LJH685
作者：齊岳
發(fā)布時間：2023-08-30
09:02:45
點擊數(shù)：
產(chǎn)品名稱：LJH685
產(chǎn)品描述：
| 產(chǎn)品描述 | LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM). |
| 靶點活性 | RSK3:4 nM, RSK1:6 nM, RSK2:5 nM |
| 體外活性 | 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] |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 分子量 | 381.42 |
| 分子式 | C22H21F2N3O |
| CAS No. | 1627710-50-2 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
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 )
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