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.
For research use only. We do not sell to patients.
- CAS No.: 428830-84-6
- Formula: C21H15N5OS
- Molecular Weight:385.44
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
More
Biological Activity
Description
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c-nu nude mice with PC3 xenograft (male, 6-7 weeks old)[1]
-
Dosage:15 mg/kg
-
Administration:i.p.; once every other day for 20 days
-
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.
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Protein Extraction
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- MTT Cell Proliferation Assay
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
-
CAS No. 428830-84-6
-
Molecular Weight 385.44
-
Formula C21H15N5OS
-
SMILES
CC1=CC=C(C2=NN(C(/C3=C/C4=CNC5=C4C=CC=C5)=N)C(S2)=NC3=O)C=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)