LJH685 |
| Catalog No.GC16039 |
LJH685 est un puissant inhibiteur RSK compétitif et sélectif pour l'ATP, inhibe les activités biochimiques RSK1, 2 et 3 avec des IC50 de 6, 5, 4 nM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1627710-50-2
Sample solution is provided at 25 µL, 10mM.
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IC50: 6 nM, 5 nM and 4 nM for the biochemical activities of RSK1, RSK2, and RSK3, respectively
LJH685 is a RSK (p90 ribosomal S6 kinase) inhibitor.
The p90 ribosomal S6 kinase (RSK) family of serine/threonine kinases is found to be expressed in a variety of cancers and its substrate phosphorylation has been implicated in direct regulation of cell proliferation, cell survival, as well as cell polarity.
In vitro: In a previous study, the structural analysis results confirmed the binding of LJH685 to the RSK2 N-terminal kinase ATP-binding site, which suggested that the inhibitor LJH685 adopted an unusual nonplanar conformation that explained its excellent selectivity for RSK family kinases. In addition, LJH685 and it analog LJI308 could efficiently inhibit RSK activity in vitro and in cells. Moreover, in a subset of examined cell lines, the cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 were found to be closely associate with the inhibition of cell growth in an anchorage-independent growth setting [1].
In vivo: So far, there is no animal in vivo data reported for LJH685.
Clinical trial: Up to now, LJH685 is still in the preclinical development stage.
Reference:
[1] Aronchik I, Appleton BA,Basham SE,Crawford K,Del Rosario M,Doyle LV,Estacio WF,Lan J,Lindvall MK,Luu CA,Ornelas E,Venetsanakos E,Shafer CM,Jefferson AB. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res.2014 May;12(5):803-12.
| Cas No. | 1627710-50-2 | SDF | |
| Chemical Name | 2,6-difluoro-4-(4-(4-(4-methylpiperazin-1-yl)phenyl)pyridin-3-yl)phenol | ||
| Canonical SMILES | OC1=C(F)C=C(C2=C(C3=CC=C(N4CCN(C)CC4)C=C3)C=CN=C2)C=C1F | ||
| Formula | C22H21F2N3O | M.Wt | 381.42 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:7): 0.125 mg/ml,Ethanol: 2.5 mg/ml | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6218 mL | 13.1089 mL | 26.2178 mL |
| 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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