| Identification | Back Directory | [Name]
KDOAM-25 | [CAS]
2230731-99-2 | [Synonyms]
KDOAM-25
KDOAM-25 trihydrochloride
4-Pyridinecarboxamide, 2-[[[2-[[2-(dimethylamino)ethyl]ethylamino]-2-oxoethyl]amino]methyl]- | [Molecular Formula]
C15H25N5O2 | [MDL Number]
MFCD30146416 | [MOL File]
2230731-99-2.mol | [Molecular Weight]
307.39 |
| Hazard Information | Back Directory | [Uses]
KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells[1]. | [Biochem/physiol Actions]
KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM. JARID1A and JARID1B are independently overexpressed in some cancers with JARID1B (KDM5B, PLU1) also identified as a potential oncogene, a repressor of tumour repressor genes. JARID1C (KDM5C) and JARID1D (KDM5D) are located on the X- and Y-chromosomes respectively. KDOAM25′s closest off-target is JMJD2C (selectivity >400 fold). It shows no activity on other tested 2-OG family members, including FIH, NO66, MINA53 and PHD2. KDOAM25 is active in cells. | [References]
[1] Tumber A, et al. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol. 2017 Mar 16;24(3):371-380. DOI:10.1016/j.chembiol.2017.02.006 |
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