LLY507 |
カタログ番号GC16261
One-Click Copy Product Info
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LLY507 は、タンパク質リジンメチルトランスフェラーゼ SMYD2 の強力かつ選択的な阻害剤です。 LLY507 は、SMYD2 が p53 ペプチドをメチル化する能力を IC50 <15 nM で強力に阻害します。 LLY507 は、癌やその他の生物学的プロセスにおける SMYD2 機能の分析を支援する貴重な化学プローブとして機能します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1793053-37-8
Sample solution is provided at 25 µL, 10mM.
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IC50: < 15 nM
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].
In vivo: So far, there is no animal data reported.
Clinical trial: Up to now, LLY-507 is still in the preclinical development stage.
Reference:
[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.
| Cas No. | 1793053-37-8 | SDF | |
| 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 | ||
| Canonical SMILES | N#CC1=CC(C(NCCCN2CCCC2)=O)=CC(C3=CC=CC=C3N4CCN(CC4)CCN5C=C(C6=C5C=CC=C6)C)=C1 | ||
| Formula | C36H42N6O | M.Wt | 574.76 |
| 溶解度 | ≥ 57.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7399 mL | 8.6993 mL | 17.3986 mL |
| 5 mM | 348 μL | 1.7399 mL | 3.4797 mL |
| 10 mM | 174 μL | 869.9 μL | 1.7399 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)