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TAK-243 (MLN7243) UAE inhibitor

Name: TAK-243 (MLN7243)
Brand: Selleck Chemicals
SKU: S8341
Availability: InStock
Rating: 5 (78 reviews)

Cat.No.S8341

TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress, abrogates NFκB pathway activation and promotes apoptosis.

Chemical Structure

Molecular Weight: 519.52

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Quality Control

Batch: Purity: 99.61%

99.61

Related Targets	Proteasome E3 Ligase DUB SUMO p97 E2 conjugating
Other E1 Activating Inhibitors	MLN4924 (Pevonedistat) PYR-41 ML792 Pevonedistat hydrochloride TAS4464 COH000 DKM 2-93 PYZD-4409 NEDD8 inhibitor M22

Q&A of TAK-243 (MLN7243): Insights Rooted in Extensive Publications, Every Answer Cited

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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 100 mg/mL (192.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (192.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (192.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (192.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Search directly for a cell line, or select a cell line to find matched working concentrations

Mechanism of Action

Information	TAK-243 (MLN7243) is a potent E1 ubiquitin-activating enzyme (UBA1/UBA6) inhibitor. It affects ubiquitin-proteasome and ER stress signaling by blocking ubiquitin conjugation, effectively inhibiting tumor cell proliferation and viral infection.
Read more about TAK-243 (MLN7243) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	519.52	Formula	C₁₉H₂₀F₃N₅O₅S₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1450833-55-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	N[S;v6](=O)(=O)OCC1CC(NC2=CC=NC3=CC(=N[N]23)C4=CC(=CC=C4)SC(F)(F)F)C(O)C1O

TAK-243 (MLN7243) Combination Database

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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TAK-243 (MLN7243) UAE inhibitor

Molecular Weight: 519.52

Quality Control

Solubility in DMSO or Water

Molarity Calculator

In vivo Formulation Calculator (Clear solution)

Working Concentrations for Cell Culture Treatment

Search directly for a cell line, or select a cell line to find matched working concentrations

Mechanism of Action

Chemical Information, Storage & Stability

TAK-243 (MLN7243) Combination Database

Tech Support