SETDB1 (human, recombinant)

Histone-lysine N-methyltransferase SETDB1 is a member of the SUV39-related protein lysine methyltransferase (PKMT) family and is involved in epigenetic regulation.¹ It is composed of an N-terminal domain that contains two nuclear export signals, two nuclear localization signals, three tudor domains that facilitate complexation with transcriptional regulators, and a methyl-CpG-binding domain (MBD), which binds to DNA, and a C-terminal domain that contains pre-SET, SET, and post-SET domains, which are responsible for the methyltransferase activity. Alternative splicing of SETDB1 produces two shorter isoforms with either a truncated post-SET domain, which retains enzymatic activity, or a full C-terminal truncation, which lacks enzymatic activity. SETDB1 is ubiquitously expressed and localizes to the nucleus and cytoplasm.^2,3 It induces gene silencing by di- and trimethylation of histone H3 at lysine 9 (H3K9) using S-adenosylmethionine as the methyl donor and regulates various cellular processes, including cell division and proliferation, retroelement suppression, immune cell function, X chromosome inactivation, nervous system development, and the formation of promyelocytic leukemia nuclear bodies (PML-NBs).¹ Overexpression of SETDB1 increases the number of colon cancer cells in the S and G₂/M phases in vitro and promotes tumor growth in vivo.⁴ Increased SETDB1 protein levels are associated with schizophrenia, and mutations in SETDB1 have been found in patients with inflammatory bowel disease (IBD).¹ Cayman’s SETDB1 (human, recombinant) protein can be used for enzyme activity assays.

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1. Markouli, M., Strepkos, D., and Piperi, C. Structure, activity and function of the SETDB1 protein methyltransferase. Life (Basel) 11(8), 817 (2021).

2. Blackburn, M.L., Chansky, H.A., Zielinska-Kwiatkowska, A., et al. Genomic structure and expression of the mouse ESET gene encoding an ERG-associated histone methyltransferase with a SET domain. Biochim. Biophys. Acta 629(1-3), 8-14 (2003).

3. Cho, S., Park, J.S., and Kang, Y.-K. Regulated nuclear entry of over-expressed Setdb1. Genes Cells 18(8), 694-703 (2013).

4. Yu, L., Ye, F., Li, Y.-Y., et al. Histone methyltransferase SETDB1 promotes colorectal cancer proliferation through the STAT1-CCND1/CDK6 axis. Carcinogenesis 41(5), 678-688 (2020).