PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth[1].
PROTAC BRAF-V600E degrader-1 (compound 23) (1 nM-10 μM; 72 h) inhibits the cell viability of A375 and HT-29[1].
PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h or 0-24 h) inhibits p-ERK and BRAF-V600E protein in A375 cells[1].
Cell Viability Assay[1]
| Cell Line: | A375 and HT-29 |
| Concentration: | 1 nM-10 μM |
| Incubation Time: | 72 h |
| Result: | Inhibited the cell viability of A375 and HT-29 with IC50s of 46.5 nM and 51 nM. |
Western Blot Analysis[1]
| Cell Line: | A375 |
| Concentration: | 1, 4, 12, 37, 111, 333 and 1000 nM |
| Incubation Time: | 16 h or 0-24 h |
| Result: | Induced the reduction in the phosphorylation of ERK. Inhibited p-ERK and BRAF-V600E in a dose- and time-dependent manner. |
[1]. Han XR, et al. Discovery of Selective Small Molecule Degraders of BRAF-V600E. J Med Chem. 2020 Apr 23;63(8):4069-4080.