VARS1-IN-1
VARS1-IN-1 is a valyl-tRNA synthetase (VARS1) inhibitor with a Kd of 0.213 μM. VARS1-IN-1 suppresses VARS1’s tRNA aminoacylation activity, reduces charged levels of valine tRNAs and redues total protein synthesis rate. VARS1-IN-1 suppresses aggressive tumor growth and cell proliferation in PC3 prostate cancer xenograft models. VARS1-IN-1 can be used for the research of prostate cancer.
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- CAS No.: 428830-84-6
- Formule: C21H15N5OS
- Masse moléculaire:385.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
VARS1-IN-1 (Compound 2701) (10 µM; 2 days) interfers VARS1’s tRNA aminoacylation activity but not its expression with a reduction in charged to total tRNA-Val ratio in prostate cancer cells[1].
VARS1-IN-1 (10 µM; 2 days) redues total protein synthesis rate in PC3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu nude mice with PC3 xenograft (male, 6-7 weeks old)[1]
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Dosage:15 mg/kg
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Administration:i.p.; once every other day for 20 days
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Result:Inhibited tumor growth with significant reduction in tumor weight compared to DMSO control.
Decreased cell proliferation index as shown by Ki-67 immunohistochemical staining.
Chemical Information
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CAS No. 428830-84-6
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Masse moléculaire 385.44
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Formule C21H15N5OS
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SMILES
CC1=CC=C(C2=NN(C(/C3=C/C4=CNC5=C4C=CC=C5)=N)C(S2)=NC3=O)C=C1
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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)