LLY 507
Discontinued Product
Chemical Name: 3-Cyano-5-[2-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl]phenyl]-N-[3-(pyrrolidin-1-yl)propyl]benzamide
Purity: ≥98%
Biological Activity
LLY 507 is a potent SMYD2 inhibitor (IC50 = 15 nM). Exhibits >100-fold selectivity for SMYD2 over 25 other methyltransferases including SMYD3, SUV420H1 and SUV420H2. Inhibits SMYD2-mediated p53 methylation in vitro. Also inhibits proliferation of a range of esophageal, liver and breast cancer cell lines.External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of LLY 507 is reviewed on the chemical probes website.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2
NP Coussens, SC Kales, MJ Henderson, OW Lee, KY Horiuchi, Y Wang, Q Chen, E Kuznetsova, J Wu, S Chakka, DM Cheff, K Chih-Chien, P Shinn, KR Brimacombe, M Shen, A Simeonov, M Lal-Nag, H Ma, A Jadhav, MD Hall
J. Biol. Chem., 2018;0(0):. -
LLY-507, a cell-active, potent, and selective inhibitor of protein-lysine methyltransferase SMYD2.
Nguyen et al.
J.Biol.Chem., 2015;290:13641
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