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HomeProduct name listLLY-507

LLY-507

  • CAS NO.:1793053-37-8
  • Empirical Formula: C36H42N6O
  • Molecular Weight: 574.76
  • MDL number: MFCD28902312
  • Update Date: 2024-11-13 18:13:23
LLY-507 Structural

What is LLY-507?

The Uses of LLY-507

LLY-507 is a small molecule inhibitor of SMYD2 (lysine N-methyltransferase), preventing p53 lysine methylation in squamous cell carcinoma cells. Shows a >100-fold selective for SMYD2 over 27 other protein methyltransferases (and non-methyltransferase) targets.

Biological Activity

lly-507 is a potent inhibitor of smyd2.smyd2, a lysine methyltransferase, catalyzes the monomethylation of several protein substrates including p53. smyd2 is reported to be overexpressed in a significant percentage of esophageal squamous primary carcinomas, and such overexpression related with poor patient survival.

in vitro

lly-507 has been identified as a cell-active, potent small molecule inhibitor of smyd2. lly-507 was found to be >100-fold selective for smyd2 over a broad range of methyltransferase and non-methyltransferase targets. the crystal structure of smyd2 in complex with lly-507 showed it bound in the substrate peptide binding pocket. lly-507 was active in cells as demonstrated by the reduction of smyd2-induced monomethylation of p53 lys(370) at submicromolar concentrations. furthermore, ms-based proteomics indicated that cellular histone methylation levels were not affected by smyd2 inhibition with lly-507 significantly, and subcellular fractionation studies showed that smyd2 was primarily cytoplasmic, indicating that smyd2 targeted a small subset of histones. moreover, lly-507 was able to inhibit the proliferation of several liver, esophageal, as well as breast cancer cell lines in a dose-dependent manner [1].

References

[1] nguyen h, et al. lly-507, a cell-active, potent, and selective inhibitor of protein-lysine methyltransferase smyd2. j biol chem. 2015 may 29;290(22):13641-13653.

Properties of LLY-507

storage temp.  Store at -20°C
solubility  ≥57.5 mg/mL in DMSO; insoluble in H2O; ≥54.7 mg/mL in EtOH
form  solid
color  White to off-white

Safety information for LLY-507

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for LLY-507

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