Item no. |
HY-100487-5mg |
Manufacturer |
MedChem Express
|
CASRN |
1450833-55-2 |
Amount |
5 mg |
Quantity options |
100 mg
10mM/1mL
10 mg
50 mg
5 mg
|
Category |
|
Type |
Inhibitors |
Specific against |
other |
Purity |
98.38 |
Formula |
C19H20F3N5O5S2 |
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.<br/>[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.<br/>[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. |
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 |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Alias |
MLN7243 |
Available |
|
Product 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]. |
StorageTemperature |
-20°C, 3 years; 4°C, 2 years (Powder) |
Shipping |
Room Temperature |
Manufacturers Applications |
Cancer-programmed cell death |
MolecularWeight |
519.52 |
Clinical Information |
Phase 1 |
Manufacturers Research Area |
Cancer |
Solubility |
DMSO : 50 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic) |
Target |
Apoptosis; E1/E2/E3 Enzyme; NF-κB |
Manufacturers Target |
Apoptosis; E1/E2/E3 Enzyme; NF-κB |
Manufacturers Pathway |
Apoptosis; Metabolic Enzyme/Protease; NF-κB |
Manufacturers Product type |
Reference compound |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.