Description
LLY-507 is a potent, selective and cell permeable protein lysine methyltransferase SMYD2 inhibitor with IC50 <15 nM. It binds in the substrate peptide-binding pocket. It has >100-fold selectivity over other methyltransferases and other non-epigenetic targets. LLY-507 has been shown to inhibit p53K370 monomethylation in cells with an IC50 ~600 nM. It inhibited the proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.
Product information
CAS Number: 1793053-37-8
Molecular Weight: 574.76
Formula: C36H42N6O
Chemical Name: 5-cyano-2'-(4-(2-(3-methyl-1H-indol-1-yl)ethyl)piperazin-1-yl)-N-(3-(pyrrolidin-1-yl)propyl)-[1,1'-biphenyl]-3-carboxamide
Smiles: CC1=CN(CCN2CCN(CC2)C2=CC=CC=C2C2C=C(C=C(C=2)C(=O)NCCCN2CCCC2)C#N)C2=CC=CC=C21
InChiKey: PNYRDVBFYVDJJI-UHFFFAOYSA-N
InChi: InChI=1S/C36H42N6O/c1-28-27-42(34-11-4-2-9-32(28)34)22-19-40-17-20-41(21-18-40)35-12-5-3-10-33(35)30-23-29(26-37)24-31(25-30)36(43)38-13-8-16-39-14-6-7-15-39/h2-5,9-12,23-25,27H,6-8,13-22H2,1H3,(H,38,43)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
LLY-507 was used at 10 µM final concentration in various in vitro assays.
References:
- Nguyen H, et al. LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2. (2015) J Biol Chem. 290(22):13641-53.
Products are for research use only. Not for human use.
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