TAK-243
Product Specifications
UNSPSC Description
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[1][2].
Target Antigen
Apoptosis; E1/E2/E3 Enzyme; NF-κB
Type
Reference compound
Related Pathways
Apoptosis;Metabolic Enzyme/Protease;NF-κB
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/TAK-243.html
Purity
98.38
Solubility
DMSO : 50 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic)
Smiles
O=S(OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](NC2=CC=NC3=CC(C4=CC=CC(SC(F)(F)F)=C4)=NN23)C1)(N)=O
Molecular Weight
519.52
References & Citations
[1]Hyer ML, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat Med. 2018 Feb;24(2):186-193.|[2]Best SR, et al. TAK-243, a small molecule inhibitor of ubiquitin-activating enzyme (UAE), induces ER stress and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. Blood 2017 130:1533.|[3]Samir H. Barghout, et al. TAK-243 Is a Selective UBA1 Inhibitor That Displays Preclinical Activity in Acute Myeloid Leukemia (AML). Blood 2017, 130:814.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-100487/TAK-243-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-100487/TAK-243-SDS-MedChemExpress.pdf
Clinical Information
Phase 1
CAS Number
1450833-55-2
Available Sizes
Curated Selection
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