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GSK2879552, LSD1 Inhibitor

GSK2879552, LSD1 Inhibitor

$129.00
A highly potent, selective and orally bioavailable irreversible inhibitor of Lysine Specific Demethylase 1 (LSD1).
Catalog No. Unit Price Qty
M60297-2s 2 mg solid $129.00

Details

Product Information
Molecular Weight: 437.41
Formula: C23H28N2O2.2HCl
Purity: ≥98%
CAS#: 1401966-69-5
Solubility: DMSO up to 50 mM; Water up to 50 mM
Chemical Name: 4-((4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid hydrochloride
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

GSK2879552 is a highly potent, selective and orally bioavailable irreversible inhibitor of Lysine Specific Demethylase 1 (LSD1). It is highly selective over related enzymes such as MAO-A/B. A proliferation screen of cell lines representing a number of tumor types indicated that small cell lung carcinoma (SCLC) is sensitive to GSK2879552’s inhibition. It increases H3K4 methylation selectively at genomic regions bound by LSD1. It demonstrates efficacy in preclinical models of SCLC. Currently GSK2879552 is in phase I clinical trials targeting Acute Myeloid Leukemia (AML) and Relapsed/Refractory Small Cell Lung Carcinoma. 

How to Use:

In vitro: GSK2879552 was used at 1 µM in vitro and cellular assays.
In vivo: GSK2879552 was orally dosed to mice at 1.5-10 mg/Kg once per day.

Reference:

  • 1. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. (2015) Cancer Cell. 28(1):57-69. 
  • 2. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. (2015) Epigenomics. 7(4):609-26.

GSK2879552_spec.pdf       
GSK2879552_MSDS.pdf 

Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 437.41
Formula: C23H28N2O2.2HCl
Purity: ≥98%
CAS#: 1401966-69-5
Solubility: DMSO up to 50 mM; Water up to 50 mM
Chemical Name: 4-((4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid hydrochloride
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

GSK2879552 is a highly potent, selective and orally bioavailable irreversible inhibitor of Lysine Specific Demethylase 1 (LSD1). It is highly selective over related enzymes such as MAO-A/B. A proliferation screen of cell lines representing a number of tumor types indicated that small cell lung carcinoma (SCLC) is sensitive to GSK2879552’s inhibition. It increases H3K4 methylation selectively at genomic regions bound by LSD1. It demonstrates efficacy in preclinical models of SCLC. Currently GSK2879552 is in phase I clinical trials targeting Acute Myeloid Leukemia (AML) and Relapsed/Refractory Small Cell Lung Carcinoma. 

How to Use:

In vitro: GSK2879552 was used at 1 µM in vitro and cellular assays.
In vivo: GSK2879552 was orally dosed to mice at 1.5-10 mg/Kg once per day.

Reference:

  • 1. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. (2015) Cancer Cell. 28(1):57-69. 
  • 2. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. (2015) Epigenomics. 7(4):609-26.

GSK2879552_spec.pdf       
GSK2879552_MSDS.pdf 

Products are for research use only. Not for human use.

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