MK204 Chemical Properties

Boiling point:

721.4±60.0 °C(Predicted)

Density 

2.242±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 3mg/mL, clear (warmed)

form 

powder

pka

2.94±0.10(Predicted)

color 

white to beige

MK204 Usage And Synthesis

Uses

MK204 is an aldose reductase (AR) inhibitor that can be used in diabetes research[1].

Biological Activity

MK204 is a potent and selective inhibitor of aldo-keto reductase family member 1B10 (AKR1B10). AKR1B10 is induced in several cancer types, in particular, hepatocellular carcinoma, and may be involved with drug resistance. MK204 appears to target a distinct AKR1B10 inner specificity pocket not present in the closely related aldose reductase. MK204 had an IC50 value of 80 nM compared to an IC50 value of 21.7 μM for aldose reductase.

References

[1] Cousido-Siah A, 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