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Results for "

SETD8

" in MedChemExpress (MCE) Product Catalog:

10

Inhibitors & Agonists

1

Peptides

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100625
    BVT948
    2 Publications Verification

    		 Phosphatase Cytochrome P450 Histone Methyltransferase Cancer
    BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
    BVT948
  • HY-100624
    Ryuvidine

    		CDK Cancer
    Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20 in vitro . Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM and is cytotoxic against a range of human cancer cells .
    Ryuvidine
  • HY-12335
    UNC0379
    Maximum Cited Publications
    7 Publications Verification

    		 Histone Methyltransferase Inflammation/Immunology Cancer
    UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .
    UNC0379
  • HY-121093
    DC-S239

    		Histone Methyltransferase Cancer
    DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .
    DC-S239
  • HY-13807
    UNC0646
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM .
    UNC0646
  • HY-148817
    WDR5-0102

    		WDR5 Cancer
    WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5 .
    WDR5-0102
  • HY-P10570
    [Nle20] H4 peptide (16−23)

    		Histone Methyltransferase Cancer
    [Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase SETD8 (Kd=0.14 μM), which inhibits SETD8's methylation of histone H4 by competing with SETD8's substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy .
    [Nle20] H4 peptide (16−23)
  • HY-116255
    MS453

    		Histone Methyltransferase Others
    MS453 is a potent and highly selective SETD8 inhibitor with an IC50 value of 804 nM. MS453 specifically modifies a cysteine residue close to the inhibitor binding site. MS453 is selective for 28 other methyltransferases. The crystal structure of MS453 reveals its binding mode to SETD8, providing an atomic-level view for the development of high-quality chemical probes for SETD8 .
    MS453
  • HY-138886
    RL5a

    		Histone Methyltransferase Cancer
    RL5a (compund C23) is a SETD8 inhibitor .
    RL5a
  • HY-12335A
    UNC0379 TFA

    		Histone Methyltransferase Inflammation/Immunology Cancer
    UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .
    UNC0379 TFA

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