Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells.Additionally, Remodelin curtails the development of prostate cancer and hepatocellular carcinoma in xenograft models and prolongs the lifespan in models of Hutchinson-Gilford Progeria Syndrome (HGPS)[1].[2].[3].[4].
体外研究
When applied in concentrations ranging from 10 to 40 μΜ over a period of 1 to 7 days, Remodelin systematically diminishes NAT10 activity and cell growth in a concentration-responsive manner across both AR-positive and AR-negative prostate cancer cell types[2].
At a dosage of 20 μΜ for a duration of 24 hours, it specifically reduces NAT10 activity and decelerates DNA synthesis in prostate cancer cells[2].
Moreover, a 7-day treatment with Remodelin at 1 μΜ lessens nuclear abnormalities and bolsters genomic integrity in LmnaG609G/G609G fibroblasts[3].
Intraperitoneal injection (i.p.), once every two days for 4 weeks, Remodelin significantly reduced AR-negative prostate cancer tumor growth in PC-3 cells tumor xenograft model in nude athymic BALB/c nu/nu mice[2].
Remodelin HBr 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HL1 cells
2.5 µM
24 hours
Remodelin inhibited the proliferation of HL1 cells.
Nat Commun. 2024 Mar 8;15(1):2137.
AC16 cells
2.5 µM
24 hours
Remodelin inhibited the proliferation of AC16 cells.
Nat Commun. 2024 Mar 8;15(1):2137.
Cardiomyocytes
40 µM
24 hours
To test the effect of Remodelin on cardiomyocytes
Redox Biol. 2024 Jun;72:103145.
Mouse cardiomyocytes
2.5 µM
24 hours
Remodelin inhibited the proliferation of mouse cardiomyocytes.
Nat Commun. 2024 Mar 8;15(1):2137.
SW620
20 µM
24 hours
To evaluate the inhibitory effect of Remodelin on CRC cell proliferation, the results showed that Remodelin significantly inhibited the proliferation of SW620 and SW48 cells.
J Exp Clin Cancer Res. 2025 Feb 4;44(1):37.
SW48
20 µM
24 hours
To evaluate the inhibitory effect of Remodelin on CRC cell proliferation, the results showed that Remodelin significantly inhibited the proliferation of SW620 and SW48 cells.
J Exp Clin Cancer Res. 2025 Feb 4;44(1):37.
4T1 cells
70 µM
24 hours
To investigate the effect of Remodelin on the migration of 4T1 cells, results showed that Remodelin significantly inhibited the migration of 4T1 cells.
J Exp Clin Cancer Res. 2024 Oct 4;43(1):278.
BT549 cells
70 µM
24 hours
To investigate the effect of Remodelin on the migration of BT549 cells, results showed that Remodelin significantly inhibited the migration of BT549 cells.
J Exp Clin Cancer Res. 2024 Oct 4;43(1):278.
MDA-MB-468 cells
70 µM
24 hours
To investigate the effect of Remodelin on the migration of MDA-MB-468 cells, results showed that Remodelin significantly inhibited the migration of MDA-MB-468 cells.
J Exp Clin Cancer Res. 2024 Oct 4;43(1):278.
SW480 cells
20 µM
48 hours
Remodelin inhibited the binding of NAT10 to KIF23 mRNA and reduced the expression of KIF23 and β-catenin, thereby suppressing the proliferation, migration, and invasion of SW480 cells.
J Exp Clin Cancer Res. 2022 Dec 15;41(1):345.
LmnaG609G/G609G mouse skin fibroblasts
1 µM
7 days
Remodelin treatment reversed HGPS-induced genomic instability and nuclear shape defects
Nat Commun. 2018 Apr 27;9(1):1700.
Remodelin HBr 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
LmnaG609G/G609G mouse model
Oral
100 mg/kg
Daily from 3 weeks of age until the endpoint
Remodelin significantly delayed age-dependent weight loss and improved cardiovascular pathology in HGPS mice
Nat Commun. 2018 Apr 27;9(1):1700.
Mice
Cardiac ischemia-reperfusion injury model
Oral gavage
100 mg/kg
Once daily for 7 days
To evaluate the protective effect of Remodelin on cardiac ischemia-reperfusion injury
Redox Biol. 2024 Jun;72:103145.
BALB/c Nude mice
Xenograft tumor models and metastasis models
Oral or intraperitoneal
100 mg/kg (oral) or 5 mg/kg (intraperitoneal)
Once daily for 15 days (oral) or every other day for 4 weeks (intraperitoneal)
Remodelin significantly inhibited the growth of xenograft tumors and the metastasis of SW480 cells to the lungs or liver.
J Exp Clin Cancer Res. 2022 Dec 15;41(1):345.
C57BL/6 mice
High-fat diet-induced MASLD model
Intraperitoneal injection
20 mg/kg
Once daily for 16 days
Remodelin significantly ameliorated high-fat diet-induced liver steatosis and dyslipidemia, reducing liver inflammation and fibrosis.
Mol Metab. 2024 Nov;89:102030
Mice
Apex resection model
Intraperitoneal injection
25 mg/kg/day
Daily for 7 consecutive days
Remodelin attenuates neonatal heart regeneration.
Nat Commun. 2024 Mar 8;15(1):2137.
Balb/c mice
4T1 tumor model
Intraperitoneal injection
3 mg/kg
Every four days until the end of the experiment
To investigate the effect of Remodelin on 4T1 tumor growth, results showed that Remodelin significantly inhibited tumor growth and lung metastasis.
J Exp Clin Cancer Res. 2024 Oct 4;43(1):278.
C57BL/KaLwRij mice
5TMM3VT myeloma model
Intraperitoneal injection
5 mg/kg
Twice weekly
Remodelin significantly extended the survival period of myeloma mice
Acta Pharm Sin B. 2022 Aug;12(8):3313-3325
C57BL/6 mice
4-NQO-induced OSCC mouse model
Intraperitoneal injection
5 mg/kg
Once every two days for 4 weeks
Remodelin significantly inhibited HNSCC tumorigenesis and prolonged the overall survival of mice.
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