NVS MLLT-1 (compound 3) is a potent and selective MLLT1 inhibitor with Kd values of 0.18 μM, 0.24 μM, and 0.22 μM for wild-type, T1 mutants, and T3 mutants, respectively[1][2].
Biological Activity
NVP-MLLT-1 is a potent and selective inhibitor against YEATS domain (YD) of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3).
References
[1] Ni X, et al. Structure and Inhibitor Binding Characterization of Oncogenic MLLT1 Mutants. ACS Chem Biol. 2021 Apr 16;16(4):571-578. DOI:10.1021/acschembio.0c00960 [2] Lee J, et al. The Promise and Peril of Chemical Probe Negative Controls. ACS Chem Biol. 2021 Apr 16;16(4):579-585. DOI:10.1021/acschembio.1c00036
