ArtNr |
HY-100487-10mM |
Hersteller |
MedChem Express
|
CAS-Nr. |
1450833-55-2 |
Menge |
10mM/1mL |
Quantity options |
100 mg
10mM/1mL
10 mg
50 mg
5 mg
|
Kategorie |
|
Typ |
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 |
Lieferbar |
|
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 |
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