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].
Applications: Cancer-programmed cell death
Formula: C19H20F3N5O5S2
References: [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.
CAS Number: 1450833-55-2
Molecular Weight: 519.52
Compound Purity: 98.38
Research Area: Cancer
Solubility: DMSO : 50 mg/mL (ultrasonic)/H2O : < 0.1 mg/mL (ultrasonic)
Target: Apoptosis;E1/E2/E3 Enzyme;NF-κB
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