GSK2879552 dihydrochloride是一种可口服的，不可逆的 LSD1/ KDM1A 抑制剂，具有抗肿瘤活性。
货号:ajcx34280
CAS:1902123-72-1
分子式:C23H30Cl2N2O2
分子量：437.4
溶解度:DMSO : 50 mg/mL (114.31 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity[1][2].

GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1].

GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice[2].

[1]. Huang M, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Apr 2;398:12-21.
[2]. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell. 2015 Jul 13;28(1):57-69.