| Bioactivity | (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[1]. |
| Invitro | (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[1].(4aS,8aR)-NPD-001 (0-120 μM, 100 min) inhibits the activation of DNMT3A_R882H by DNMT3L[1].(4aS,8aR)-NPD-001 (0-30 μM, 72 h) induces apoptosis and and differentiation in AML cell lines in a concentration-dependent manner[1].(4aS,8aR)-NPD-001 (5 μM, 20 days) leads to a time-dependent decrease of global 5-methylcytosine[1]. Apoptosis Analysis[1] Cell Line: |
| Name | (4aS,8aR)-NPD-001 |
| CAS | 2366272-43-5 |
| Formula | C33H40N6O4 |
| Molar Mass | 584.71 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |