SMILES string
FC1=CC(C2=CN=C(C)C(C3=CC(F)=C(O)C(F)=C3)=C2)=CC(F)=C1O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
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).
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).
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