Powder: -20°C for 3 years | In solvent: -80°C for 2 years
LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 33.00 | |
2 mg | In stock | $ 45.00 | |
5 mg | In stock | $ 81.00 | |
10 mg | In stock | $ 147.00 | |
25 mg | In stock | $ 296.00 | |
50 mg | In stock | $ 471.00 | |
100 mg | In stock | $ 688.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 93.00 |
Description | LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM). |
Targets&IC50 | RSK3:4 nM, RSK2:5 nM, RSK1:6 nM |
In vitro | LJH685 modulates YB1 phosphorylation by potently and selectively inhibiting RSK in cells. In MAPK pathway–dependent cancer cell lines, LJH685 shows antiproliferative effects, and causes cell-cycle regulation and apoptosis induction. [1] |
Kinase Assay | Inhibition of RSK1, RSK2, and RSK3 activity: Enzymatic activity of RSK isoforms 1, 2, and 3 (PV4049, PV4051, and PV3846) is assessed using recombinant full-length RSK protein. RSK1 (1 nmol/L), RSK2 (0.1 nmol/L), or RSK3 (1 nmol/L) is allowed to phosphorylate 200 nmol/L peptide substrate (biotin-AGAGRSRHSSYPAGT-OH) in the presence of ATP at concentration equal to the Km for ATP for each enzyme (RSK1, 5 μmol/L; RSK2, 20 μmol/L; and RSK3, 10 μmol/L) and appropriate dilutions of RSK inhibitors. |
Cell Research | Cell growth under attached conditions is assessed by plating 1000 cells per well on 96-well tissue culture-treated plates in cell growth medium. Appropriate dilutions of compound are added medium above cells and cell growth is assessed after 72 hrs by addition of CellTiter Glo reagent according to manufacturer's directions.(Only for Reference) |
Molecular Weight | 381.42 |
Formula | C22H21F2N3O |
CAS No. | 1627710-50-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 71 mg/mL (186.1 mM)
Ethanol: 16 mg/mL (41.9 mM)
H2O: <1 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
LJH685 1627710-50-2 Apoptosis MAPK PI3K/Akt/mTOR signaling S6 Kinase S6K LJH-685 inhibit Ribosomal S6 Kinase (RSK) LJH 685 Inhibitor inhibitor