WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407272
Description: A-196 is the first potent and selective chemical probe for SUV420H1 and SUV420H2. The in vitro activity of A-196 includes inhibition of SUV420H1 with IC50 = 25 nM and SUV420H2 with IC50 = 144 nM for methylation of H4K20me and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cell assays, A-196 inhibits the di- and tri-methylation of H4K20me in multiple cell lines with IC50 < 1 µM.
MedKoo Cat#: 407272
Chemical Formula: C18H16Cl2N4
Exact Mass: 358.0752
Molecular Weight: 359.254
Elemental Analysis: C, 60.18; H, 4.49; Cl, 19.74; N, 15.60
Synonym: A-196; A 196; A196.
IUPAC/Chemical Name: 6,7-dichloro-N-cyclopentyl-4-(pyridin-4-yl)phthalazin-1-amine
InChi Key: ABGOSOMRWSYAOB-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H16Cl2N4/c19-15-9-13-14(10-16(15)20)18(22-12-3-1-2-4-12)24-23-17(13)11-5-7-21-8-6-11/h5-10,12H,1-4H2,(H,22,24)
SMILES Code: ClC1=C(Cl)C=C(C(C2=CC=NC=C2)=NN=C3NC4CCCC4)C3=C1
Histone H4 lysine 20 methylation is emerging as a crucial modification to ensure genomic integrity both in the absence and presence of genotoxic stress. The majority of histone H4 methylation is detected in the lysine 20 (H4K20) and is evolutionarily conserved from yeast to human. Each methylation state results in distinct biology: dimethylated H4K20 (H4K20me2) is involved in DNA replication and DNA damage repair, and trimethylated H4K20 (H4K20me3) results in silenced heterochromatic regions . Loss of histone H4 lysine 20 trimethylation (H4K20me3) is characteristic of human cancer and a potential prognostic marker in many types of cancers.