GSK2879552 dihydrochloride
- Parent CAS: 1401966-69-5
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C23H28N2O2.2HCl
- MW: 437.4
Description
GSK2879552 is a first-in-class, orally bioavailable, potent, selective, and mechanism-based irreversible inhibitor of Lysine specific demethylase 1 (LSD1). LSDI, a histone H3K4me1/2 demethylase found in various transcriptional co-repressor complexes, including Histone Deacetylases (HDAC1/2) and Co-Repressor for Element-1-Silencing Transcription factor (CoREST). Studies have implicated that LSD1 is a key regulator of the epigenome that modulates gene expression through post-translational modification of histones and through its presence in transcriptional complexes, and is overexpressed in certain tumor cells. Inhibition of LSD1 enhances H3K4 methylation and increases the expression of tumor-suppressor genes.
More Information
| Parent CAS No. | 1401966-69-5 |
|---|---|
| Chemical Name | 4-((4-(((1R,2S)-2-Phenylcyclopropylamino)methyl)piperidin-1-yl)methyl)benzoic acid |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C=CC([C@H]2[C@H](NCC3CC[N@](CC4C=CC(C(O)=O)=CC=4)CC3)C2)=CC=1.Cl.Cl |&1:4,5,11,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C23H28N2O2/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)/t21-,22+/m0/s1 |
| InChiKey | LRULVYSBRWUVGR-FCHUYYIVSA-N |
| CID | 66571643 |
| Short Description | LSD1 inhibitor |
References
- M Huang et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Jul 10;398:12-21.
- HP Mohammad et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell. 2015 Jul 13;28(1):57-69.
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