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and has weaker activity against monoamine oxidase proteins MAO-A and MAO-B with IC50 ~0
It potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Kiapp 0
Right now MK-1775 is in phase I/II clinical trials for various cancers
InChi: InChI=1S/C26H29NO2/c1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h5-17
Bromosporine shows moderate cytotoxicity in HeLa cells at 18 µM
(R)-2-HG - a-KG-dependent dioxygenases inhibitor. CAS# 103404-90-6 60225 and has weaker activity againstMutations, CAS No. 103404 90 6, in IDH1 and IDH2, the genes coding for isocitrate dehydrogenases 1 and 2, are common in several human cancers, such as leukemia and glioma, and result in overproduction of the (R) enantiomer of 2 hydroxyglutarate [(R) 2 HG]. Elucidation of the role of IDH mutations and (R) 2 HG in leukemogenesis has been hampered by a lack of appropriate cell based models. It has been recently reported that a canonical IDH1 mutant, IDH1
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