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TAK-243 (Standard)

CAT: 0804-HY-100487RSize: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-100487RSize:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
TAK-243 (Standard) is the analytical standard of TAK-243. This product is intended for research and analytical applications. 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].
CAS Number
1450833-55-2
Target
Apoptosis; E1/E2/E3 Enzyme; NF-κB; Reference Standards
Related Pathways
Apoptosis; Metabolic Enzyme/Protease; NF-κB; Others
Field of Research
Cancer
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 Formula
C19H20F3N5O5S2
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
Scientific Category
Reference Standards

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