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Subasumstat [1858276-04-6]

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Conditionnement : 5mg

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Subasumstat

(Synonyms: TAK-981) Copy Product Info

Synonyms: TAK-981

Catalog No. T8428 Copy Product Info

Purity: 98.22%

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

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

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]
Synonyms	TAK-981

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	1.7298 mL	8.6490 mL	17.2980 mL	86.4902 mL
5 mM	0.3460 mL	1.7298 mL	3.4596 mL	17.2980 mL
10 mM	0.1730 mL	0.8649 mL	1.7298 mL	8.6490 mL
20 mM	0.0865 mL	0.4325 mL	0.8649 mL	4.3245 mL
50 mM	0.0346 mL	0.1730 mL	0.3460 mL	1.7298 mL
100 mM	0.0173 mL	0.0865 mL	0.1730 mL	0.8649 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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

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.

Stock Solution Preparation:

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.

Preparation of the In Vivo Formulation:

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.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

Ubiquitin ligaseUbiquitin conjugating enzymeUbiquitin activating enzymeTAK981TAK 981SUMOylationSubasumstatInhibitorinhibitE3EnzymeE3 ligating enzymeE3 EnzymeE2EnzymeE2 EnzymeE2 conjugating enzymeE1EnzymeE1/E2/E3 EnzymeE1 EnzymeE1 activating enzyme

Related Tags: Subasumstat chemical structure | Subasumstat in vivo | Subasumstat in vitro | Subasumstat formula | Subasumstat molecular weight