Catalog No.: PC-42081Not For Human Use, Lab Use Only.
A-196 is a potent, selective and substrate-competitive inhibitor of protein lysine methyltransferases (PKMTs) SUV420H1 and SUV420H2 with IC50 of 25 nM and 144 nM, respectively.
A-196 is a potent, selective and substrate-competitive inhibitor of protein lysine methyltransferases (PKMTs) SUV420H1 and SUV420H2 with IC50 of 25 nM and 144 nM, respectively.
A-196 shows no activity for other PKMTs including PR-SET7, and PRMTs, DNMTases.
A-196 induces a global decrease in H4K20me2 and H4K20me3 (EC50= 262 and 370 nM, respectively) and a concomitant increase in H4K20me1 (EC50=735 nM) in U2OS cells, inhibits 53BP1 foci formation upon ionizing radiation and reduces NHEJ-mediated DNA-break repair but does not affect homology-directed repair.
