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Subasumstat (TAK-981), a selective inhibitor of the SUMOylation enzymatic cascade, has potential immune-activating and antineoplastic activities.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $76 | In Stock | In Stock | |
| 2 mg | $108 | In Stock | In Stock | |
| 5 mg | $163 | In Stock | In Stock | |
| 10 mg | $255 | In Stock | In Stock | |
| 25 mg | $478 | In Stock | In Stock | |
| 50 mg | $689 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $198 | In Stock | In Stock |
| 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) |
| Color | Yellow |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (69.19 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
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