MLN7243 (TAK-243, AOB 87172)

Background Information:

MLN7243 (TAK-243) is a cell permeable small molecule inhibitor
targeting ubiquitin-activating enzymes (UAE, also known as E1 enzymes).
The enzymes, found more active in cancer cells than in normal, healthy
cells, catalyze the first step in ubiquitination reaction, targeting a
protein for degradation via Proteasome. This covalent attachment of
ubiquitin or ubiquitin-like proteins to targeted proteins is a major
mechanism for regulating protein function in eukaryotic organisms.
Inhibition of the enzyme prevents both protein ubiquitination and
subsequent ubiquitin-mediated proteasomal degradation, resulting in an
excess of proteins in the cells that may lead to endoplasmic reticulum
(ER) stress-mediated apoptosis, thus inhibit tumor (cancer) cell
proliferation and survival. MLN7243 is the first-in-class inhibitor
specifically targeting this class of enzyme to be studied clinically.

APIM050051: MLN7243 (TAK-243, AOB 87172)

CAS No.: 1450833-55-2.
Molecular Formula: C₁₉H₂₀F₃N₅O₅S_2.
Molecular Weight: 519.5.
Purity: 100% Stereomerical Purity (Chiral HPLC), 99% Chemical Purity (HPLC at 220 and 254 nm),.
QC: HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.