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编 号：F751562
分子式：C33H40N6O4
分子量：584.71
分子式：C33H40N6O4
分子量：584.71
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CAS No: 2366272-43-5
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生物活性：
(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882.
体外研究：
(4aS,8aR)-NPD-001 (compound 2) (60 μM) disrupts DNMT3A-DNMT3L interactions at the DNMT3A tetramer interface, inhibits the stimulation of DNMT3A_WT activity by DNMT3L, but does not inhibit the activation of DNMT3A_WT by H3 peptides.(4aS,8aR)-NPD-001 (0-120 μM, 100 min) inhibits the activation of DNMT3A_R882H by DNMT3L.(4aS,8aR)-NPD-001 (0-30 μM, 72 h) induces apoptosis and and differentiation in AML cell lines in a concentration-dependent manner.(4aS,8aR)-NPD-001 (5 μM, 20 days) leads to a time-dependent decrease of global 5-methylcytosine.
(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882.
体外研究：
(4aS,8aR)-NPD-001 (compound 2) (60 μM) disrupts DNMT3A-DNMT3L interactions at the DNMT3A tetramer interface, inhibits the stimulation of DNMT3A_WT activity by DNMT3L, but does not inhibit the activation of DNMT3A_WT by H3 peptides.(4aS,8aR)-NPD-001 (0-120 μM, 100 min) inhibits the activation of DNMT3A_R882H by DNMT3L.(4aS,8aR)-NPD-001 (0-30 μM, 72 h) induces apoptosis and and differentiation in AML cell lines in a concentration-dependent manner.(4aS,8aR)-NPD-001 (5 μM, 20 days) leads to a time-dependent decrease of global 5-methylcytosine.
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