SGC0946 - DOT1L inhibitor. CAS# 1561178-17-3 60287 acting as an antagonist of

acting as an antagonist of Smoothened

InChi: InChI=1S/C22H20F5N3O3/c1-20(2

6-dichloro-1H-indole-3-propanoic acid

1154097-71-8

b-AP15 was dosed to mice with HCT-116 colon carcinoma xenografts by intraperitoneal injection at 5 mg/Kg

SGC0946 - DOT1L inhibitor. CAS# 1561178-17-3 60287 acting as an antagonist ofSGC0946, 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,