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15(1):39-48
Smiles: COC1=CC=CC=C1C(=O)NC1=CC2=C(C=C1N1CCCCC1)N(C)C(=O)N2C
It inhibited the activity of human PRC2-containing wild-type EZH2 with an inhibition constant (Ki) value of 2
Smiles: O=C(COC1C=CC(=CC=1)C(=O)C1C=CC=CC=1)NC1CCN(CC2C=CC=CC=2)CC1
CAS Number: 147591-46-6
IDH-C227 - IDH1 Inhibitor. CAS# 1355324-14-9 0232 15(1):39-48IDH C227, CAS No. 1355324 14 9, is a potent and selective IDH1 R132H inhibitor first reported in patent WO2012009678. It can inhibit the enzymatic activity of IDH1 R132H in vitro with an IC50 < 0. 1 M, and 2 HG production in HT1080 and U87MG cells with IC50 < 0. 25 M. Because the mutated form of IDH1 produces the metabolite, 2 hydroxyglutarate (2HG), which may contribute to the formation and malignant progression of gliomas as well as other forms of
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