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A-196

Chemical Structure : A-196

CAS No.: 1982372-88-2

A-196 (A196;A 196)

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.

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Biological Activity

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.

Physicochemical Properties

M.Wt 359.2524
Formula C18H16Cl2N4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 31 mg/mL

Chemical Name/SMILES

6,7-dichloro-N-cyclopentyl-4-(pyridin-4-yl)phthalazin-1-amine

References

1. Bromberg KD, et al. Nat Chem Biol. 2017 Mar;13(3):317-324.

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