LLY-507
- Product Name
- LLY-507
- CAS No.
- 1793053-37-8
- Chemical Name
- LLY-507
- Synonyms
- LLY-507;CS-2196;LLY-507(CHEMBL3414623);LLY-507, 10 mM in DMSO;LLY-507; LLY507;LLY 507;5-cyano-2'-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl]-N-[3-(1-pyrrol;3-Cyano-5-[2-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]piperazin-1-yl]phenyl]-N-[3-(pyrrolidin-1-yl)propyl]benzamide;5-Cyano-2'-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl}-N-[3-(1-pyrrolidinyl)propyl]-3-biphenylcarboximidic acid;5-Cyano-2'-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)propyl]-[1,1'-biphenyl]-3-carboxamide;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
- CBNumber
- CB03051582
- Molecular Formula
- C36H42N6O
- Formula Weight
- 574.76
- MOL File
- 1793053-37-8.mol
LLY-507 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 16441
- Product name
- LLY-507
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 16441
- Product name
- LLY-507
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- 16441
- Product name
- LLY-507
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $302
- Updated
- 2024/03/01
- Product number
- 16441
- Product name
- LLY-507
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $670
- Updated
- 2024/03/01
- Product number
- L468905
- Product name
- LLY-507
- Packaging
- 1mg
- Price
- $55
- Updated
- 2021/12/16
LLY-507 Chemical Properties,Usage,Production
Uses
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].
IC 50
< 15 nm
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.
LLY-507 Preparation Products And Raw materials
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View Lastest Price from LLY-507 manufacturers
- Product
- LLY-507 1793053-37-8
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2019-12-23
- Product
- 5-Cyano-2'-{4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl}-N-[3-(1-pyrrolidinyl)propyl]-3-biphenylcarboximidic acid 1793053-37-8
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2019-12-20