GSK2879552 2HCl

製品コードS7796 バッチS779602

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

C23H28N2O2.2HCl
分子量 437.4 CAS No. 1902123-72-1
Solubility (25°C)* 体外 DMSO 87 mg/mL (198.9 mM)
Water 42 mg/mL (96.02 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.35mg/ml Taking the 1 mL working solution as an example, add 50 μL 87 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
in vitro In 165 cell lines, GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines ranged from 40% to 100%. The subset of SCLC lines and primary samples that undergo growth inhibition in response to GSK2879552 exhibit DNA hypomethylation of a signature set of probes. [1]
in vivo In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. [1]

プロトコル(参考用のみ)

キナーゼアッセイ LSD1 enzyme assay
LSD1 activity was measured using a horseradish peroxidase (HRP) coupled assay with amplex red as an electron donor. The formation of product over time is measured using fluorescence intensity, Ex 531 nm and Em 595 nm, in a PerkinElmer EnVision plate reader. Final assay conditions are: 5 nM LSD1, 2.5 μM H3K4me2 peptide, 50 mM HEPES pH 7, 1 U/ml of HRP, 1 mM CHAPS, 0.03% dBSA and 10 μM amplex red.
細胞アッセイ 細胞株 165 human cancer cell lines
濃度 ~10 μM
反応時間 6 d
実験の流れ The optimal cell seeding is determined empirically for all cell lines by examining the growth of a wide range of seeding densities in a 384-well format to identify conditions that permitted proliferation for 6 days. Cells are then plated at the optimal seeding density 24 h before treatment (in duplicate) with a 20-point twofold dilution series of GSK2879552 or 0.15% DMSO. Plates are incubated for 6 days at 37°C in 5% CO2. Cells are then lysed with CellTiter-Glo (CTG) (Promega) and chemiluminescent signal is detected with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells is harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values obtained after the 6 day treatment are expressed as a percent of the T0 value and plotted against compound concentration. Data are fit with a four-parameter equation to generate a concentration response curve and the concentration of GSK126 required to inhibit 50% of growth (growth IC50) is determined.
動物実験 動物モデル SCLC xenograft bearing mice
投薬量 1.5 mg/kg
投与方法 p.o.

カスタマーフィードバック

Data from [Data independently produced by , , Br J Haematol, 2017, doi: 10.1111/bjh.14983]

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：

Pharmacological inhibition of LSD1 suppresses growth of hepatocellular carcinoma by inducing GADD45B [ MedComm (2020), 2023, 4(3):e269] PubMed: 37250145
E3 ligase Trim35 inhibits LSD1 demethylase activity through K63-linked ubiquitination and enhances anti-tumor immunity in NSCLC [ Cell Rep, 2023, 10.1016/j.celrep.2023.113477] PubMed: 37979167
Crucial Role of Lysine-Specific Histone Demethylase 1 in RANKL-Mediated Osteoclast Differentiation [ Int J Mol Sci, 2023, 24(4)3605] PubMed: 36835016
Crucial Role of Lysine-Specific Histone Demethylase 1 in RANKL-Mediated Osteoclast Differentiation [ Int. J. Mol. Sci, 2023, 24(4)] PubMed: None
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] PubMed: 35868306
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] PubMed: 35332332
TRACE generates fluorescent human reporter cell lines to characterize epigenetic pathways [ Mol Cell, 2021, S1097-2765(21)01037-6] PubMed: 34963054
KRT6A Promotes Lung Cancer Cell Growth and Invasion Through MYC-Regulated Pentose Phosphate Pathway [ Front Cell Dev Biol, 2021, 9:694071] PubMed: 34235156
Inhibition of epigenetic modifiers LSD1 and HDAC1 blocks rod photoreceptor death in mouse models of Retinitis Pigmentosa [ J Neurosci, 2021, JN-RM-3102-20] PubMed: 34193554
HeLa TI cell-based assay as a new approach to screen for chemicals able to reactivate the expression of epigenetically silenced genes [ PLoS One, 2021, 16(6):e0252504] PubMed: 34115770

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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。

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