2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. Histone Methyltransferase Antagonist

Histone Methyltransferase Antagonist

Histone Methyltransferase Isoform Comparison

Histone Methyltransferase Antagonists (9):

Cat. No. Product Name Effect Purity
  • HY-16993
    OICR-9429
    		Antagonist 99.71%
    OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
  • HY-19347
    WDR5-0103
    		Antagonist 99.93%
    WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
  • HY-114208A
    BI-9321 trihydrochloride
    		Antagonist 98.40%
    BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-15649
    UNC1215
    		Antagonist 98.47%
    UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
  • HY-125292
    NV03
    		Antagonist 98.82%
    NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity.
  • HY-126327A
    UNC4976 TFA
    		Antagonist ≥98.0%
    UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-126327
    UNC4976
    		Antagonist
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-114208
    BI-9321
    		Antagonist
    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-150680
    SARS-CoV-2 nsp14-IN-1
    		Antagonist
    SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases.