1. Metabolic Enzyme/Protease
    NF-κB
    Apoptosis
  2. E1/E2/E3 Enzyme
    NF-κB
    Apoptosis
  3. TAK-243

TAK-243 (Synonyms: MLN7243; AOB87172)

Cat. No.: HY-100487 Purity: 99.43%
Handling Instructions

TAK-243 is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.

For research use only. We do not sell to patients.

TAK-243 Chemical Structure

TAK-243 Chemical Structure

CAS No. : 1450833-55-2

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10 mM * 1 mL in DMSO USD 274 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

TAK-243 is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis[1][2].

IC50 & Target

IC50: 1 nM (UBA1)[1]

In Vitro

TAK-243 shows anti-proliferative effect on a panel of cell lines derived from hematologic and solid tumors with variable EC50 values that ranged from 0.006 µM to 1.31 µM[1].
TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50s ranging from 15-40 nM after treatment for 48 hours[3].

In Vivo

TAK-243 significantly delays tumor growth in mice (T/C=0.02) with no toxicity as evidenced by no changes in mouse body weight, serum chemistry, or organ histology. TAK-243 reduces primary AML tumor burden in both tested samples without toxicity[3].

Clinical Trial
Molecular Weight

519.52

Formula

C₁₉H₂₀F₃N₅O₅S₂

CAS No.

1450833-55-2

SMILES

O=S(OC[[email protected]@H]1[[email protected]@H](O)[[email protected]@H](O)[[email protected]](NC2=CC=NC3=CC(C4=CC=CC(SC(F)(F)F)=C4)=NN23)C1)(N)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (96.24 mM; Need ultrasonic)

H2O : 1 mg/mL (1.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9249 mL 9.6243 mL 19.2485 mL
5 mM 0.3850 mL 1.9249 mL 3.8497 mL
10 mM 0.1925 mL 0.9624 mL 1.9249 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Normal keratinocytes (normal human keratinocytes (NHK) and recessive dystrophic epidermolysis bullosa keratinocytes (RDEBK)) and cSCC cell lines are seeded into 96 well plates and live cell number and cell death are analysed with an IncuCyte ZOOM real-time imager using the CellTox Green Cytotoxicity Assay. Relative EC50 values are determined using GraphPad Prism. For clonogenic assays cells are seeded into six well plates. Inhibitors (e.g., TAK-243; 0.01, 0.1, 1, and 10 μM) are added for the indicated times and then cells are maintained in drug-free medium for up to 2 weeks to allow colony formation. Colonies are fixed in 10% methanol, 10% acetic acid and stained with crystal violet[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
The preclinical efficacy and toxicity of TAK-243 are assessed in mouse models of AML. OCI-AML2 cells are injected subcutaneously (sc) into SCID mice, and when tumors are palpable, mice are treated with TAK-243 (20 mg/kg sc twice weekly). As an additional model, primary AML cells from 2 patients are injected into the femurs of NOD-SCID mice. Two weeks after injection, mice are treated with TAK-243 (20 mg/kg sc twice weekly). After 3 weeks of treatment, mice ae sacrificed, and AML engraftment in the non-injected femur is measured by flow cytometry[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.43%

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TAK-243
Cat. No.:
HY-100487
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