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TAK-243

Cat. No. M14330

All AbMole products are for research use only, cannot be used for human consumption.

TAK-243 Structure
Synonym:

MLN7243

Size Price Availability Quantity
2mg USD 63  USD63 In stock
5mg USD 107  USD107 In stock
10mg USD 167  USD167 In stock
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Quality Control & Documentation
Biological Activity

TAK-243 (MLN7243) 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 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.

Chemical Information
Molecular Weight 519.52
CAS Number 1450833-55-2
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Zhuoxun Wu, et al. ABCB1 limits the cytotoxic activity of TAK-243, an inhibitor of the ubiquitin-activating enzyme UBA1

[2] Yasuhisa Murai, et al. SLFN11 Inactivation Induces Proteotoxic Stress and Sensitizes Cancer Cells to Ubiquitin Activating Enzyme Inhibitor TAK-243

[3] Samir H Barghout, et al. A genome-wide CRISPR/Cas9 screen in acute myeloid leukemia cells identifies regulators of TAK-243 sensitivity

[4] Samir H Barghout, et al. Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia

[5] Marc L Hyer, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment

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Keywords: TAK-243, MLN7243 supplier, E1/E2/E3 Enzyme, inhibitors, activators

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