GSK2879552 dihydrochloride

Modify Date: 2024-01-06 15:58:58

GSK2879552 dihydrochloride Structure
GSK2879552 dihydrochloride structure
Common Name GSK2879552 dihydrochloride
CAS Number 1902123-72-1 Molecular Weight 437.40
Density N/A Boiling Point N/A
Molecular Formula C23H30Cl2N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GSK2879552 dihydrochloride


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

 Names

Name GSK2879552 dihydrochloride

 GSK2879552 dihydrochloride Biological Activity

Description GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity[1][2].
Related Catalog
In Vitro 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]. Cell Viability Assay[2]. Cell Line: 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. Concentration: 0-10000 nM. Incubation Time: 6 days. Result: Inhibited cell proliferation. RT-PCR[1]. Cell Line: Resistant HCC cells (PLC/PRF/5 and Huh7). Concentration: 0, 1, 2 μM. Incubation Time: 24 h. Result: Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9,Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.
In Vivo GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice[2]. Animal Model: NCI-H526 and NCI-H1417 xenografts[2]. Dosage: 1.5 mg/kg. Administration: PO daily for 25-35 days. Result: There was 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 demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.
References

[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.

 Chemical & Physical Properties

Molecular Formula C23H30Cl2N2O2
Molecular Weight 437.40