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VARS1-IN-1 is a valyl-tRNA synthetase (VARS1) inhibitor with a Kd value of 0.213 μM. It suppresses the aminoacylation activity of VARS1, decreases the charging level of valine tRNA, and reduces the overall protein synthesis rate. Additionally, VARS1-IN-1 inhibits the growth and cell proliferation of aggressive tumors in PC3 prostate cancer xenograft models, making it a valuable tool in prostate cancer research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | VARS1-IN-1 is a valyl-tRNA synthetase (VARS1) inhibitor with a Kd value of 0.213 μM. It suppresses the aminoacylation activity of VARS1, decreases the charging level of valine tRNA, and reduces the overall protein synthesis rate. Additionally, VARS1-IN-1 inhibits the growth and cell proliferation of aggressive tumors in PC3 prostate cancer xenograft models, making it a valuable tool in prostate cancer research. |
| In vitro | VARS1-IN-1 (Compound 2701) at 10 µM for 2 days disrupts the tRNA aminoacylation activity of VARS1 without affecting its expression, resulting in a decreased ratio of charged tRNA-Val to total tRNA-Val in prostate cancer cells. Additionally, VARS1-IN-1 (10 µM for 2 days) reduces the overall protein synthesis rate in PC3 cells. |
| In vivo | VARS1-IN-1 (Compound 2701), administered at 15 mg/kg via intraperitoneal injection every other day for 20 days, effectively inhibits tumor growth and cell proliferation in the PC3 prostate cancer xenograft model using male BALB/c-nu nude mice. |
| Molecular Weight | 385.45 |
| Formula | C21H15N5OS |
| Cas No. | 428830-84-6 |
| Smiles | O=C1N=C2SC(=NN2C(=N)C1=CC3=CNC=4C=CC=CC34)C=5C=CC(=CC5)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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