Subasumstat [1858276-04-6]

Cat# T8428-5mg

Size : 5mg

Marca : TargetMol


Subasumstat

(Synonyms: TAK-981) Copy Product Info
Subasumstat (TAK-981), a selective inhibitor of the SUMOylation enzymatic cascade, has potential immune-activating and antineoplastic activities.
Subasumstat
Cas No. 1858276-04-6
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:98.22%
Appearance:Solid
Color:White to Yellow
COA LCMS HNMR

Product Introduction

Bioactivity
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]
SynonymsTAK-981
Chemical Properties
Molecular Weight578.1
FormulaC25H28ClN5O5S2
Cas No.1858276-04-6
SmilesCc1sc(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 & Solubility Information
StorageThe 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
1mg5mg10mg50mg
1 mM1.7298 mL8.6490 mL17.2980 mL86.4902 mL
5 mM0.3460 mL1.7298 mL3.4596 mL17.2980 mL
10 mM0.1730 mL0.8649 mL1.7298 mL8.6490 mL
20 mM0.0865 mL0.4325 mL0.8649 mL4.3245 mL
50 mM0.0346 mL0.1730 mL0.3460 mL1.7298 mL
100 mM0.0173 mL0.0865 mL0.1730 mL0.8649 mL
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.

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