Name | PROTAC BRAF-V600E degrader-1 |
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Description | 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]. |
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Related Catalog | |
Target |
BRAF-V600E:2 nM (Kd) Braf:2.4 nM (Kd) |
In Vitro | 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. |
References |
Molecular Formula | C48H54F2N10O10S |
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Molecular Weight | 1001.07 |