Chemical Structure : NUV-244
CAS No.:
NUV-244
(NUV244)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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372.87
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Formula
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C19H17ClN2O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(2-chloro-5-hydroxyphenyl)-4-methyl-2-(3-methylbenzyl)thiazole-5-carboxamide
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References
1. Steigemann P, et al. iScience. 2025 Apr 8;28(5):112384.
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