| Identification | Back Directory | [Name]
GSK2879552 | [CAS]
1401966-69-5 | [Synonyms]
CS-1621
GSK2879552
GSK2879522
GSK-2879552;GSK 2879552
LSD1 inhibiror GS2879552
GSK2879552 DIHYDROCHLORIDE
4-[[4-[[((1R,2S)-2-Phenylcyclopropyl)amino]methyl]piperidin-1-yl]methyl]benzoic acid
Benzoic acid, 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]- | [Molecular Formula]
C23H28N2O2 | [MOL File]
1401966-69-5.mol | [Molecular Weight]
364.48 |
| Chemical Properties | Back Directory | [Boiling point ]
534.2±50.0 °C(Predicted) | [density ]
1.20±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 25 mg/ml) or in Water (up to at least 25 mg/ml) | [form ]
solid | [pka]
4.03±0.10(Predicted) | [color ]
White | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
GSK2879552 (1401966-65-5, free base) is potent, selective, and irreversible inhibitor of Lysine Demethylase 1 (LSD1) via covalent modification of the LSD1 cofactor FAD (Ki = 1.7 μM). It is selective for LSD1 over the closely related LSD2, MAO-A, MAO-B, and the FAD dependent enzymes D-amino acid oxidase and glutathione reductase. Tested against a panel of 165 cancer cell lines, GSK2879552 inhibited the proliferation of 9 small cell lung carcinoma lines and 20 AML cell lines. | [Uses]
GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity[1][2]. | [Definition]
ChEBI: GSK2879552 is a member of the class of piperidines that is piperidine substituted by (4-carboxyphenyl)methyl and {[(1R,2S)-2-phenylcyclopropyl]amino}methyl groups at positions 1 and 4, respectively. It is a potent and irreversible inhibitor of lysine specific demethylase 1 (LSD1, also known as KDM1A). It was under clinical investigation for the treatment of acute myeloid leukaemia and small cell lung carcinoma. It has a role as an EC 1.14.99.66 (lysine-specific histone demethylase 1A) inhibitor and an antineoplastic agent. It is a member of benzoic acids, a monocarboxylic acid, a member of piperidines, a member of cyclopropanes, a tertiary amino compound, a secondary amino compound and a member of benzenes. | [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]. | [IC 50]
KDM1/LSD1 | [References]
1) Mohammad?et al.?(2015),?A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC; Cancer Cell?28?57 |
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| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Telephone: |
020-13556033878 2965585218 13556033878 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList15061/0_EN.htm |
| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
| Company Name: |
parabiochem
|
| Telephone: |
025-83453382-8005 |
| Website: |
www.parabiochem.cn |
|