| Bioactivity | MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo[1]. |
| Invitro | MIR002 (24 h) shows antiproliferative activity at nanomolar concentrations (IC50s of 0.25, 2.8, 0.6, 0.41 µM in NCI-H460, H460-R9A, A2780, A2780-DX; IC50s of 0.9, 1.2, 0.22, 0.71, 2.1, 0.52, 0.038, 0.18, 0.42, 1.9, 0.64, 1.1 µM in MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells, respectively)[1].MIR002 (0.0001,0.01, 1, 10 µM) shows inhibitory activity on HDAC11 with an IC50 of 6.09 µM[1]. MIR002 (0.1, 0.25, 0.4 µM, 24 h) shows a dose-dependent p53 acetylation and p21 induction as well as H2AX Phosphorylation[1].MIR002 (72 h) leads to cell cycle arrest at the G1-S phase[1]. Cell Proliferation Assay[1] Cell Line: |
| Name | MIR002 |
| CAS | 2217671-64-0 |
| Formula | C27H29NO5 |
| Molar Mass | 447.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |