 localization to lipid droplets.
NUV-244 dose-dependently leads to a decrease of PNPLA3-tagRFP with a similar potency (EC50=214 nM), does not specifically target mutant PNPLA3.
NUV-244 is active in a wide range of liver-derived cells, including hepatic stellate cells, dose-dependently decreases lipid-droplet associated PNPLA3 I148M-tagRFP.
NUV-244 acts as a molecular glue, leading to 26S-proteasome and E3 ligase BFAR dependent PNPLA3 I148M-tagRFP reduction on lipid droplets and its degradation.

物理化学性质&存储条件

分子量	372.87
分子式	C19H17ClN2O2S
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-(2-chloro-5-hydroxyphenyl)-4-methyl-2-(3-methylbenzyl)thiazole-5-carboxamide

参考文献

1. Steigemann P, et al. iScience. 2025 Apr 8;28(5):112384.

NUV-244 (NUV244)

生物&药学活性

物理化学性质&存储条件

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NUV-244 (NUV244)

生物&药学活性

物理化学性质&存储条件

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