Histone Methyltransferase

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  1. CBX4 /CBX7 chromodomains antagonist

    UNC3866 is a potent antagonist of CBX4 and CBX7 chromodomains with a Kd of ~100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.
  2. G9a inhibitor

    CPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity .
  3. Dot1L inhibitor

    Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.
  4. SMYD3 inhibitor

    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
  5. SUV39H2 inhibitor

    OTS186935 is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM.
  6. SMYD2 inhibitor

    SMYD2-IN-1 is a SMYD2 inhibitor extracted from patent WO2016166186A1, compound example 1.1, has an IC50 of 4.45 nM.
  7. Dot1L inhibitor

    Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
  8. EZH1/2 dual inhibitor

    Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor, used in the research of relapsed/refractory peripheral T-cell lymphoma.
  9. WDR5/MLL inhibitor

    MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction.
  10. CARM1 inhibitor

    DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM.
  11. SMYD2 inhibitor

    A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
  12. EZH2 inhibitor

    PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition.
  13. DOT1L inhibitor

    EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
  14. CARM1 inhibitor

    SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with IC50 of 50 nM.

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