TAK-243

• 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].

• 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

• CAS Number :

  [1450833-55-2]