NUV-244
NUV-244 is a molecular glue degrader of PNPLA3 I148M. NUV-244 induces degradation via the ubiquitin-proteasome system involving the E3 ligase BFAR. NUV-244 promotes 26S proteasome-dependent degradation of PNPLA3 I148M. NUV-244 restores lipid droplet morphology and cellular fitness in hepatocytes expressing PNPLA3 I148M. NUV-244 can be used in the research of metabolic dysfunction-associated fatty liver disease.
For research use only. We do not sell to patients.
- Formula: C19H17ClN2O2S
- Molecular Weight:372.87
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PNPLA3 I148M |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
228 nM
|
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
365 nM
|
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
302 nM
|
Restoration of normal lipid droplet morphology and dispersion in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
Restoration of normal lipid droplet morphology and dispersion in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
525 nM
|
Restoration of normal lipid droplet morphology and dispersion in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
Restoration of normal lipid droplet morphology and dispersion in Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content immunofluorescence imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
214 nM
|
Reduction of PNPLA3 WT-tagRFP signal at lipid droplets in Huh7 cells expressing PNPLA3 WT-tagRFP by immunofluorescence imaging assay after 24 h incubation.
Reduction of PNPLA3 WT-tagRFP signal at lipid droplets in Huh7 cells expressing PNPLA3 WT-tagRFP by immunofluorescence imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
124 nM
|
Reduction of untagged PNPLA3 I148M signal at lipid droplets in Huh7 cells expressing untagged PNPLA3 I148M by immunofluorescence imaging assay after 24 h incubation.
Reduction of untagged PNPLA3 I148M signal at lipid droplets in Huh7 cells expressing untagged PNPLA3 I148M by immunofluorescence imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
257 nM
|
Reduction of untagged PNPLA3 WT signal at lipid droplets in Huh7 cells expressing untagged PNPLA3 WT by immunofluorescence imaging assay after 24 h incubation.
Reduction of untagged PNPLA3 WT signal at lipid droplets in Huh7 cells expressing untagged PNPLA3 WT by immunofluorescence imaging assay after 24 h incubation.
|
40322074 |
| HepG2 | EC50 |
296 nM
|
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in HepG2 cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in HepG2 cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
|
40322074 |
| Hep3B | EC50 |
40 nM
|
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in Hep3B cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in Hep3B cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
|
40322074 |
| LX-2 | EC50 |
188 nM
|
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in LX-2 hepatic stellate cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in LX-2 hepatic stellate cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
289 nM
|
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in oleic acid-treated Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
Reduction of PNPLA3 I148M-tagRFP signal on lipid droplets in oleic acid-treated Huh7 cells stably expressing PNPLA3 I148M-tagRFP by high-content imaging assay after 24 h incubation.
|
40322074 |
| Huh-7 | EC50 |
199 nM
|
Reduction of total PNPLA3 I148M-HiBiT levels in Huh7 cells stably expressing PNPLA3 I148M-HiBiT by HiBiT luminescence quantification assay after 24 h incubation.
Reduction of total PNPLA3 I148M-HiBiT levels in Huh7 cells stably expressing PNPLA3 I148M-HiBiT by HiBiT luminescence quantification assay after 24 h incubation.
|
40322074 |
In Vitro
NUV-244 (1 μM; 24 h) significantly reduces the levels of PNPLA3I148M on lipid droplets and restores normal lipid droplet morphology in Huh7 cells stably expressing PNPLA3 I148M‑tagRFP[1].
NUV-244 (24 h) significantly reduces the levels of lipid droplet-associated untagged PNPLA3 I148M and untagged wild-type PNPLA3 in Huh7 cells, indicating that its activity does not depend on the presence of the tagRFP fusion tag[1].
NUV-244 (24 h) exhibits activity in multiple liver-derived cell lines, including hepatocellular carcinoma cells and hepatic stellate cells, and retains equivalent potency in cells treated with Oleic acid (HY-N1446) to induce lipid droplet accumulation[1].
NUV-244 (24 h) effectively degrades total intracellular PNPLA3I148M and total PNPLA3 wild-type protein in viable Huh7 cells, confirming that the observed reduction of PNPLA3 signal at lipid droplets corresponds to complete degradation of this protein[1].
NUV-244 (1-5 μM; 0-20 h) triggers a rapid reduction of PNPLA3I148M on lipid droplets in Huh7 cells within 2 hours of administration, with the reduction approaching half of the maximum value[1].
NUV-244 (25 μM) directly and selectively binds to purified PNPLA3 WT and PNPLA3 I148M proteins in a cell-free assay, and no interaction with PNPLA2 is detected[1].
NUV-244 (24 h) effectively reduces the PNPLA3I148M protein level in differentiated adipocytes, with an EC50 of 2.02 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Huh7 cells stably expressing PNPLA3 I148M-tagRFP
-
Concentration:1, 5 μM
-
Incubation Time:0-20 h
-
Result:Induces rapid reduction of PNPLA3 I148M-tagRFP intensity on lipid droplets, reaching half-maximal effect at approximately 2 hours post-incubation.
Chemical Information
-
Molecular Weight 372.87
-
Formula C19H17ClN2O2S
-
SMILES
CC1=CC(CC2=NC(C)=C(C(NC3=CC(O)=CC=C3Cl)=O)S2)=CC=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)