SGC0946 - DOT1L inhibitor. CAS# 1561178-17-3 60287 Epigenetic compounds library of Hypoxia

Epigenetic compounds library of Hypoxia Inducible Factor

The overexpression of KDM4A/KDM4B in prostate cancer and their association with androgen receptor suggest that KDM4A/KDM4B are potential progression factors for prostate cancer

InChi: InChI=1S/C22H20F5N3O3/c1-20(2

1154097-71-8

Smiles: O=C(C1C=CC(F)=CC=1)N1C[C@H](CCC1)C1=NC(=NO1)C1C=CC(F)=CC=1

SGC0946 - DOT1L inhibitor. CAS# 1561178-17-3 60287 Epigenetic compounds library of HypoxiaSGC0946, CAS No. 1561178 17 3, is a highly potent and selective inhibitor of DOT1L methyltransferase. It selectively blocks binding of the cofactor, S adenosylmethionine, to DOT1L, and inhibits the enzyme with an IC50 of 0. 3 nM in a radioactive enzyme assay and is over 100 fold selective for other histone methyltransferases HMTs. SGC0946 potently reduces H3K79 dimethylation with cellular IC50 of 2. 6 nM in A431 cells, and 8. 8 nM in MCF10A cells,