GSK2879552, LSD1 Inhibitor


Catalog No. size PriceQuantity
M60297-2S 2 mg solid $129
M60297-10S 10mg solid $516

Description

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.

Product information

CAS Number: 1902123-72-1

Molecular Weight: 437.40

Formula: C23H30Cl2N2O2

Related CAS Number:

1401966-69-5 (free base)

2002466-63-7 (2 HCl+4H2O)

1401966-63-9 (meso)

2121592-35-4 (meso, HCl)

Chemical Name: 4-((4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid hydrochloride

Smiles: Cl.Cl.OC(=O)C1=CC=C(CN2CCC(CN[C@@H]3C[C@H]3C3C=CC=CC=3)CC2)C=C1

InChiKey: QEKGSBZKRLHQSZ-VSIGASKDSA-N

InChi: InChI=1S/C23H28N2O2.2ClH/c26-23(27)20-8-6-18(7-9-20)16-25-12-10-17(11-13-25)15-24-22-14-21(22)19-4-2-1-3-5-19;;/h1-9,17,21-22,24H,10-16H2,(H,26,27);2*1H/t21-,22+;;/m0../s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM; Water up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

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.

References:

  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.

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

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