VRK-IN-1，10MG，SML4138-10MG，Sigma

Biochem/physiol Actions

Potent and selective vaccinia-related kinases 1 (VRK1) inhibitor that blocks VRK1-mediated histone H3 & H4 posttranslational epigenetic modifications.

VRK-IN-1 is a potent and selective vaccinia-related kinases 1 (VRK1) inhibitor (VRK1 IC50 = 150 nM; % inhibition at 1 µM = 78/MAP4K4, 53/CAMKK2, and <25 against 46 other kinases). VRK1 is reported to modulate histone H3 & H4 posttranslational epigenetic modifications, VRK-IN-1 treatment downregulates H4K16ac (by 36%, 45%, 73%, respectively, post 24h incubation with 200, 400, 600 nM VRK-IN-1 in serum-deprived A549 cultures) and H3K4me3 (by 70% post 24h 600 nM treatment; A549 cells), while upregulates H3K9me3 (by 200% post 24h 600 nM treatment; A549 cells).