Cas No.: | |
Chemical Name: | KDOAM25(GTPL8576) |
Synonyms: | KDOAM-25; KDOAM 25; KDOAM25; GTPL8576; GTPL-8576; GTPL 8576; LQT. |
SMILES: | O=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)N |
Formula: | C15H25N5O2 |
M.Wt: | 307.398 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | KDOAM-25, also known as GTPL8576, is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM. KDOAM-25 Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. KDOAM-25 shows biochemical half maximal inhibitory concentration values of <100 nM for KDM5A-D in vitro, high selectivity toward other 2-OG oxygenases sub-families, and no off-target activity on a panel of 55 receptors and enzymes. In human cell assay systems, KDOAM-25 has a half maximal effective concentration of ∼50 μM and good selectivity toward other demethylases. |