2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. SMYD2 Isoform

SMYD2

SMYD2 (SET and MYND domain-containing protein 2) is a lysine methyltransferase that catalyzes the methylation of both histone and non-histone proteins, regulating chromatin accessibility and transcriptional activity[1][2]. Mechanistically, SMYD2 facilitates signal transduction in key pathways, including BMP/SMAD, STAT3, and NF-κB, by methylating substrates such as BMPR2, STAT3, p65, and TRAF2[3][4][5][6]. In disease models, aberrant SMYD2 expression drives tumor progression in triple-negative breast cancer, gastrointestinal cancers, and non-small-cell lung cancer, and contributes to vascular and renal pathologies, including neointimal hyperplasia and polycystic kidney disease[7][8][9][10]. Compared with related isoforms such as SMYD1 and SMYD3, SMYD2 exhibits distinct substrate specificity and tissue distribution, showing cytoplasmic localization and preference for non-histone targets, which differentiates its regulatory roles[1][2][11]. For experimental applications, selective chemical probes and inhibitors such as LLY-507, AZ505, A-893, and BAY-598 have enabled precise interrogation of SMYD2 functions in vitro and in vivo, suppressing methylation-dependent activation of oncogenic and inflammatory pathways[6][12][13]. These inhibitors provide valuable tools for dissecting SMYD2-mediated epigenetic regulation and validating its therapeutic potential across multiple disease contexts[12][13].

References:

SMYD2 Related Products (8):

Cat. No. Product Name Effect Purity
  • HY-19313
    LLY-507
    		Inhibitor 99.09%
    LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.
  • HY-15226
    AZ505
    		Inhibitor 99.99%
    AZ505 is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM.
  • HY-19546
    BAY-598
    		Inhibitor 99.33%
    BAY-598, a chemical probe, is selective small molecule inhibitor of SMYD2 with an IC50 of 27 nM.
  • 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-15226A
    AZ505 ditrifluoroacetate
    		Inhibitor 99.89%
    AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
  • HY-134828
    AZ506
    		Inhibitor 99.74%
    AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal.
  • 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-19563
    A-893
    		Inhibitor
    A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.