2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. SETD7/KMT7 Isoform

SETD7/KMT7

SETD7 (KMT7) is a SET domain-containing lysine methyltransferase that primarily catalyzes histone H3 lysine 4 monomethylation (H3K4me1), an epigenetic mark associated with transcriptional activation and enhancer function[1][2]. Mechanistically, SETD7 regulates gene expression through both histone and non-histone substrate methylation, extending its influence beyond chromatin remodeling to the control of protein stability, subcellular localization, and protein-protein interactions[3][4]. In addition to histone H3, SETD7 methylates multiple regulatory proteins, including p53, TAF10, and cGAS, thereby linking lysine methylation to transcriptional regulation, stress responses, and innate immune signaling[2][3]. Consequently, SETD7 participates in diverse biological processes, including cell differentiation, cell-cycle control, apoptosis, epithelial-mesenchymal transition, and DNA damage responses[4]. In disease settings, extensive evidence implicates SETD7 in cancer-associated pathways, although its biological effects are highly dependent on cellular context and substrate availability[4][5]. For example, SETD7-mediated methylation can stabilize tumor-suppressive proteins such as p53 or promote degradation of oncogenic KRAS, thereby attenuating RAS/MEK/ERK signaling in non-small cell lung cancer models[3][5]. Compared with other lysine methyltransferases that predominantly target histones, SETD7 is distinguished by its broad repertoire of non-histone substrates and its ability to directly modulate signaling networks through substrate-specific methylation events[2][3]. For experimental applications, SETD7 is frequently investigated as a regulator of epigenetic signaling and protein methylation, making it a useful target for mechanistic studies of transcriptional control, cancer biology, and cellular stress responses[4].

SETD7/KMT7 Related Products (5):

Cat. No. Product Name Effect Purity
  • HY-18627A
    PFI-2 hydrochloride
    		Inhibitor 99.48%
    PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.
  • 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-18627
    PFI-2
    		Inhibitor 99.68%
    PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride, a chemical probe, is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.
  • 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-119164
    DC-S238
    		Inhibitor
    DC-S238 is an orally active and highly selective histone methyltransferase SET7 (SETD7) inhibitor (IC50=4.88 μM). DC-S238 is promising for research of cancer, diabetes and inflammatory diseases.