Braftide

Description: Braftide is an allosteric inhibitor of BRAF kinase that exerts its effect by targeting the surface of BRAF kinase dimers, thereby preventing their formation. It inhibits both wild-type BRAF and oncogenic BRAFG469A, with IC50 values of 364 nM and 172 nM, respectively. When combined with the TAT sequence, Braftide can suppress the MAPK signaling pathway, inhibiting the proliferation of KRAS-mutant tumor cells, with EC50 values of 7.1 µM for HCT116 and 6.6 µM for HCT-15. Target: Raf, Kras, Ras. Smiles: [C@@H](CC1=CN=CN1)(NC([C@@H](NC([C@H]([C@@H](C)O)N)=O)CCCNC(=N)N)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H](CCSC)C(O)=O)=O)=O)CC(C)C)=O)CC(C)C)=O)[C@H](CC)C)=O)CC(N)=O)=O)[C@H](C)C)=O