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LLY-507

Cat. No. M6288
LLY-507 Structure
Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 700 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 is able to potently inhibit the methylation of H4 peptide by SMYD2 enzyme with an IC50 of 31 nM. It has 100-fold selectivity for SMYD2 over 24 other protein or DNA methyltransferases including related family members SMYD3, SUVH420H1, and SUV420H2. LLY-507 inactives (>20 μM) against 454 kinases, 35 G protein-coupled receptors, 14 nuclear hormone receptors, and three cytochrome P450 enzymes. LLY-507 inhibits the proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner.

Protocol
Cell Experiment
Cell lines HEK293 cells
Preparation method To examine the methylation status of p53 in HEK293 cells treated with LLY-507 by Western blotting, 2 × 105 cells are seeded in 6-well plates in triplicate and co-transfected with FLAG-tagged p53 and FLAG-tagged SMYD2 using Lipofectamine® 2000. The day after transfection, cells are treated with 0-2.5 μM LLY-507 for 28 h, then collected, and lysed in radioimmunoprecipitation assay (RIPA) buffer. Cell lysates are subject to 10% SDS-PAGE and transferred to a PVDF membrane.
Concentrations 0-2.5 μM
Incubation time 28 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 574.76
Formula C36H42N6O
CAS Number 1793053-37-8
Purity >98%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

Quantitative Profiling of the Activity of Protein Lysine Methyltransferase SMYD2 Using SILAC-Based Proteomics.
Olsen JB, et al. Mol Cell Proteomics. 2016 Mar;15(3):892-905. PMID: 26750096.

LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
Nguyen H, et al. J Biol Chem. 2015 May 29;290(22):13641-53. PMID: 25825497.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LLY-507 supplier, Histone Methyltransferase, inhibitors

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