MK181 is an AKR1B10 inhibitor. MK181 can bind into the external loop A subpocket. AKR1B10 has evolved as a tumor marker and promising antineoplastic target. It shares high structural similarity with the diabetes target enzyme aldose reductase (AR).
Uses
MK181 is an aldose reductase (AR) inhibitor with IC50s of 0.71 μM and 4.5 μM for aldose reductase and AKR1B10, respectively. MK181 can bind into the external loop A subpocket of AKR1B10[1].
References
[1] Alexandra Cousido-Siah, et al. IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors. ACS Chem Biol. 2016 Oct 21;11(10):2693-2705. DOI:10.1021/acschembio.6b00382
