ASS1 activator 1
ASS1 activator 1 (Compound 10f) is a ASS1 activator with an EC50 of 1.90 μM. ASS1 activator 1 enhances the activity of ASS1 and promotes AMPK phosphorylation. ASS1 activator 1 induces cell Apoptosis. ASS1 activator 1 exhibits anticancer activity against triple-negative breast cancer, colorectal cancer and liver cancer.
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- Formule: C41H65N3O9
- Masse moléculaire:743.97
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
ASS1 activator 1 potently activates recombinant ASS1 protein, with an EC50 of 1.90 μM[1].
ASS1 activator 1 (48 h) inhibits the viability of various human cancer cell lines (HT-29, HepG2, MDA-MB-231, T47D, MCF-7, SK-BR-3) with IC50 values ranging from 1.9 to 14.4 μM, while it shows low activity against normal MCF-10A mammary epithelial cells, with an IC50 of 28.5 μM[1].
ASS1 activator 1 (2-8 μM; 24 h) inhibits the migration of MDA-MB-231 triple-negative breast cancer cells in a concentration-dependent manner[1].
ASS1 activator 1 (5 μM; incubated at 37 °C until equilibrium is reached) shows a high plasma protein binding rate, with a binding rate of 98.3% in human plasma and 96.3% in rat plasma at 5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231
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Concentration:2 μM, 4 μM, 8 μM
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Incubation Time:18 h
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Result:Upregulated p-AMPK levels in a concentration-dependent manner without affecting total AMPK or ASS1 levels.
Decreased SQSTM/p62 levels and increased LC3B-II levels, indicating increased autophagic flux.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-t | AUC0-∞ | CL | Vz | Vss | MRT0-∞ | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 263 ± 34.3 ng/mL | 0.10 ± 0.00 h | 6.32 ± 0.34 h | 619 ± 79.6 ng·h/mL | 654 ± 86.3 ng·h/mL | 1.55 ± 0.21 L/h/kg | 14.1 ± 1.37 L/kg | 10.0 ± 1.30 L/kg | 6.47 ± 0.25 h | / |
| Rat[1] | 5 mg/kg | p.o. | 53.5 ± 3.61 ng/mL | 4.0 ± 0.00 h | 5.00 ± 0.69 h | 538 ± 30.8 ng·h/mL | 562 ± 41.1 ng·h/mL | / | / | / | 7.89 ± 0.72 h | 17.4 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 4−6 weeks old)[1]
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Dosage:5 mg/kg
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Administration:intraperitoneally; every other day; 23 days
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Result:Reduced final tumor weights and tumor volumes significantly compared to vehicle control.
Decreased Ki67-positive cells (cell proliferation marker) significantly in tumor tissue relative to controls.
Increased LC3B levels (autophagy marker) significantly in tumor tissue relative to controls.
Caused no significant changes in mouse body weight.
Showed no pathological changes in major organs (heart, liver, spleen, lung, kidney) via H&E staining, indicating no apparent systemic toxicity.
Chemical Information
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Masse moléculaire 743.97
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Formule C41H65N3O9
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SMILES
C[C@@H]1O[C@@H](O[C@@H]2C[C@]3(C=C[C@]4([C@@]([H])(C(C5=O)=C[C@]4([C@@]3(C2)[H])[H])CC(O[C@H](CCC/C([C@H]5C)=N\OCCCCN6CCNCC6)CC)=O)[H])[H])[C@H](OC)[C@H](OC)[C@H]1OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ASS1 activator 1 Related Classifications
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