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Synonyms: TAK-981
| Description | Subasumstat (TAK-981), a selective inhibitor of the SUMOylation enzymatic cascade, has potential immune-activating and antineoplastic activities. |
| In vitro | Methods: HL-60 cells were treated with TAK-981 (10nM; 100nM) for 24 h, and the levels of SUMO-1 and SUMO-2/3 were detected by Western blot. To characterize the effect of the SUMOylation inhibitor TAK-981 on AML cells, we first monitored its effect on SUMOylation in three AML model cell lines HL-60, U937, and THP-1. Results: TAK-981 significantly reduced the global SUMOylation level mediated by SUMO-1 and SUMO-2/3 at 10 nM concentration and almost completely abolished it at 100 nM concentration. [1] |
| In vivo | Methods: TAK-981 (15 mg/kg) was injected intravenously into the tumor model mice to detect the anti-tumor activity in vivo. Results: TAK981 significantly inhibited tumor growth. [2] |
| Synonyms | TAK-981 |
| Molecular Weight | 578.1 |
| Formula | C25H28ClN5O5S2 |
| Cas No. | 1858276-04-6 |
| Smiles | Cc1sc(cc1[C@@H]1NCCc2ccc(Cl)cc12)C(=O)c1cncnc1N[C@H]1C[C@H](O)[C@@H](COS(N)(=O)=O)C1 |
| Relative Density. | 1.474 g/cm3 (Predicted) |
| Storage | The compound is unstable in solution. Please use soon Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 122.5 mg/mL (211.9 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.46 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.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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