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GSK2879552 2HCl (1401966-69-5(free base))

Catalog No. T4418 CAS T4418

GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

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GSK2879552 2HCl (1401966-69-5(free base)) Chemical Structure

GSK2879552 2HCl (1401966-69-5(free base)), CAS T4418

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 78.00
5 mg	In stock	$ 111.00
10 mg	In stock	$ 185.00
25 mg	In stock	$ 308.00
50 mg	In stock	$ 433.00
100 mg	In stock	$ 642.00
500 mg	In stock	$ 1,370.00
1 mL * 10 mM (in DMSO)	In stock	$ 111.00

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Purity: 99.88%

Purity: 99.87%

Purity: 98.08%

Purity: 98%

Biological Description

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Storage & Solubility Information

Description	GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
Targets&IC50	LSD1:
In vitro	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
In vivo	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
Cell Research	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.

Molecular Weight	437.41
Formula	C23H30Cl2N2O2
CAS No.	T4418

Storage

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

Solubility Information

DMSO: 4.37 mg/mL (10 mM)

References and Literature

1. Huang M,etal.Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma.Cancer Lett. 2017 Jul 10;398:12-21. 2. Mohammad HP,etal.A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.Cancer Cell. 2015 Jul 13;28(1):57-69.

Citations

1. Lv S, Zhao X, Zhang E, et al. Lysine demethylase KDM1A promotes cell growth via FKBP8-BCL2 axis in hepatocellular carcinoma. Journal of Biological Chemistry. 2022: 102374.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Clinical Compound Library Bioactive Compound Library Bioactive Compounds Library Max Epigenetics Compound Library Chromatin Modification Compound Library

Related Products

Related compounds with same targets

LSD1-IN-5 KDM2B-IN-2 LSD1-IN-6 T-448 free base Iadademstat dihydrochloride OG-L002 GSK467 KDM2A/7A-IN-1

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Keywords

GSK2879552 2HCl (1401966-69-5(free base)) T4418 Chromatin/Epigenetic Histone Demethylase GSK2879552 2HCl (1401966 69 5(free base)) GSK2879552 2HCl (1401966695(free base)) GSK-2879552 2HCl (1401966-69-5(free base)) inhibitor inhibit

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