化合物GSK2879552 2HCl T4418

Product Introduction
Bioactivity


英文名: GSK2879552 2HCl (1401966-69-5(free base))

描述: GSK2879552 2HCl (1401966-69-5(free base)) 是一种口服的、不可逆的赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂，具有潜在的抗肿瘤活性。

细胞实验: Viable cells are measured in Cell Counting Kit-8 (CCK8) assay. Briefly, cells are cultured in a 96-well plate overnight at a density of 5×103 cells per well and treated with the indicated concentrations of sorafenib (0 μM, 40 μM or 80 μM) for 24 h. Subsequently, the cells are incubated with 10 μL CCK8 for 60 min at 37°C, 5% CO2. The absorbance of optical density at 450 nm (A450) is determined with Varioskan Flash.

体外活性: GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 derepresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1]. GSK2879552 is 280-fold selective over D-amino acid oxidase, allowing for direct comparison of inactivation efficiency (KIapp=520 ± 170 μM, kinact=0.12 ± 0.01 min?1, kinact/KIapp=2.3×10-4 ± 1.31×10-5 min-1 μM-1). GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines, with EC50 of 2-240 nM

体内活性: GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice. There is 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrate partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI is observed for SHP77 bearing mice

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.37 mg/mL (10 mM)


关键字: GSK2879552 2HCl (1401966 69 5(free base)) | GSK2879552 2HCl (1401966695(free base)) | GSK2879552 2HCl (1401966-69-5(free base)) | GSK-2879552 2HCl (1401966-69-5(free base))

相关产品: NCGC00244536 | JIB-04 | PFI-90 | TAK-418 | GSK-LSD1 dihydrochloride | Procaine | DDP-38003 dihydrochloride | LSD1-IN-30 | Tranylcypromine hemisulfate | KDM5A-IN-1

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Hematonosis Compound Library | NO PAINS Compound Library

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