| Bioactivity | PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC)[1]. |
| Invitro | PARP1/BRD4-IN-2 (compound BP44) can directly bind to BRD4 and PARP1 in MDA-MB-468 cells and improve their thermal stability[1].PARP1/BRD4-IN-2 has antiproliferative activity against MDA-MB-231 and MDA-MB-468 with IC50s of 6.61±0.58 μM and 3.01±0.83 μM, respectively[1].PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates Bcl-2 and up-regulates Bax and cleaved caspase3 at 20 μM; inhibits colony formation and promotes cell apoptosis in MDA-MB-468 cells[1].PARP1/BRD4-IN-2 (5, 10, and 20 μM) down-regulates DNA damage-related proteins CtIP, Mre11, Rad51, and p-RPA32 dose-dependently; causes DNA damage repair defects by down-regulating Rad51 and p-RPA32[1]. |
| Name | PARP1/BRD4-IN-2 |
| Formula | C25H20N4O4 |
| Molar Mass | 440.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |