TAK-243

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].

Product Specifications

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.