TAK-243 是一种选择性的泛素激活酶，UAE 抑制剂，IC50值为 1 nM，可阻断泛素结合，破坏单泛素信号传导以及整体蛋白质泛素化。它诱导内质网应激反应，消除 NF-Κb 通路激活并促进细胞凋亡，具有潜在的抗肿瘤活性。

TAK-243 is a small molecule inhibitor of ubiquitin-activating enzyme (UAE ,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,with potential antineoplastic activity.

TAK-243 (formerly known as MLN7243) as a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade.?TAK-243 treatment caused depletion of cellular ubiquitin conjugates, resulting in disruption of signaling events, induction of proteotoxic stress, and impairment of cell cycle progression and DNA damage repair pathways[1].

TAK-243 treatment caused death of cancer cells and, in primary human xenograft studies, demonstrated antitumor activity at tolerated doses.?Due to its specificity and potency, TAK-243 allows for interrogation of ubiquitin biology and for assessment of UAE inhibition as a new approach for cancer treatment[1].

1450833-55-2

C19H20F3N5O5S2

519.52

MLN7243

H2O:1 mg/mL (1.92 mM),Need ultrasonic
DMSO:50 mg/mL (96.24 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years