| Bioactivity | TP-472 is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7[1][2]. TP-472 induces apoptosis of melanoma cells[3]. | ||||||||||||
| Invitro | TP-472 (1 µM, 3 µM; 24-216 hours) yields concentration-dependent growth defects in ESCs[2].TP-472 (0.1-10 μM; 24 h) effectively inhibits the growth of both the BRAF mutant melanoma cell lines at 5 and 10 µM concentrations[3].TP-472 (for 2 weeks) also strongly inhibits the long-term survival of multiple melanoma cell lines (M14, SKMEL-28, A375, and A2058) at concentrations of 5 and 10 µM[3].TP-472 (5-10 μM; 24 h) treatment downregulates genes encoding various extracellular matrix (ECM) proteins, including integrins, collagens, and fibronectins in A375 cells[3].TP-472 (0.1-10 μM; 24 h) results in the upregulation of pro-apoptotic genes (BAX, MDM2, CDKN1A) in A375 cells[3]. Cell Viability Assay[2] Cell Line: | ||||||||||||
| Name | TP-472 | ||||||||||||
| CAS | 2079895-62-6 | ||||||||||||
| Formula | C20H19N3O2 | ||||||||||||
| Molar Mass | 333.38 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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