LJH685

製品コードS7870 バッチS787001

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H21F2N3O
分子量 381.42 CAS No. 1627710-50-2
Solubility (25°C)* 体外 Ethanol 20 mg/mL (52.43 mM)
DMSO 10 mg/mL (26.21 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Calu6, NCI-H2122, NCI-H358, NCI-H727, NCI-H2087, SW620, SW480, HT29, Capan-2, MiaPaCa2, SW1990, Panc02.03, MDA-MB-231, A375, G361, Colo205, Malme3M, WM1799, WM983B and WM266-4 cells
濃度 ~100 μM
反応時間 72 h
実験の流れ 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.

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2017, 8(22):35761-35775]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A hotspot mutation targeting the R-RAS2 GTPase acts as a potent oncogenic driver in a wide spectrum of tumors [ Cell Rep, 2022, 38(11):110522] PubMed: 35294890
ERK phosphorylation disrupts the intramolecular interaction of capicua to promote cytoplasmic translocation of capicua and tumor growth [ Front Mol Biosci, 2022, 9:1030725] PubMed: 36619173
Oncogene-dependent sloppiness in mRNA translation [ Mol Cell, 2021, S1097-2765(21)00736-X] PubMed: 34562372
Adaptive RSK-EphA2-GPRC5A signaling switch triggers chemotherapy resistance in ovarian cancer. [ EMBO Mol Med, 2020, 12(4):e11177] PubMed: 32115889
Proteomic and transcriptomic profiling identifies mediators of anchorage-independent growth and roles of inhibitor of differentiation proteins in invasive lobular carcinoma [ Sci Rep, 2020, 10(1):11487] PubMed: 32661241
RSK3 mediates necroptosis by regulating phosphorylation of RIP3 in rat retinal ganglion cells. [ J Anat, 2020, 12] PubMed: 32162697
Human melanoma cells resistant to MAPK inhibitors can be effectively targeted by inhibition of the p90 ribosomal S6 kinase. [Kosnopfel C, et al. Oncotarget, 2017, 8(22):35761-35775] PubMed: 28415756

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。