Overview

  • Product name

    A-196, SUV420H1 and SUV420H2 inhibitor
  • Description

    Potent and selective inhibitor of SUV420H1 and SUV420H2
  • Biological description

    A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively. It is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. In cells, A-196 induces a global decrease in H4K20me2 and H4K20me3 whilst increasing H4K20me1. It has no effect on other histone modifications. A-196 inhibits H4K20me di- and tri-methylation in cell-based assays. 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, including the other H4K20-modifying enzyme, PR-SET7, and those that utilize H3K4, H3K9, H3K27, and H3K79 as substrates.

  • Purity

    > 99%
  • CAS Number

    1384071-99-1
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-[4-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[2-fluoro-5-(trifluoromethyl)phenyl]urea

  • Molecular weight

    473.43
  • Molecular formula

    C22H19F4N7O
  • PubChem identifier

    117072548
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • Solubility overview

    Soluble in DMSO to 25 mM and in ethanol to 25 mM

  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    C1CCC(C1)NC2=NN=C(C3=CC(=C(C=C32)Cl)Cl)C4=CC=NC=C4
  • Source

    Synthetic

References

ab223600 has not yet been referenced specifically in any publications.

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