2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. SMYD3 Isoform

SMYD3

SMYD3 is a SET and MYND domain-containing lysine methyltransferase that catalyzes the methylation of histone and non-histone substrates[1][2]. Mechanistically, SMYD3 coordinates transcriptional regulation by forming complexes with proteins such as SMAD3 and RACK1, thereby promoting target gene expression involved in cell proliferation and migration[3][4][5]. In disease models, SMYD3 overexpression is associated with enhanced epithelial-mesenchymal transition (EMT), tumor invasion, and metastasis in breast, colorectal, and liver cancers[3][4][5][6]. Compared with related isoforms, including SMYD2 and SMYD5, SMYD3 demonstrates distinct substrate specificity and structural features, such as a TPR-containing C-terminal domain that forms a narrow substrate-binding pocket critical for enzymatic activity[7][2]. Structural studies also indicate that the DNA-binding MYND domain further modulates its catalytic function, enhancing histone methylation[2]. For experimental applications, pharmacological inhibitors such as BCI121 effectively block SMYD3-mediated chromatin association and reduce malignant phenotypes in cancer cell lines and zebrafish xenograft models[3][5]. Additionally, SMYD3 influences skeletal and cardiac muscle differentiation by targeting myogenic transcription factors, highlighting its utility in developmental and stem cell research[8][9]. These combined functional and structural insights establish SMYD3 as a distinct epigenetic regulator with both oncogenic and developmental relevance[1][2].

References:

SMYD3 Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-19324
    EPZ031686
    		Inhibitor 99.71%
    EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC50 value of 3 nM. EPZ031686 can be used for cancer research.
  • HY-21972
    BCI-121
    		Inhibitor 99.89%
    BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
  • HY-141877
    MS4322
    		Degrader 99.14%
    MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-112080
    BAY-6035
    		Inhibitor 99.51%
    BAY-6035, a chemical probe, is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC50 of 88 nM.
  • HY-151379
    EM127
    		Inhibitor 99.94%
    EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours.
  • HY-104009A
    GSK2807 Trifluoroacetate
    		Inhibitor 99.83%
    GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM.
  • HY-128352
    SMYD3-IN-1
    		Inhibitor 98.03%
    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.
  • HY-141877B
    MS4322 (isomer)
    		99.87%
    MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-152228
    SMYD3-IN-2
    		Inhibitor
    SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer.