Name:TAK-243 (MLN7243)
Synonyms:N/A
CAS Number:1450833-55-2
Formula:C19H20F3N5O5S2
M.w.:519.52
DMSO (mg/mL)Max Solubility:100
DMSO (mM)Max Solubility:192.49
Form:Free base
SMILES:N[S;v6](=O)(=O)OCC1CC(NC2=CC=NC3=CC(=N[N]23)C4=CC(=CC=C4)SC(F)(F)F)C(O)C1O
ALogP:2.805
Target:Apoptosis related,E1 Activating,NF-κB
Pathway:Ubiquitin
Information:TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress, abrogates NFκB pathway activation and promotes apoptosis.
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