Structure of Remodelin HBr
CAS No.: 1622921-15-6
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Remodelin hydrobromide is a selective inhibitor of acetyl-transferase protein NAT10.
Synonyms: Remodelin hydrobromide; Remodelin (hydrobromide)
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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CAS No. : | 1622921-15-6 |
Formula : | C15H15BrN4S |
M.W : | 363.28 |
SMILES Code : | N#CC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1.[H]Br |
Synonyms : |
Remodelin hydrobromide; Remodelin (hydrobromide)
|
MDL No. : | MFCD28137688 |
InChI Key : | XNWBCMSPDCSWSD-UHFFFAOYSA-N |
Pubchem ID : | 86280479 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Description |
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].
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In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
mouse cardiomyocytes | 2.5 μM | 24 hours | Remodelin inhibited the proliferation of mouse cardiomyocytes. | PMC10923914 |
HL1 cells | 2.5 μM | 24 hours | Remodelin inhibited the proliferation of HL1 cells. | PMC10923914 |
AC16 cells | 2.5 μM | 24 hours | Remodelin inhibited the proliferation of AC16 cells. | PMC10923914 |
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. | PMC11792579 |
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. | PMC11792579 |
cardiomyocytes | 40 μM | 24 hours | To test the effect of Remodelin on cardiomyocytes | PMC11002668 |
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. | PMC11451012 |
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. | PMC11451012 |
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. | PMC11451012 |
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. | PMC9753290 |
LmnaG609G/G609G mouse skin fibroblasts | 1 µM | 7 days | Remodelin treatment reversed HGPS-induced genomic instability and nuclear shape defects | PMC5923383 |
In Vivo:
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 | PMC5923383 |
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. | PMC9753290 |
C57BL/KaLwRij mice | 5TMM3VT myeloma model | Intraperitoneal injection | 5 mg/kg | Twice weekly | Remodelin significantly extended the survival period of myeloma mice | PMC9366180 |
Mice | apex resection model | intraperitoneal injection | 25 mg/kg/day | daily for 7 consecutive days | Remodelin attenuates neonatal heart regeneration. | PMC10923914 |
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. | PMC10620198 |
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 | PMC11002668 |
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. | PMC11451012 |
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. | PMC11462375 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.75mL 0.55mL 0.28mL |
13.76mL 2.75mL 1.38mL |
27.53mL 5.51mL 2.75mL |
Tags: Remodelin | Histone Acetyltransferase | HATs | HAT | HGPS | telomerase | migration | Remodelin hydrobromide | NAT10 inhibitor | acetyltransferase NAT10 | acetyltransferase | N-acetyltransferase | 1622921-15-6
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