A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC₅₀ values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

A 196

white to light brown powder

DMSO : ≥ 31 mg/mL (86.29 mM)

SUV420H1 ,SUV420H2

In cells, A-196 induces a global decrease in H4K20me2 and H4K20me3 and a concomitant increase in H4K20me1, but has no effect on any of the other histone modifications. A-196 inhibits 53BP1 foci formation upon ionizing radiation and reduces NHEJ-mediated DNA-break repair but does not affect homology-directed repair. A-196 potently inhibits SUV420H1 and SUV420H2 at both 1 and 10 μM of A-196, but has no activity at either concentration against any of the other PKMTs in the panel, including the other H4K20-modifying enzyme, PR-SET7, and those that utilize H3K4, H3K9, H3K27, and H3K79 as substrates.