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GSK2879552 is a potent, selective, and irreversible inhibitor of Lysine Demethylase 1 (LSD1) through covalent modification of the LSD1 cofactor FAD (Ki = 1.7 μM). It demonstrates high selectivity for LSD1 over related enzymes such as LSD2, MAO-A, MAO-B, D-amino acid oxidase, and glutathione reductase. GSK2879552 has shown efficacy in inhibiting the proliferation of various cancer cell lines, including small cell lung carcinoma and AML cell lines.

1401966-69-5

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1401966-69-5 Usage

Uses

Used in Pharmaceutical Industry:
GSK2879552 is used as an inhibitor for Lysine Demethylase 1 (LSD1) for its potential role in the treatment of various types of cancer. Its high selectivity and potency make it a promising candidate for targeted cancer therapies.
Used in Cancer Research:
GSK2879552 is used as a research tool to study the role of LSD1 in cancer cell proliferation and the development of novel therapeutic strategies against cancer. Its effectiveness in inhibiting the growth of specific cancer cell lines provides valuable insights into the underlying mechanisms and potential applications in cancer treatment.
Used in Drug Development:
GSK2879552 serves as a lead compound in the development of new drugs targeting LSD1, which may have applications in the treatment of various cancers. Its unique properties and selectivity make it a valuable starting point for designing and optimizing new therapeutic agents.
Used in Drug Screening:
GSK2879552 is used in high-throughput screening assays to identify potential synergistic or antagonistic effects with other compounds, further enhancing its potential as a therapeutic agent in cancer treatment.
Used in Preclinical Studies:
GSK2879552 is utilized in preclinical studies to evaluate its safety, efficacy, and pharmacokinetics, providing essential data for the progression towards clinical trials and eventual application in cancer treatment.

in vitro

six days of gsk2879552 treatment resulted in potent anti-proliferative growth effects in 19 of 25 aml cell lines representing a range of aml subtypes. treating for longer time periods revealed sensitivity in all aml cell lines. aml blast colony forming ability was also inhibited in 4 of 5 bone marrow samples derived from primary aml patient samples [1].

in vivo

after 17 days of gsk2879552 treatment, control mice had 80% gfp+ cells in the bone marrow whereas treated mice had only 2.8% gfp positive cells, and the treated animals survived weeks beyond control mice [1].

References

1) Mohammad?et al.?(2015),?A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC; Cancer Cell?28?57

Check Digit Verification of cas no

The CAS Registry Mumber 1401966-69-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,0,1,9,6 and 6 respectively; the second part has 2 digits, 6 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1401966-69:
(9*1)+(8*4)+(7*0)+(6*1)+(5*9)+(4*6)+(3*6)+(2*6)+(1*9)=155
155 % 10 = 5
So 1401966-69-5 is a valid CAS Registry Number.

1401966-69-5Downstream Products

1401966-69-5Relevant academic research and scientific papers

The Degradation Chemistry of GSK2879552: Salt Selection and Microenvironmental pH Modulation to Stabilize a Cyclopropyl Amine

Campbell, John M.,Lee, Mei,Clawson, Jacalyn,Kennedy-Gabb,Bethune,Janiga, Ashley,Kindon, Leanda,Leach, Kevin P.

, p. 2858 - 2864 (2019/06/18)

The cyclopropyl amine moiety in GSK2879552 (1) degrades hydrolytically in high pH conditions. This degradation pathway was observed during long-term stability studies and impacted the shelf life of the drug product. This article describes the work to identify the degradation impurities, elucidate the degradation mechanism, and design a stable drug product. It was found that salt selection and control of the microenvironmental pH of the drug product formulation blend significantly improved the chemical stability of the molecule in the solid state.

Cyclopropylamines as LSD1 inhibitors

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Page/Page column 61, (2016/06/14)

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

LSD1 Fluorocyclopropylamine as inhibitor

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Paragraph 0207, (2016/10/09)

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

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