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TAK-243

CAT: 0804-HY-100487-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-100487-01Size:5 mg
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
[1450833-55-2]
Product Name Alternative
MLN7243
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
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
Concentration
10mM
Purity
98.38
Solubility
DMSO : 50 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 Formula
C19H20F3N5O5S2
Molecular Weight
519.52
Precautions
H302, H315, H319, H335
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)
Scientific Category
Reference compound1
Clinical Information
Phase 1

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Alternative Products

CatalogName
MBS3601939-01TAK-243
A20369-25TAK-243 25mg
A20369-2TAK-243 2mg
A20369-50TAK-243 50mg
A20369-100TAK-243 100mg
A20369-1TAK-243 1mg
A20369-5TAK-243 5mg
A20369-10TAK-243 10mg
C13356-01TAK-243 (MLN7243)
A20369-10mM-DTAK-243 10mM * 1mL in DMSO

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