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GSK-LSD1
Axon 2375
- Parent CAS: 1431368-48-7
- Optical Purity: Mixture of trans-diastereomers
- Soluble in water and DMSO
- MF: C14H20N2.2HCl
- MW: 289.24
Description
Irreversible inhibitor of the KDM1 family histone demethylase LSD1 (IC50 value 16 nM). GSK-LSD1 is >1000 fold selective over closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B), induces gene expression changes in cancer cell lines (average EC50 <5 nM), and inhibits cancer cell line growth (average EC50 <5 nM).
More Information
| Parent CAS No. | 1431368-48-7 |
|---|---|
| Chemical Name | rel-N-((1R,2S)-2-phenylcyclopropyl)piperidin-4-amine dihydrochloride |
| SMILES | [C@H]1(NC2CCNCC2)[C@H](C2C=CC=CC=2)C1.Cl.Cl |&1:0,8,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C14H20N2.2ClH/c1-2-4-11(5-3-1)13-10-14(13)16-12-6-8-15-9-7-12;;/h1-5,12-16H,6-10H2;2*1H |
| InChiKey | PJFZOGMSPBHPNS-UHFFFAOYSA-N |
| CID | 91826516 |
| Short Description | LSD1 inhibitor |
References
- O. Munoz et al. Aryl- and heteroarylcyclopropylamine compounds as LSD1 inhibitors and their preparation. PCT Int. Appl. (2013), WO 2013057320 A1 20130425.
- D.P. Mould et al. Reversible Inhibitors of LSD1 as Therapeutic Agents in Acute Myeloid Leukemia: Clinical Significance and Progress to Date. Med Res Rev. 2014 Nov 24.
- J. McGrath et al. Targeting histone lysine methylation in cancer. Pharmacol Ther. 2015 Jan 9. pii: S0163-7258(15)00003-0.
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