A-196

CAS No.

A-196 ( A196;A 196 )

Catalog No. M17056 CAS No.

A potent, selective and substrate-competitive inhibitor of protein lysine methyltransferases (PKMTs) SUV420H1 and SUV420H2 with IC50 of 25 nM and 144 nM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    A-196
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective and substrate-competitive inhibitor of protein lysine methyltransferases (PKMTs) SUV420H1 and SUV420H2 with IC50 of 25 nM and 144 nM, respectively.
  • Description
    A potent, selective and substrate-competitive inhibitor of protein lysine methyltransferases (PKMTs) SUV420H1 and SUV420H2 with IC50 of 25 nM and 144 nM, respectively; shows no activity for other PKMTs including PR-SET7, and PRMTs, DNMTases; 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.
  • Synonyms
    A196;A 196
  • Pathway
    Chromatin/Epigenetic
  • Target
    HMTase
  • Recptor
    HMTase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    --
  • Formula Weight
    359.25
  • Molecular Formula
    C18H16Cl2N4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 31 mg/mL
  • SMILES
    ClC1=C(Cl)C=C(C(C2=CC=NC=C2)=NN=C3NC4CCCC4)C3=C1
  • Chemical Name
    6,7-dichloro-N-cyclopentyl-4-(pyridin-4-yl)phthalazin-1-amine

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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